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Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Developing a PROTAC to Degrade the Constitutively Active Onco-GPCR in Uveal Melanoma Date & Time Friday, November 3rd / 4:20 PM About Victoria Rasmussen "Victoria Rasmussen is a graduate fellow in Dr. Thomas Sakmar’s laboratory at Rockefeller University, where she studies the signaling and degradation of G protein-coupled receptors. She completed her undergraduate education at Providence College, receiving a B.S. in Biology and a B.A. in Psychology. During her time at Providence College, she received the Walsh Grant Fellowship to develop novel methods of synthesizing 2-imidazoline scaffolds to be used as proteasome modulators in the laboratory of Travis Bethel. Victoria started her Ph.D. at the Tri-Institutional Ph.D. program in Chemical Biology, where she joined the lab of Thomas Sakmar at Rockefeller University. She is currently working to understand the signaling and degradation of GPCRs in disease states to help test the feasibility of using protein-targeted degradation as a therapeutic strategy. " Victoria Rasmussen on the web Tri-Institutional PhD Program Chemical Biology LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Leaving for City Center Coming Soon < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Leave for dinner reception Coming Soon < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Student Flash Presentations Health and Disease, Metabolism, Nervous System, Proteomics and Transcriptomics, Receptor Structure, Signaling and Activation Mechanism Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Abhishek Kumar Singh Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Alex Torrelli-Diljohn GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Emmanouil Kyrloglou A single cell GPCR map of thermogenic fat Vasiliki Karagiannakou GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Lara-Sophie Brodmerkel Novel isoforms of adhesion G protein coupled receptor B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Rashed Rezwan Parag Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Hailey Steichen Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tyler Bernadyn Next Generation MBD2 inhibitors for Brain Cancer Therapy Jesse Stillwell Adgrg6/Gpr126 is Required for Myocardial Notch Activity and N-cadherin Localization to Attain Trabecular Identity Abhishek Kumar Singh Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Srivastava, Swati1; Singh, Abhishek Kumar1; Gunawan, Felix2; Gentile, Alessandra2; Petersen, Sarah C.3; Stainier, Didier Y.R.2; Engel, Felix B.1 1 Experimental Renal and Cardiovascular Research, Department of Nephropathology, Institute of Pathology, Friedrich-Alexander-Universität Erlangen-Nürnberg, Kussmaulallee 12, 91054 Erlangen, Germany 2 Developmental Genetics, Max-Planck-Institute for Heart and Lung Research, Ludwigstrasse 43, 61231 Bad Nauheim, Germany 3 Department of Developmental Biology, Washington University in St. Louis, 660 S. Euclid Ave, St. Louis, MO 63108, USA. Present address: Department of Neuroscience, Kenyon College, 203 North College Road, Gambier, OH 43022, USA" About Abhishek Kumar Singh "I am a doctoral student in the lab of Prof. Felix B. Engel. Since my undergraduate studies, I became fascinated with the class of adhesion GPCRs, owing to their potential, scarcity of knowledge on them, diverse expression profile, and the complexity with which they seem to be working. This made me pursue my higher education in the field of adhesion GPCRs. Accordingly, I worked with Prof. Hsi-Hsien Lin as summer intern twice, and finally joined the lab of Prof. Engel. I hope to develop my skillsets so as to be able to establish my own lab in future to work on adhesion GPCRs employing highly interdisciplinary field." Abhishek Kumar Singh on the web Uniklinikum Erlangen Google Scholar X (Twitter) Investigating The Role of ADGRB3 Loss of Expression in Brain Tumor Formation in Li-Fraumeni Syndrome Alex Torrelli-Diljohn Abstract "Li-Fraumeni syndrome (LFS) is a rare cancer predisposition syndrome caused by a germline mutation in the TP53 tumor suppressor gene. Glioblastoma (GBM) is the most prevalent central nervous system tumor in LFS, with TP53 mutations detected in 30% of sporadic GBMs. GBM is the most aggressive primary brain neoplasm that affects adults, with a median survival of 12-15 months. Recent studies implicate the dysregulation of adhesion G-Protein coupled receptors (GPCRs) in GBM development. Brain angiogenesis inhibitor 3 (BAI3/ADGRB3), a member of the BAI1-3 subfamily of adhesion GPCRS, has been observed to have low expression in brain tumors according to TCGA data, but the significance of this observation has not been explored. However, while its sister protein BAI1 has demonstrated tumor suppressor functions in the brain, it remains unclear whether BAI3 shares this role. To test this, an LFS mouse model (germline Tp53 deletion) with a second floxed allele under the control of Nestin-Cre was crossed to Bai3-/- mice. Preliminary findings indicate that the simultaneous loss of Bai3 and Tp53 expression in our mouse model increased spontaneous brain tumor formation incidence from 34% to 71%, in contrast to the loss of p53 alone. These observations lead me to hypothesize that ADGRB3 functions as a tumor suppressor in the brain, and its silencing, in the context of p53 mutation, facilitates GBM formation. Isolated GBM stem cells were collected for further genomic analyses and to test whether overexpression of BAI3 will save the tumor phenotype." Authors & Affiliations "Vukadin L, Park B, Mohamed M, Li H, Elkholy A, Torrelli-Diljohn A, Kim JH, Jeong K, Murphy JM, Harvey CA, Dunlap S, Gehrs L, Lee H, Kim HG, Sah JP, Lee SN, Stanford D, Barrington RA, Foote JB, Sorace AG, Welner RS, Hildreth BE 3rd, Lim SS, Ahn EE. A mouse model of Zhu-Tokita-Takenouchi-Kim syndrome reveals indispensable SON functions in organ development and hematopoiesis. JCI Insight. 2024 Mar 8;9(5):e175053. doi: 10.1172/jci.insight.175053. PMID: 38290089; PMCID: PMC10972584. University of Alabama at Birmingham" About Alex Torrelli-Diljohn "Alex completed his undergraduate & master’s degrees in Neurobiology & Cognitive sciences from the University of South Florida, where he researched early-onset Alzheimer’s disease in the lab of Dr. Angele Parent. He is interested in working on Li-Fraumeni syndrome and helping patients afflicted with this condition. He is also interested in working on Glioma Brain Organoid models." Alex Torrelli-Diljohn on the web The University of Alabama at Birmingham LinkedIn GPR124 Mediates Adhesion Of Leukemic Stem Cells To Their Niche And Leads To Myeloid Skewing Emmanouil Kyrloglou Abstract Only available for AGPCR 24 Workshop Attendees About Emmanouil Kyrloglou "Studied medicine at the University of Groningen. Now PhD-candidate at the Experimental Hematology lab of the University Medical Center Groningen (UMCG)." Emmanouil Kyrloglou on the web Adhesion GPCR Consortium LinkedIn A single cell GPCR map of thermogenic fat Vasiliki Karagiannakou Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Karagiannakou Vasiliki, El Merahbi Rabih, Herzig Stephan , Georgiadi A , Helmholtz Center Munich, Institute of Diabetes and Cancer" About Vasiliki Karagiannakou "MSc in Bioinformatics, PhD student since 2022 in the Institute for Diabetes and Cancer IDC, Helmholtz Centre Munich" Vasiliki Karagiannakou on the web Helmholtz Centre Munich GAIN Domain Dynamics And Its Relevance For Adhesion GPCR Signaling In Vivo Lara-Sophie Brodmerkel Abstract "Over the last years, Adhesion G Protein-coupled receptors (aGPCR) have been shown to play a crucial role in the perception of mechanical signals. However, the molecular details underlying their activation and how mechanical forces are translated into an intracellular response remains largely unknown. Recent Molecular Dynamics (MD) simulations of several aGPCRs predicted two flexible regions, termed flaps, located within the GPCR autoproteolysis inducing (GAIN) domain. These flaps could theoretically enable partial decryption of the Stachel through lateral movement and affect activation of the receptor independent of NTF-CTF dissociation. However, the physiological relevance of flap flexibility on receptor activation and signaling remains unclear. To investigate whether flexibility of GAIN flaps affects aGPCR function under native conditions, we strategically inserted specific mutations into the GAIN domain of the Latrophilin homologue Cirl in Drosophila melanogaster, with the intention to alter flap dynamics. Our goal is to understand if and how flap dynamics influence Cirl function and consequently the mechanosensory faculty of neurons in vivo. To this end, we combine behavioral, biochemical, immunohistochemical and functional readouts, with the overarching ambition to expand our knowledge on the mechanistic details underlying aGPCR activation in mechanosensation." Authors & Affiliations "Brodmerkel Lara-Sophie 1, Bormann Anne 1, Seufert Florian 2, Hildebrand Peter 2,3 ´, Ljaschenko Dmitrij 1´, Scholz Nicole 1´ 1Rudolf Schönheimer Institute of Biochemistry, Division of General Biochemistry, Medical