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Hello everyone! Don't miss out on our latest coverage of GPCRs for this week. We have a total of 34 insightful GPCR research papers and seven updates from the industry. Stay informed and up to date with the latest GPCR research and industry news. This week's highlight includes congrats to: Drs. Sara Marsango and Graeme Milligan for their research on the Regulation of the pro-inflammatory G protein-coupled receptor GPR84 Drs. Chakit Arora, J Silvio Gutkind, and Francesco Raimondi for their work on The landscape