Faculty, Leipzig University, Leipzig, Germany 2Institute for Medical Physics and Biophysics, Medical Faculty, Leipzig University, Leipzig, Germany 3Institute of Medical Physics and Biophysics, Charité – Universitätsmedizin Berlin, Berlin, Germany ´ correspondence: scholzlab@gmail.com , Dmitrij.Ljaschenko@medizin.uni-leipzig.de , peter.hildebrand@medizin.uni-leipzig.de *contributed equally" About Lara-Sophie Brodmerkel "I am a medical student and I´m currently working on my MD thesis in the lab of Dr. Nicole Scholz. We are investigating the relevance of GAIN domain dynamics for aGPCR signaling in Drosophila melanogaster." Lara-Sophie Brodmerkel on the web University of Leipzig Novel isoforms of adhesion GPCR B1 (ADGRB1/BAI1) generated from an alternative promoter in intron 17 Rashed Rezwan Parag Abstract "Brain-specific angiogenesis inhibitor 1 (BAI1) belongs to the adhesion G-protein-coupled receptors, which exhibit large multi-domain extracellular N-termini that mediate cell-cell and cell-matrix interactions. To explore the existence of BAI1 isoforms, we queried genomic datasets for markers of active chromatin and new transcript variants in the ADGRB1 (adhesion G protein-coupled receptor B1) gene. Two major types of mRNAs were identified in human/mouse brain, those with a start codon in exon 2 encoding a full-length protein of a predicted size of 173.5/173.3 kDa and shorter transcripts starting from alternative exons at the intron 17/exon 18 boundary with new or exon 19 start codons, predicting shorter isoforms of 76.9/76.4 and 70.8/70.5 kDa, respectively. Immunoblots on wild-type and Adgrb1 exon 2-deleted mice, reverse transcription PCR and promoter-luciferase reporters confirmed that the shorter isoforms originate from an alternative promoter in intron 17. The shorter BAI1 isoforms lack most of the N-terminus and are very close in structure to the truncated BAI1 isoform generated through GPS processing from the full-length receptor. The cleaved BAI1 isoform has a 19 amino acid extracellular stalk that can serve as a receptor agonist, while the alternative transcripts generate BAI1 isoforms with extracellular N-termini of 5 or 60 amino acids. Further studies are warranted to compare the functions of these isoforms and examine the distinct roles they play in different tissues and cell types." About Rashed Rezwan Parag "Rashed is from Bangladesh. He has received his BSc and MS degree from the Department of Biochemistry and Molecular Biology, University of Chittagong, Bangladesh. Before joining UAB as a graduate student, he worked in the EuGEF Research Group to identify novel prognostic biomarkers and therapeutic options for Metastatic Breast Cancer (BC) and Head and Neck Squamous Cell Carcinoma (HNSCC). Currently, he is working to elucidate the role of ADGRB1 and ADGRB3 in medulloblastoma (pediatric brain tumor)." Rashed Rezwan Parag on the web Google Scholar Identification of Differentially Expressed Gpr116 (Adgrf5) Transcript Variants in Mouse Kidney Hailey Steichen Abstract "Adhesion G protein-coupled receptors (aGPCRs) are important and understudied modulators of physiological processes. Previous work suggests that aGPCRs, and Adgrf5 in particular, undergo significant tissue-specific mRNA processing that results in holoreceptors with unique and variable N-terminal structures (Knierim et al. 2019). Recently, it was shown that transcripts of the postsynaptic aGPCR Latrophilin-3 (Lphn3/Adgrl3) undergo physiologically relevant alternative splicing, which determined heterotrimeric signaling through Gαs- or Gα12/13- mediated pathways (Südhof et al. 2024). These results demonstrate that identifying precise, tissue-specific transcript variants is critical to understanding the physiological relevance of aGPCRs. Moreover, these studies highlight the possibility that tissue expression of single aGPCRs is likely comprised of multiple transcript variants. We previously demonstrated that kidney-specific Adgrf5/Gpr116 knockout causes luminal membrane accumulation of V-ATPase in acid-secreting A-type intercalated cells (AICs) in the collecting ducts and a significant reduction in urine pH (Zaidman et al. 2020). Renal Adgrf5 is restricted to two distinct populations of cells: AICs and endothelial cells (ECs). We hypothesized that cell-specific Adgrf5 transcript variants are expressed in renal AICs and ECs, and therefore are activated by distinct mechanisms unique to the cellular microenvironment. We detected and aligned three Adgrf5 exons that undergo differential expression in the kidney: exons 2, 12, and 22. Adgrf5 transcripts in FACS-sorted GFP+ ICs do not contain the exon 2 variable region, or the alternative exons 12 and 22, while ECs contain all three. However, EC markers were detected in GFP+ ICs, demonstrating some EC contamination in the sorted ICs. Detection of transcripts that do, and do not, contain multiple variable regions suggests expression of multiple mRNAs in specific cells. These data demonstrate that Adgrf5 transcript variants are cell-specific in the kidney. Moreover, the complete repertoire of aGPCRs expressed in the kidney is undefined. We performed single-nucleus RNA sequencing on male and female kidneys. snRNAseq revealed abundant, cell-specific expression of six aGPCRs (Adgrl4, Adgre5, Adgrf1, Adgrf5, Adgrg1, and Adgrg3). Detection of these, as well as 18 other aGPCRs, was confirmed by PCR screening for GAIN/GPS domains on cDNA from whole-kidney lysates. These results reveal the complete set of aGPCRs expressed in the murine kidney. Future studies will focus on determining the physiological roles and tissue-specific variants of these receptors." Authors & Affiliations "Department of Biochemistry & Molecular Biology, University of New Mexico Health Sciences Center Xue, Jianxiang; Yan, Teagan; Eaton, Krystin, and Zaidman, Nathan" About Hailey Steichen "I currently work in Dr. Nathan Zaidman’s lab at the University of New Mexico Health Sciences Center. I am researching the physiological relevance of Adgrf5 (Gpr116) transcript variants in specific cell types in the kidney. I have also worked in the laboratory of Dr. James Bridges at National Jewish Health in Denver, CO researching molecular mechanisms of lung injury and repair mediated by Adgrf5. I received my MS in Applied Toxicology from the University of Washington, and my BA in Biology from Vassar College." Hailey Steichen on the web Zaidman Physiology Lab Elucidating The Role Of GPR97/ADGRG3 In Neutrophil Biology Tyler Bernadyn Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Gandhi, Riya; Chandan, Nancy; Kwarcinski, Frank; Smrcka, Alan; and Tall, Gregory G." About Tyler Bernadyn "4th year Pharmacology Ph.D. Student in Greg Tall's Lab." Tyler Bernadyn on the web LinkedIn Next Generation MBD2 inhibitors for Brain Cancer Therapy Jesse Stillwell Abstract "Medulloblastoma (MB) is one of the most lethal pediatric brain tumors. Standard of care for MB includes tumor resection, chemotherapy, and cranio-spinal radiation. This regimen has long lasting side-effects, including neuroendocrine and cognitive problems, and ~ 30% of patients still do not survive 5 years past diagnosis. Clearly, a new, less toxic therapeutic is needed. Our lab has previously shown that expression of adhesion GPCR BAI1 (ADGRB1) is lost by epigenetic silencing in MB. Restoration of ADGRB1 expression slowed tumor growth and improved survival in mice bearing MB xenografts. The ADGRB1 promoter is methylated in MB, and this allows for Methyl CpG Binding Domain protein 2 (MBD2) to silence the gene through recruitment of the NuRD silencing complex. KCC-07 is an inhibitor that prevents MBD2 from binding to DNA, allowing re-expression of BAI1. To further optimize the chemical scaffold, we synthesized KCC07 analogs that we’re testing for their ability to reactivate BAI1 expression. The current methods for testing KCC-07’s ability to reactivate ADGRB1 expression involve western blotting and RT-qPCR, both of which are semi-quantitative methods that require large numbers of cells and high volumes of analogs, creating a bottleneck in screening. These methods are time consuming, and their inherent variability makes precise quantification difficult. This research focuses on the design of a new endogenous ADGRB1 activation reporter assay to test analogs faster and with more reproducibility." Authors & Affiliations "Erwin Van Meir, University of Alabama at Birmingham/Sadanandan Velu, University of Alabama at Birmingham/Takahiro Yamamoto, Kumamoto University" About Jesse Stillwell "Jesse Stillwell is a 3rd year graduate student with a research focus in drug development. His project is drug discovery focused, with particular interest in use of a novel epigenetic therapy to reactivate ADGRB1 expression." Jesse Stillwell on the web Van Meir Lab – Heersink School of Medicine < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VIII * Physiological and pathological roles of AGPCRs in the periphery The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Tobias Langenhan Characterization of Phenotypes Associated with GPR110 Deletion Hee-Yong Kim The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alain Garcia De Las Bayonas Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Gabriela Aust The CELSR/ADGRC Homolog Flamingo Is Not Autoproteolytically Processed By The GAIN Domain Tobias Langenhan Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Tobias Langenhan, Nicole Scholz, Genevieve M. Auger, Helen Strutt, David Strutt" About Tobias Langenhan "1997-2004: Medical school and Dr. med. Neuroanatomy (Würzburg, Germany); 2004-2005: M.Sc. Neuroscience (Oxford, UK); 2005-2009: D.Phil. Neuroscience (Oxford, UK); 2009-2016: Group leader, Institute of Neurophysiology (Würzburg, Germany); 2016: Heisenberg professorship (Würzburg, Germany); 2016-to date: Professor and Chair in Biochemistry (Leipzig, Germany)" Tobias Langenhan on the web Langenhan Lab LinkedIn Characterization of Phenotypes Associated with GPR110 Deletion Hee-Yong Kim Abstract "G-protein coupled receptor 110 (ADGRF1, GPR110), an adhesion GPCR recently deorphanized, plays an important role in in the development of neurons and cognitive function. Synaptamide, an endogenous ligand for GPR110, binds to the N-terminal G-protein autoproteolysis-inducing (GAIN) domain of GPR110, and activates GPR110/cAMP signaling. This activation promotes neurogenic differentiation of neural stem cells, neurite growth, and synaptogenesis of developing neurons. In addition, a significant role of GPR110 in blood brain barrier (BBB) function has been discovered. GPR110 is highly expressed in mouse and human NPCs and neurons, while its expression was absent in astrocytes. GPR110 is also highly expressed in the kidney, however, little is known about the function of this receptor in renal physiology. To extend our understanding of the role of GPR110 signaling in kidney, we evaluated the urine albumin level in mice devoid of GPR110 gene (GPR110 KO) compared to the wild type (WT). To provide the molecular basis for the renal phenotype, we analyzed in parallel differential expression of kidney proteins in GPR110 KO and WT mice by label-free LC-MS/MS and pathway analysis. We found that the albumin to creatinine ratio was significantly elevated in urine samples obtained from GPR110 KO mice, indicating glomerular filtration dysfunction. The change in protein expression of key proteins including VEGFA is associated with the abnormal renal phenotype of albumin urea in GPR110 KO mice. In addition to the central nervous system phenotype such as learning and memory deficit and BBB dysfunction, our study revealed a new renal phenotype associated with lack of GPR110 signaling. " Authors & Affiliations "Laboratory of Molecular Signaling, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, USA" About Hee-Yong Kim "Senior Investigator and Chief of the Laboratory of Molecular Signaling at NIAAA, NIH" Hee-Yong Kim on the web NIH The Adhesion GPCR Cupidon Regulates Mating In The Closest Relatives Of Animals Alain Garcia De Las Bayonas Abstract "All animals develop through the recognition, adhesion, and fusion of a differentiated sperm and egg. Although fundamental, the evolution of gametogenesis and fertilization in animals is poorly understood. Recently, evidence for sex has been described in choanoflagellates, the closest living relatives of animals. Under nutrient depletion, the model choanoflagellate Salpingoeca rosetta forms distinct cell types that aggregate, fuse, and undergo meiotic recombination. Additionally, the bacterium Vibrio fischeri also induces mating in S. rosetta cultures, suggesting that multiple environmental cues can trigger sex. Importantly, the signaling pathways underlying sexual reproduction in these different contexts have not been investigated. In this study, we report the discovery of an adhesion GPCR, named Cupidon, that regulates the switch from vegetative growth to sexual reproduction in S. rosetta. We found that the knock-out of cupidon induces a gain in cell adhesion and cell fusion, resembling the mating behavior of wild-type cells under nutrient depletion. Cupidon mutants, similar to starved wild-type cells, upregulate various extracellular matrix-related genes, including teneurins and metalloproteases. Finally, we showed that nutrient availability controls the dissociation of the N-terminal fragment in Cupidon. Together, our results suggest that Cupidon prevents sexual reproduction in S. rosetta under high nutrient availability, by inhibiting genes involved in gamete recognition. " Authors & Affiliations "King Nicole, Howard Hughes Medical Institute and Department of Molecular and Cell Biology, University of California Berkeley" About Alain Garcia De Las Bayonas "Hi everyone! I am currently finishing my postoc in the laboratory of Pr Nicole King at UC Berkeley where I am studying the evolution of GPCR families in choanoflagellates, the sister group of animals. I have a particular interest in understanding the premetazoan function of adhesion GPCRs." Alain Garcia De Las Bayonas on the web King Lab Critical role for CD97/ADGRE5 in the induction of allergic airway inflammation Gabriela Aust Abstract Only available for AGPCR 24 Attendees Authors & Affiliations Coming Soon About Gabriela Aust Coming Soon Gabriela Aust on the web Coming Soon < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session I Tethered agonist - dependent/independent activation mechanism in AGPCRs Signaling Properties of ADGRL3 Signe Mathiasen An ECR-Mediated and TA-independent Mechanism of aGPCR Activation: Direct Communication of Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Demet Araç Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Andrew Dates Discriminating between the extracellular scaffolding and G protein signaling roles of GPR56/ADGRG1 via the characterization of a non-cleavable point mutant knock-in mouse, H381S Frank Kwarcinski Tethered Peptide Activation Mechanism of Adhesion GPCRs Peng Xiao Signaling Properties of ADGRL3 Signe Mathiasen Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Rosell, Júlia (1) Holmkvist, Jesper L. (1) Arastoo, Mohammad Reza (1) Vejre, Phillip C. (1) Regmi, Rajesh (1) Perry-Hauser, Nicole A. (2) Bendix, Poul Martin (3) Javitch, Jonathan A. (2) Mathiasen, Signe (1) 1. Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark. 2. Departments of Psychiatry and Molecular Pharmacology and Therapeutics, Columbia University Vagelos College of Physicians and Surgeons, New York, New York, USA; Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York, USA 3. Niels Bohr Institute, Faculty of Natural Sciences, University of Copenhagen, Copenhagen, Denmark" About Signe Mathiasen "2022-present Assistant Professor (Tenure Track) and Group Leader Department of Biomedical Sciences, University of Copenhagen. 2020 – 2022: Assistant Professor Department of Biomedical Sciences, University of Copenhagen. 2014-2021: Postdoc / Assistant Professor Department of Psychiatry, Columbia University, New York, USA. New York State Psychiatric Institute, Research Foundation for Mental Hygiene, New York, USA. Postdoc Supervisor Professor Jonathan Javitch 2013: PhD in Nanoscience/Biophysics. Department of Chemistry, University of Copenhagen, Copenhagen Denmark. PhD Supervisor Professor Dimitrios Stamou." Signe Mathiasen on the web University of Copenhagen Mathiasen Group An ECR-Mediated and TA-independent Mechanism of aGPCR Activation: Direct Communication of Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Demet Araç Abstract "According to the Tethered Agonist (TA)-mediated model of aGPCR activation, the ECR acts as a protective cap for the TA peptide to hide it within the GAIN domain. However, several recent observations suggest that other mechanisms of aGPCR activation are possible. For example, some aGPCRs do not undergo autoproteolysis, which is required for TA release. Even the aGPCRs that are cleaved do not always require cleavage for mediating some aspects of wild type functions. It has been suggested that the TA can regulate receptor signaling without coming out of the GAIN domain or by being partially exposed, however the recent TA-bound 7TM structures of multiple aGPCRs showed that the critical phenylalanine residue and other important TA residues have to reach deep into the 7TM orthosteric pocket for receptor activation, suggesting that non-release or partial release of the TA is unlikely to activate the receptor. In this talk, I summarize accumulating data from our lab and the aGPCR field that suggests an additional model in which the conformation of the Extracellular Region (ECR) has a direct role in modulating the 7TM signaling, independently of TA-mediated activation. Our results provide evidence for the ECR-mediated activation of aGPCR as a complementary mechanism for the TA-mediated activation of aGPCRs. Many biological forces are smaller than 200 pN, the force that is needed to separate the TA from the GAIN domain. To sense these smaller forces, and to regulate aGPCR function on and off, a mechanism that does not depend on ECR dissociation and TA exposure might be at work. At low force or no force conditions, aGPCR may be reversibly regulated by binding and dissociation of a ligand to the ECR without ECR shedding and TA exposure. In this ECR-mediated mechanism of activation, the ECR-7TM communication is altered by transient interactions between ECR and 7TM. The TA peptide remains at its original position and is not involved in signaling. Because the TA-mediated mechanism is a “one and done” mechanism that is irreversible and prevents the receptor from going back to its inactive resting state, the ECR-mediated mechanism may operate in situations where a reversible regulation is needed. The ECR-mediated mechanism may also enable responding to compressing forces on the receptor, that directly “push” on the protein. In cases where a large “pulling” force is executed on the ECR, the ECR may be removed from the 7TM releasing the tethered agonist and activating the aGPCR irreversibly but acutely. ECR-mediated mechanism opens new possibilities for drugging aGPCRs. Future work that dissects different activation mechanisms of aGPCRs in different physiological contexts will shed light on this fascinating family of receptors. " Authors & Affiliations "Kordon Szymon P.1, 2, Cechova Kristina3, Bandekar Sumit J.1, 2, Ethan Dintzner1, 2, Leon Katherine1, 2, Dutka Przemysław1, Siffer Gracie3, Kossiakoff Anthony A.1, Sando Richard 4, Vafabakhsh Reza3, Araç Demet1, 2 1. Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago; 2. Neuroscience Institute, Institute for Biophysical Dynamics, and Center for Mechanical Excitability, The University of Chicago, 3. Department of Molecular Biosciences, Northwestern University; 4. Vanderbilt University" About Demet Araç "Demet was an undergraduate at Bilkent University in Turkey, where she majored in Molecular Biology and Genetics. She moved to the University of Texas Southwestern Medical Center at Dallas in 2000 to work with Dr. Jose Rizo-Rey as a graduate student to elucidate the mechanisms of neurotransmitter release. After finishing her graduate training, she joined Dr. Axel Brunger’s lab at Stanford University to study the structure and function of cell-adhesion proteins at the synapse. In 2013, Demet began her independent research career at the University of Chicago within the Department of Biochemistry and Molecular Biology." Demet Araç on the web Araç Laboratory at UChicago X (Twitter) Heterogeneity of Tethered Agonist Signaling in Adhesion G Protein-Coupled Receptors Andrew Dates Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Daniel T.D. Jones (Harvard Medical School); Jeffrey S. Smith (Harvard Medical School, Brigham and Women's Hospital); Meredith A. Skiba (Harvard Medical School); Maria F. Rich (University of Cincinnati School of Medicine); Maggie M. Burruss (Harvard Medical School); Andrew Kruse (Harvard Medical School); Stephen C. Blacklow (Harvard Medical School)" About Andrew Dates "Drew Dates received his B.S. in Biological Chemistry from Carnegie Mellon University in 2018. As an undergraduate, he studied opioid receptor trafficking and G protein conformational dynamics in the laboratories of Manojkumar Puthenveedu and Roger Sunahara, respectively. As part of his doctoral work in the Blacklow laboratory at Harvard Medical School, Drew studied structure-function relationships in the Adhesion Family of GPCRs." Andrew Dates on the web Harvard Medical School Discriminating between the extracellular scaffolding and G protein signaling roles of GPR56/ADGRG1 via the characterization of a non-cleavable point mutant knock-in mouse, H381S Frank Kwarcinski Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations ""Tyler F. Bernadyn, Mariane Nascimento, Xinyi Lu, Pauline L. Pan, Michael Holinstat and Gregory G. Tall Department of Pharmacology, University of Michigan "" About Frank Kwarcinski "I am research faculty within the department of Pharmacology at the University of Michigan. I work under the supervision of Dr. Gregory Tall and our research primarily focuses on the structural and biochemical characterization of adhesion GPCRs (AGPCR) for mechanism of action and pathogenesis studies. We utilize several genetically modified mouse models to investigate requirements for receptor activator and continuously work to identify novel chemical modulators of AGPCRs through assay development and high-throughput screening efforts. I have previous work experience at two separate contract research organizations centered on assay development, and I am formally trained as a chemical biologist." Frank Kwarcinski on the web LinkedIn Tethered Peptide Activation Mechanism of Adhesion GPCRs Peng Xiao Abstract Only available for AGPCR 24 Workshop Attendees About Peng Xiao "I joined Prof. Jin-Peng Sun’s Lab since I graduated from Shandong University in 2012, and worked under the guidance of Prof. Sun as a postdoc/research associate/assistant professor. Since then, I have been working on dissecting the three-dimensional architecture and underlying molecular signaling mechanism of GPCR using cryo-electron microscopy (cryo-EM). So far, I have published 20 peer-reviewed papers as correspondence (or co- correspondence) or first (or co-first) authors, among which, four papers were published in Nature (2022a, 2022b, 2021, 2020); one paper was published in Cell (2021); on paper was published in Science (2023); two papers were published in Nat Chem Biol. (2022, 2018)." Peng Xiao on the web ResearchGate < Previous Session Next Session >

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Interrogating Multiscale Receptors Functions in Space Date & Time Saturday, November 4th / 10:35 AM Abstract Coming Soon About Martin Beaulieu Dr. Beaulieu received a Ph.D. in Neurological Sciences from McGill University and completed his post-doctoral training at Duke University. Prior to his recruitment Dr. Beaulieu was an associate professor and Canada Research Chair (Tier2) in the Department of Psychiatry and Neuroscience at Laval University. Dr. Beaulieu’s research is aimed at understanding how cellular and molecular mechanisms regulated by psychoactive drugs intersect with genetic risk factors for mental illnesses such as schizophrenia, depression, and bipolar disorder. Dr. Beaulieu has pioneered work establishing a role for Beta-arrestin signaling in the brain in vivo and has established its importance in D2 dopamine receptors (D2R) functions. These receptors belong to the super-family of G-protein coupled receptors (GPCR), the major molecular target for drug development. In particular, D2R is the main pharmacological target of antipsychotic drugs prescribed for schizophrenia and bipolar disorders. Work by the Beaulieu Lab has demonstrated that mood stabilizer drugs (e.g. lithium) used for bipolar disorder therapy target signaling mechanisms regulated by dopamine receptors, thus providing a framework to understand how different drug classes can engage overlapping cellular mechanisms to exert their action. The Beaulieu group is presently investigating how cell surface express proteins can act as allosteric modulators of D2R signaling and explores the potential usefulness of beta-arrestins for the development of new pharmaceutical agents. Translational validation is important to validate findings obtained from experimental models research and bridge the gap between bench and bedside. Working in collaboration with geneticists, the Beaulieu-Lab has identified interactions between cellular mechanisms engaged by D2R and psychiatric drugs with genetic risk factors implicated in schizophrenia by large whole-genome association studies (GWAS) in humans. These investigations have led to the identification of an RNA binding protein (FXR1P) involved in the regulation of protein synthesis as a potential downstream effector of the action of mood stabilizers and other psychoactive drugs. In addition to basic research, the Beaulieu group is also actively implicated in translational research and industry collaboration to develop new drugs and drug development technology. Martin Beaulieu on the web University of Toronto Google Scholar LinkedIn ResearchGate Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Departure < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda State of the Art Talk Adhesion GPCR in Mechanobiology Abstract Only Available for AGPCR24 Attendees About Tobias Langenhan "1997-2004: Medical school and Dr. med. Neuroanatomy (Würzburg, Germany); 2004-2005: M.Sc . Neuroscience (Oxford, UK); 2005-2009: D.Phil. Neuroscience (Oxford, UK); 2009-2016: Group leader, Institute of Neurophysiology (Würzburg, Germany); 2016: Heisenberg professorship (Würzburg, Germany); 2016-to date: Professor and Chair in Biochemistry (Leipzig, Germany)" Tobias Langenhan on the web Langenhan Lab LinkedIn < Previous Session Next Session >

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session VIII Physiological and pathological roles of AGPCRs in the periphery ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Cheng-Chih Hsiao Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Anastasia Georgiadi ADGRF5-mediated regulation of cardiac health and disease Douglas Tilley ADGRG1/GPR56 regulates survival of terminally differentiated CD8+ T cells Cheng-Chih Hsiao Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "Cheng-Chih Hsiao1,2, Hendrik J. Engelenburg1, Joost Smolders1,3, and Jörg Hamann1,2 1Department of Neuroimmunology, Netherlands Institute for Neuroscience, Amsterdam, The Netherlands; 2Department of Experimental Immunology, Amsterdam institute for Immunology and Infectious diseases, Amsterdam University Medical Center, Amsterdam, The Netherlands; 3MS center ErasMS, Departments of Neurology and Immunology, Erasmus Medical Center, Rotterdam, The Netherlands" About Cheng-Chih Hsiao "2012-2015: PhD in Immunology, University of Amsterdam; 2015-2019: Postdoctoral researcher, Amsterdam UMC; 2019-2022: Senior postdoctoral researcher, Netherlands Institute for Neuroscience; 2022 - present: Researcher associate, Netherlands Brain Bank" Cheng-Chih Hsiao on the web LinkedIn ReseachGate Adhesion GPCR GPR116/Adgrf5 controls a lineage of anti-thermogenic adipocytes with implications for adaptive thermogenesis during prolonged cold exposure Anastasia Georgiadi Abstract Only available for AGPCR 24 Attendees Authors & Affiliations "El Merabhi Rabih1*, Karagiannakou Vasiliki1*, Kardinal Ronja2, Jäckstein Michelle3 Yvonne, Kumar Jha Ankush1, Krokidi Sissy Thodou1, Wachten Dagmar2, Heeren Jörg3, Herzig Stephan1, Georgiadi Anastasia1 *equal contributions , Institutions : 1. Institute for Diabetes and Cancer, Helmholtz Centre Munich, Germany, 2. Institute of Innate Immunity, University Hospital Bonn, University of Bonn, 3. Centre for Experimental Medicine, Institute for Biocehmistry and Molecular Cell Biology, University Medical Center Hamburg-Eppendorf" About Anastasia Georgiadi "Head of Junior Group Endocrine Pharmacology, Institute of Diabetes and Cancer (IDC). Professional Background Since 2021 Group Leader, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2018 - 2021 Project Team Leader, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2015 - 2018 Postdoctoral fellow, Department of Adipose Tissue Biology, Institute for Diabetes and Cancer, Helmholtz Diabetes Centre, Munich 2012 - 2015 Postdoctoral fellow, Department of Cell and Molecular Biology, Karolinska Institute, Sweden" Anastasia Georgiadi on the web Endocrine Pharmacology Google Scholar ADGRF5-mediated regulation of cardiac health and disease Douglas Tilley Abstract Only available for AGPCR 24 Attendees About Douglas Tilley "Research in the Tilley laboratory focuses primarily upon aspects of GPCR regulation of cardiac function, inflammation and remodeling during HF or following acute cardiac injury. Much of this work centered on elucidating novel mechanisms by which β-adrenergic receptors impact cardiac structure and function, and has evolved to encompass their roles in regulating immune cell response to acute cardiac injury or chronic stress. Additionally, the lab has begun to investigate potential roles for previously unrecognized cardiac-expressed GPCRs in the regulation of physiologic/pathologic function in the heart in an effort to uncover novel therapeutic directions for HF, including adhesion GPCRs (AGPCRs). In all, research in the Tilley lab spans molecular pharmacology to pathophysiology studies focused primarily in the cardiovascular realm." Douglas Tilley on the web Lewis Katz School of Medicine at Temple University < Previous Session Next Session >

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Complex Allosteric Cannabinoid Receptor Pharmacology Date & Time Friday, November 3rd / 11:30 AM Abstract Coming Soon About Robert Laprairie "Dr. Robert Laprairie is an Associate Professor and the Saskatchewan Research Chair in Drug Discovery and Development at the College of Pharmacy and Nutrition, University of Saskatchewan. Robert was the President and Director of Education for the Canadian Consortium for the Investigation of Cannabinoids (CCIC) and the 2021 Recipient of the William A. Devane Young Investigator Award from the International Cannabinoid Research Society (ICRS). Robert and his lab have been interested in the molecular pharmacology of cannabinoids for nearly 10 years and he has published more than 50 studies in the field." Robert Laprairie on the web University of Saskatchewan Pubmed Twitter Instagram ResearchGate Google Scholar Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Welcome Reception and Poster Session 1 Date & Time Thursday, November 2nd / 5:30 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 3 Date & Time Friday, November 3rd / 10:25 AM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Coffee Break with lights snacks Complimentary < Previous Session Next Session >

Strategic Partners Dr. GPCR Podcast << Back to podcast list Dr. Lauren M. Slosky About Dr. Lauren M. Slosky Lauren Slosky is an Assistant Professor in the Department of Pharmacology and a member of the Medical Discovery Team on Addiction, a multidisciplinary initiative within the University of Minnesota’s Medical School to advance research and treatment in the field of drug addiction. Dr. Slosky’s research is focused on understanding how neuropeptide G protein-coupled receptors (GPCRs) regulate motivated behavior and how these receptors can be targeted for therapeutic benefit. Dr. Slosky was awarded a B.S. with honors in Molecular and Cellular Biology and Psychology from The University of Arizona in 2011. She received a Ph.D. in Medical Pharmacology from The University of Arizona in 2015 and completed a postdoctoral fellowship in the laboratory of Dr. Marc G. Caron at Duke University. Dr. Slosky opened her laboratory at the University of Minnesota Medical School in 2021. While a postdoctoral fellow, Dr. Slosky characterized a new class of β-arrestin biased allosteric modulators (BAMs) for the neurotensin receptor 1. These ligands stimulate receptor β-arrestin recruitment without activating canonical G protein signaling. Critically, these ligands reduce addiction-associated behaviors in animal models without the side effects characteristic of balanced receptor activation. Because BAMs engage less well-conserved allosteric sites and exert pathway-specific effects on receptor signaling, they are exciting tools for linking distinct signaling pathways with their physiological effects and may serve as the basis for more selective therapeutics. This work was made possible by the optimization of longitudinal intravenous self-administration paradigms for genetically modified mice. Integrating GPCR biology, behavioral pharmacology, and systems neuroscience approaches, the Slosky Lab is now working to understand how the principles of receptor allosterism and functional selectivity can be leveraged in the development of safe and effective treatments for stimulant and opioid use disorders. Dr. Slosky’s work has been recognized through several travel and research awards, including the William James Psychology Award, the Hank Yamamura Endowed Fellowship in Pharmacology, an NIH F32 Postdoctoral Fellowship, and an NIH K99/R00 Pathway to Independence Award. In addition to research, Dr. Slosky is passionate about training the next generation of scientists and increasing diversity, equity, and inclusion in science. An advocate for trainees at all levels, she served as Service Chairperson and Interim President of the Duke University Postdoctoral Association. She is currently a faculty trainer for the University of Minnesota's MS and Ph.D. programs in Pharmacology, Graduate Program in Neuroscience, and Life Sciences Summer Undergraduate Research Program and is working to build relationships with key stakeholders through institutional and community service. Dr. Lauren M. Slosky on the web Twitter University of Minnesota Department Page LinkedIn Google Scholar PubMed Research Gate Dr. GPCR Ecosystem Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles The Truth About GPCR Product Launches: Years in the Making Innovative Data-Driven Solutions: The pHSense Revolution How a Failed Med School Dream Sparked a GPCR Biotech Revolution Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

Strategic Partners Dr. GPCR Podcast << Back to podcast list Dr. Paul Insel About this episode In 1975, Dr. Paul Insel was at the FASEB experimental biology meeting in Atlantic City. During dinner with colleagues and Alfred Gillman , co-recipient of the 1994 Nobel Prize in Physiology or Medicine for their discovery of G-proteins and their role in signal transduction in cells, Paul was designated to go to Gillman’s lab . That summer, he used radioligand binding methods to dissect receptor function from the adenylyl cyclase activated by ligands, including adrenaline. From that point on, Paul was hooked and has since studied receptor function in human physiology, receptor molecular pharmacology in cells, and animal models, and as he puts it has now he’s "gone full circle" back to studying GPCRs important in human pathophysiology. Today, Paul and his team focus on previously unrecognized receptors with the hopes to use these as novel drug targets. Dr. Paul Insel on the web Insel Laboratory Institute of Engineering in Medicine UC San Diego UCSD Profiles Google PubMed Dr. GPCR Ecosystem Enjoying the Dr. GPCR Podcast? Leave a Review. Leave a quick review to help more scientists find the show—and help us keep improving every episode. It takes <60 seconds and makes a big difference. ★ Review on Apple Podcasts ★ Rate on Spotify ✉️ Send feedback to the team Recent Podcast Articles The Truth About GPCR Product Launches: Years in the Making Innovative Data-Driven Solutions: The pHSense Revolution How a Failed Med School Dream Sparked a GPCR Biotech Revolution Thanks for listening to this podcast episode Follow us on your favorite Podcast Player << Previous Podcast Episode Next Podcast Episode >>

The Practical Assessment of Signaling Bias Dr. Terry Kenakin Get Started Premium Members benefits: - Subscribe and save 25% on every GPCR Course - Early-bird access - Recordings will be available < Back to GPCR courses Watch recording Your Instructor Dr. Terry Kenakin

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Targeting adenosine signaling for immuno-oncology Date & Time Friday, November 3rd / 4:35 PM Abstract "Adenosine (ADO) signaling through A2A and A2B G protein-coupled receptors is increasingly recognized as an important immune checkpoint in the generation of anti-tumor immunity. Potent inhibitors of ADO signaling are currently being tested in cancer patients, including in randomized Phase 3 trial. I will present our recent work on adenosine-producing ectonucleotidases and adenosine signaling and discuss unexpected links between the adenosinergic pathway, DNA damage response and metabolic regulation." Authors and Affiliations John Stagg , David Allard . Centre de Recherche du Centre Hospitalier de l'Université de Montréal; Faculté de Pharmacie. 900 St-Denis, Montréal, QC, H2X 0A9. About John Stagg "John Stagg is a Professor of Pharmacy at Université de Montréal and researcher at the CHUM Research Centre. Distinguished immunologist, Dr Stagg is recognized for having identified the adenosine-producing enzyme CD73 as a new cancer target, and for his translational work in immuno-oncology. Dr Stagg has served as an expert consultant in the development of adenosine-targeting drugs, several of which now in clinical trials. Dr Stagg is a member of the Board of Directors of BioCanRx, Canada's Immunotherapy Network, co-founder and permanent member of the Scientific Advisory Board (SAB) of Surface Oncology, a clinical stage company developing next generation immunotherapies, and member of the SAB of Domain Therapeutics, a biopharmaceutical company focused on GPCR in immuno-oncology." John Stagg on the web University of Montréal Québec Cancer Consortium The University of Montreal Hospital Research Centre Pubmed LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Registration & Coffee with light breakfast < Previous Session Next Session >

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Inhibition of Relaxin Autocrine Signaling Confers Therapeutic Vulnerability in Ovarian Cancer Date & Time Friday, November 3rd / 3:55 PM Abstract Coming Soon About Robert Rottapel "Dr. Rottapel is a Senior Scientist at the Princess Margaret Cancer Centre where he holds the Amgen Chair for Cancer Research. He is a Professor in the Departments of Medicine, Immunology and Medical Biophysics at the University of Toronto. After completing his medical studies at George Washington University, the NIH and UCLA, he pursued his postdoctoral studies with Allan Bernstein at the Lunenfeld Research Institute in Toronto and with Patrice Dubreuil at INSERM, France. Dr. Rottapel is a clinical rheumatologist at St. Michael's Hospital, University of Toronto. His clinical expertise is in monogenic autoinflammatory disorders and the autoimmune adverse effect resulting from checkpoint inhibitors in cancer patients. Dr. Rottapel’s research interests lies in the elucidation of signal transduction pathways in cancer, immune and bone cells. He has focussed on developing a comprehensive map of ovarian cancer essential genes using whole genome RNAi and CRISPR technology. This approach has provided insight into novel drivers resulting from the widespread gene copy number aberrations observed in ovarian cancer and the identification of emergent vulnerabilities associated with adaptation pathways required to buffer cancer associated stress states. Several of these targets are being developed for potential new therapeutic strategies in ovarian and pancreatic cancer. A second area of interest has been the elucidation of the molecular basis for a rare autosomal human disease called Cherubism. The adapter protein 3BP2 is mutated in Cherubism. The Rottapel lab has shown that 3BP2 has pleiotrophic function controlling bone homeostasis, immune cell function and scavenger receptor activation." Robert Rottapel on the web The Rottapel Lab Ontario Institute for Cancer Research University of Toronto Pubmed Google Scholar LinkedIn Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 1 Date & Time Thursday, November 2nd / 2:45 PM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Unveiling Non-Canonical Functions for Gαq Signaling Pathways Date & Time Friday, November 3rd / 11:55 AM About Catalina Ribas " Dr. Catalina Ribas, is currently an Associate Professor at the University Autonomous of Madrid (UAM) and she has been Academic Secretary of Molecular Biology Department for several years. The research group led by Dr. Catalina Ribas, located in the Centro de Biología Molecular “Severo Ochoa” (UAM/CSIC) and belongs also to the Health Research Institute La Princesa, has extensive experience in the field of GPCR. Dr. Catalina Ribas made a postdoctoral stay in the laboratory of Dr. SM. Lanier in the MUSC (USA). During this period and her doctoral thesis, she has deepened the regulatory mechanisms of GPCR signaling. In her postdoctoral period, she has participated in the identification and characterization of proteins that act at the level of G proteins and which are part of a multimolecular signaling complex (AGS, de “Activators of G-protein signaling). In Spain, Dr. Ribas continued working on the regulation of GPCR. The group of Dr. Ribas has characterized the existence of a new signaling pathway with a relevant role in cardiac hypertrophy led by a new Gαq interactome. Recently, Dr. Ribas' group has described a new interaction region in a cellular protein that has turned out to be very relevant in the control of the cellular process known as autophagy. These results have been published in the journal Nature Communications (12 (1):4540, 2021) with the title "Gαq controls autophagy via modulation of the mTORC1 signaling hub". Furthermore, Dr. Ribas has also described a new protective role of G protein-coupled receptor kinase 2 (GRK2), a known regulator of Gq-GPCR signaling in HNSCC tumor progression (International Journal of Cancer, 2020). " Catalina Ribas on the web Severo Ochoa Molecular Biology Center X (Twitter) Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Biased agonism at the GLP-1 receptor: from structure to animal models of disease Date & Time Friday, November 3rd / 11:05 AM Abstract Coming Soon About Patrick Sexton " Patrick Sexton is a NHMRC Senior Principal Research Fellow and Director, ARC Centre for Cryo-electron Microscopy of Membrane Proteins ( www.ccemmp.org ). He is a leader in the study of GPCRs. Recently, his team has applied cryo-EM to elucidation of the structure and dynamics of GPCRs. Prof. Sexton has published over 335 peer reviewed journal articles and has been cited >29,000 times (Google Scholar). He is a 2022 Clarivate Analytics Highly Cited Researcher in two disciplines: Pharmacology & Toxicology; Biology & Biochemistry, a corresponding member of NC-IUPHAR, a member of the Faculty of 1000 and an elected Fellow of the British Pharmacological Society (BPS). Prof. Sexton’s awards include the ASCEPT Lecturer award, Endocrine Society (Australia) Senior Plenary award, Rand Medal (ASCEPT), Paxinos-Watson Award (Australian Neuroscience Society), Vane Medal (BPS), Gordon Hammes Lectureship Award (American Chemical Society) and the GSK Research Excellence award. Prof. Sexton is also a co-founder of Septerna Inc. " Patrick Sexton on the web CCeMMP Monash University Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Breakfast 1 Date & Time Friday, November 3rd / 7:30 AM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Removing the GPCR-mediated brake on exocytosis enhances insulin action, promotes adipocyte browning, and protects against diet-induced obesity Date & Time Friday, November 3rd / 2:45 PM Abstract Coming Soon Authors and Affiliations Ryan P. Ceddia 1, *, Zack Zurawski 2,3,*, Analisa Thompson Gray 2, Feyisayo Adegboye 2, Ainsley McDonald-Boyer 3, Fubiao Shi 1, Dianxin Liu 1, Jose Maldonado 5, Jiesi Feng 4, Yulong Li 4, Simon Alford 5, Julio E. Ayala 5, Owen P. McGuinness 5, Sheila Collins 1,5, Heidi E. Hamm 2 1 Department of Medicine, Division of Cardiovascular Medicine, Vanderbilt University Medical Center, Nashville, TN 37232, USA 2 Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA 3, 5 Department of Molecular Physiology and Biophysics, Vanderbilt University, Nashville, TN 37232, USA 4 Peking University, China 5 Department of Anatomy and Cell Biology, University of Illinois at Chicago, Chicago, IL 60612, USA. About Heidi Hamm "Heidi E. Hamm, Ph.D. is the Aileen M. Lange and Annie Mary Lyle Chair in Cardiovascular Research, and Professor of Pharmacology, Ophthalmology and Visual Sciences, and Orthopedics at Vanderbilt University. This is one of the top Pharmacology departments in the country, judged by reputation, citation analysis, and NIH funding. She oversaw an increase of the size of the Department, as well as a quintupling of its NIH funding, in her 14 years as Chair. The Department’s strengths lie in GPCR signal transduction and neuroscience, and she has expanded it in the areas of drug discovery and structural biology of membrane proteins. Her research focuses on the structure and function of GTP binding proteins and the molecular mechanisms of signal transduction. Her laboratory has been involved in studying G protein coupled signal transduction for many years and has made key discoveries in G protein structure and mechanisms of activation by GPCRs and activation of effectors. Current areas of interest include Protease Activated Receptor signaling in the cardiovascular system and regulation of vesicular exocytosis mediated by Gi/o-coupled receptors by G subunit binding to SNAREs. Dr. Hamm obtained her Ph.D. in 1980 from the Department of Zoology at the University of Texas-Austin and did postdoctoral training in the University of Wisconsin-Madison from 1980-1983. Her initial research centered around circadian clocks and melatonin synthesis in the avian retina; her postdoctoral work investigated the role of the G protein transducin in visual transduction using blocking monoclonal antibodies. She held faculty appointments at the University of Illinois at Chicago School of Medicine and Northwestern University before moving to Vanderbilt in 2000. She has received numerous awards, including the Glaxo Cardiovascular Discovery Award, the Distinguished Investigator Award from the National Alliance for Research in Schizophrenia and Depression, the Faculty of the Year award from the University of Illinois College of Medicine, and the Stanley Cohen Award “For Research Bringing Diverse Disciplines, such as Chemistry or Physics, to Solving Biology’s Most Important Fundamental Problems” from Vanderbilt University in 2003. She gave the Fritz Lipmann Lecture at ASBMB in 2001. " Heidi Hamm on the web The Hamm Lab Vanderbilt School of Medicine Pubmed Google Scholar LinkedIn Twitter Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Coffee Break 5 Date & Time Saturday, November 4th / 9:55 AM Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Retreat 2023 About Program Registration Logo Contest Committee Sponsors GPCR Retreat Program < Back to schedule Regulation and role of mitochondria delta opioid receptors Date & Time Friday, November 3rd / 10:40 AM Abstract Coming Soon About Louis Gendron "Dr Louis Gendron, PhD is tenured Professor and Chair of the Department of Pharmacology-Physiology at the Université de Sherbrooke. He has 20+ years of experience in in vitro and in vivo GPCR pharmacology and has published seminal papers where he used various approaches to describe the role of opioid receptors in pain and anagesia as well as to study the mechanisms involved in the cellular trafficking of the delta opioid receptor. Recently, his group reported the first in vivo GPCR interactome, revealing an important number of new potential proteins interacting with GPCRs. Dr Gendron is co-director of the FRQS-funded Quebec Pain Research Network and the Editor-in-Chief in the journal Progress in Neuro-Psychopharmacology & Biological Psychiatry." Louis Gendron on the web Université de Sherbrooke Neurosciences Sherbrooke RQRD Pubmed Google Scholar LinkedIn Twitter Dr. GPCR Previous Event Next Event Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec Great Lakes GPCR Retreat and Club des Récepteurs à Sept Domaines Transmembranaires du Québec 22nd GPCR Retreat Sponsored by

Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Posters Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Interrogating The Role Of CELSR1 (ADGRC1) In Breast Cancer Caroline Formstone Abstract "Breast cancer is the most common form of cancer amongst women. Ductal carcinomas are increasingly diagnosed but identifying which will progress to invasive disease remains difficult highlighting an urgent need for new biomarkers that distinguish ductal carcinomas on this basis. Planar cell polarity (PCP) proteins contribute to tumour growth and invasion. Recent studies identify CELSR1, a key PCP gene, as a novel biomarker for early-stage breast cancer. CELSR1 is reactivated in luminal-type ductal carcinomas. The impact of CELSR1 on cancer progression, however, is unclear. Our working hypothesis is that distinct CELSR1 protein isoforms differentially regulate tissue adhesiveness by influencing the stability/plasticity of cell-cell and cell-matrix contacts. Notably, our pilot data from luminal-type breast cancer cell lines representative of breast carcinomas with lower versus higher invasive potential reveal differential enrichment of CELSR1 protein isoforms. To test the specific hypothesis that biased expression of CELSR1 isoforms will predict invasive potential of a luminal breast carcinoma we will (a) determine, via loss-of-function assays in vitro and in vivo, whether CELSR1 protein isoforms differentially influence the stability of cell-cell and/or cell-matrix adhesions to dictate breast tumour invasive mechanism (b) quantify CELSR1 isoform expression (mRNA and protein) within patient luminal carcinoma samples exhibiting non-invasive or invasive features, the latter including heterogeneous tumours with mixed pathology. Through study of known protein isoforms of CELSR1, which would be missed in gene expression microarray analyses, we hope to illuminate the prognostic potential of CELSR1 for early-stage breast cancer." Authors & Affiliations "Klena, Ladislav University of Hertfordshire" About Caroline Formstone "Cell and developmental biologist with a focus on how planar cell polarity drives complex tissue morphogenesis. I study the cell and tissue level consequences of its failure in foetal development and of its reemployment in cancer" Caroline Formstone on the web University of Hertfordshire Generation and characterization of collecting duct specific GPR56 knockout mice Jianxiang Xue Abstract "GPR56 is a multifunctional adhesin G protein-coupled receptor involved in diverse biological processes. The role of GPR56 in the kidneys has been understudied. A recent study demonstrated that GPR56 in the glomerular endothelial cells promoted diabetic kidney disease progression via regulation of eNOS. Using RNAscope in situ hybridization (ISH) for GPR56, aquaporin 2 and NKCC2 (thick ascending limb, TAL marker), we detected GPR56 mRNA highly expressed in the collecting duct and TAL of the loop of Henle with limited expression in the proximal tubule. To determine the physiological role of GPR56 in the collecting duct, we generated a collecting duct-specific GPR56 knockout (GPR56CD-KO) mouse model by crossing GPR56flox (Control) with cadherin 16 Cre mice. The deletion of GPR56 in the collecting duct was confirmed by RNAscope ISH. GPR56CD-KO mice were born at predicted Mendelian frequencies, appeared grossly indistinguishable from Con mice, and developed normally. For baseline phenotypic characterization, blood gas analysis showed no differences in blood pH, blood HCO3-, blood Na+, or blood K+ between GPR56CD-KO and control mice. Metabolic cage experiments demonstrated no differences in fluid intake, urine volume, urinary pH or urine osmolality between genotypes in baseline. 24hr water deprivation experiment showed that GPR56CD-KO mice can concentrate urine as effectively as control mice. In conclusion, we successfully generated collecting duct-specific GPR56 knockout mouse and found no defective urine concentrating ability in GPR56CD-KO mice. This mouse model will be useful to delineate the collecting duct-specific role of GPR56 for renal function, including acid-base regulation." Authors & Affiliations "Hailey Steichen, Krystin Eaton, Teagan Yan, and Nathan Zaidman; Department of Biochemistry and Molecular Biology, University of New Mexico" About Jianxiang Xue "I am a postdoctoral researcher working in the Department of Biochemistry and Molecular Biology, University of New Mexico. I earned my PhD degree in Biomedical Sciences from the University of South Florida. During my graduate studies, using various transgenic mouse models and expertise in intestinal and renal physiology, I systematically characterized the function of sodium/hydrogen exchanger 3 in the intestine and kidneys for fluid and electrolyte homeostasis and acid-base balance. My predoctoral work was supported by an American Heart Association fellowship. Since staring my postdoctoral training, I have continued to develop my expertise to answer fundamental questions on adhesion GPCR in renal physiology and pathology. In my free time, I enjoy reading, workouts, and hiking." Jianxiang Xue on the web Zaidman Physiology Lab Anti-Tumorigenic Role of Brain Angiogenesis Inhibitor 3 (BAI3) in WNT-Activated Medulloblastomas Virginea de Araujo Farias Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Van Meir, Erwin G. University of Alabama at Birmingham" About Virginea de Araujo Farias "Brain Angiogenesis Inhibitor (BAI) proteins are members of group VII of the adhesion G protein-coupled receptor (aGPCR) family. BAI1-3 are highly expressed in the brain, where they participate in synaptogenesis and synapse maintenance. In cancers, BAI1-3 expression can be lost through epigenetic silencing, copy number loss or truncating mutations. In medulloblastomas (MB), BAI3 (ADGRB3) expression is specifically reduced in the WNT-activated group (WNT-MB), but not in the other three molecular groups. WNT pathway activation in WNT-MB is driven by mutations of the CTNNB1 gene, activating ß-catenin-dependent signaling; however, no interactions between BAI3 and the WNT signaling pathway have been described so far. MAGI3, a PDZ-containing scaffolding protein is known to downregulate WNT signaling by interacting with ß-catenin in gliomas, but it is unknown whether this involves BAI3. To explore a possible connection between BAI3 and ß-catenin signaling through MAGI3 in WNT-MB, we probed for potential protein-protein interactions using co-IP experiments. We found an interaction between BAI3 and MAGI3 in mouse brain lysates. Therefore, we hypothesize that re-expression of BAI3 in WNT-MB cells will restrain ß-catenin activity through the formation of a BAI3/MAGI3/ß-catenin complex, reducing their tumorigenic properties. To test this hypothesis, we created WNT-like MB cell lines stably expressing tet-on wild-type BAI3 or a BAI3 lacking the C-terminal PDZ-binding motif (PBM). We will present the effects of BAI3 re-expression on WNT-MB cells oncogenic properties and signaling." Virginea de Araujo Farias on the web Google Scholar Conformational And Functional Coupling Between Extracellular and Transmembrane Regions of a Holo-Adhesion GPCR Szymon P. Kordon Abstract "Adhesion G Protein-Coupled Receptors (aGPCRs) are key cell-adhesion molecules involved in numerous physiological functions. aGPCRs have large multi-domain extracellular regions (ECR) that mediate cell adhesion and play roles in transmitting extracellular signals to the inside of the cell. Ligand binding and mechanical force applied on the ECR regulate receptor function. However, how the ECR communicates with the seven-pass transmembrane domain (7TM) remains elusive, because the relative orientation and dynamics of the ECR and 7TM within a holoreceptor is unclear. Here, we describe the cryo-EM reconstruction of an aGPCR, Latrophilin3/ADGRL3, and reveal that the conserved GAIN domain, that directly precedes 7TM, adopts a parallel orientation to the membrane and has constrained movement. Single-molecule FRET experiments unveil three slow-exchanging FRET states of the ECR relative to the 7TM within the holoreceptor. GAIN-targeted antibodies, and cancer-associated mutations at the GAIN-7TM interface, alter holoreceptor conformations, and modulate downstream receptor signaling. Altogether, this data demonstrates conformational and functional coupling between the ECR and 7TM, suggesting an ECR-mediated mechanism for aGPCR activation." Authors & Affiliations "Cechova Kristina (3), Bandekar Sumit J.(1, 2), Leon Katherine (1, 2), Dutka Przemysław (1, 4), Siffer Gracie (3), Kossiakoff Anthony A. (1), Vafabakhsh Reza (3), Araç Demet (1, 2) 1. Department of Biochemistry and Molecular Biology, The University of Chicago, Chicago, IL, USA; 2. Neuroscience Institute, Institute for Biophysical Dynamics, and Center for Mechanical Excitability, The University of Chicago, Chicago, IL, USA; 3. Department of Molecular Biosciences, Northwestern University, Evanston, IL, USA; 4. Current affiliation: Department of Structural Biology, Genentech, South San Francisco, CA, USA" About Szymon P. Kordon "I am a postdoctoral scholar in the Araç Lab at The University of Chicago, studying the structure and function of aGPCRs. Utilizing synthetic antibody fragments, I aim to understand better the structural basis of the aGPCRs activation and signaling and to characterize ECR-mediated signal transduction at the molecular level." Szymon P. Kordon on the web Araç Laboratory at UChicago Deorphanization Of The Adhesion GPCRs GPR110 and GPR116 Tingzhen Shen Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Frank E. Kwarcinski, Gregory G. Tall (University of Michigan, Ann Arbor)" About Tingzhen Shen "A graduate student from Tall Lab, department of Pharmacology, University of Michigan, Ann Arbor." Tingzhen Shen on the web University of Michigan Self-Cleavage of GPR110 SEA Domain and Its Impact on GAIN Domain Autoproteolysis Bill Huang Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Hee-Yong Kim, Laboratory of Molecular Signaling, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, MD, USA" About Bill Huang "Researcher" Bill Huang on the web LinkedIn Tethered Agonist Dependent ADGRL3 Signaling Activity In The G12/13 Pathway Júlia Rosell Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations "Regmi, Rajesh (1), Perry-Hauser, Nicole A. (2), Javitch, Jonathan A. (2), Mathiasen, Signe (1) (1) Department of Biomedical Sciences, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark. (2) Department of Psychiatry and Molecular Pharmacology and Therapeutics, Columbia University Vagelos College of Physicians and Surgeons, New York, USA; Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, USA" About Júlia Rosell "I am a first-year PhD student with two years of experience in the adhesion GPCR field. I completed my Master’s thesis on ADGRL3, where I conducted research involving mammalian cell cultures and techniques such as BRET assays and gene expression assays. Currently, my research focuses on the intracellular signaling of ADGRL3 from a single-molecule perspective and investigating how the binding of extracellular transsynaptic ligands modulates ADGRL3 activity, aiming to elucidate their interplay." Júlia Rosell on the web LinkedIn Endocytic Cues Determine the Signaling Profile of Adhesion GPCR ADGRL1 / Latrophilin-1 Sheila Ribalta-Mena Abstract Only available for AGPCR 24 Workshop Attendees Authors & Affiliations " Hernández-Aranda Judith 2, Correoso-Braña Kerlys 1, Vialou Vincent 3, Leduc Richard 4, Olivares-Reyes Jesús Alberto 2, Boucard Antony A1. 1 Department of Cell Biology, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 2 Department of Biochemistry, Centro de Investigación y de Estudios Avanzados del Instituto Politécnico Nacional (Cinvestav-IPN), México City, México. 3 Sorbonne Université, Inserm, CNRS, Neurosciences Paris Seine, Paris, France. 4 Department of Physiology and Pharmacology, Université de Sherbrooke, Sherbrooke, Canada " About Sheila Ribalta-Mena " Cell Biology PhD student " Sheila Ribalta-Mena on the web CINVESTAV ResearchGate LinkedIn GPR110 modulates anxiety-like behaviors and memory function in mice potentially through neuronal and neuroimmune alterations during neurodevelopment Mariam Melkumyan Abstract "GPR110, an adhesion G protein coupled receptor (GPCR), is widely expressed in developing brains but diminishes in adult stage except in the hippocampus, a region involved in learning and memory. Ligand-induced GPR110 signaling stimulates neurogenesis and synaptogenesis during development, and the absence of the ligand-induced signaling causes object recognition and spatial memory deficits in adulthood and increased neuroinflammatory responses. Nevertheless, the role of GPR110 signaling in behavioral consequences has not been fully explored. This study aimed to understand the effects of GPR110 on mouse behaviors in relation to neurodevelopmental and neuroimmune gene and protein expression. Anxiety and memory function were tested using both male and female mice at 5-6 month of age. GPR110 knockout (KO) mice displayed trends for increased anxiety-like behaviors in the elevated plus maze test and in the open field test. Memory tests, including the novel object test and the radial 8-arm maze showed worsened spatial and reference memory in the GPR110 KO mice compared to wildtype mice. The y-maze showed a significant sex by genotype interactions with GPR110 KO male mice having increased number of correct alterations and errors, while the GPR110 KO females had fewer correct alterations and errors. RNAseq data indicated significantly impaired developmental gene expression for neuronal differentiation, axonogenesis, and synaptogenesis, as well as altered neuroinflammatory marker expression in GPR110 KO mouse brains. Further studies exploring the protein expression and neural activity of these mouse brain will give insight on the mechanism underlying the behavioral consequences associated with the GPR110 receptor. " Authors & Affiliations "Joel Toro, Bill Huang, Hee-Yong Kim Laboratory of Molecular Signaling, National Institute of Alcohol Abuse and Alcoholism, NIH" About Mariam Melkumyan "Mariam Melkumyan is a postdoctoral fellow at the Laboratory of Molecular Signaling studying the role of GPR110 in neurotransmission and neuroimmune activity involved in learning and memory, anxiety, and alcohol use. Mariam, originally from Armenia, completed her bachelor's degree in Neuroscience at American University in Washington, DC and her dual-title PhD in Neuroscience and Clinical and Translational Sciences at Penn State College of Medicine in Hershey, PA. Mariam started her postdoctoral training in February 2024 and is hoping to become an academic professor and mentor the next generation of scientists." Mariam Melkumyan on the web LinkedIn Google Scholar < Previous Session Next Session >

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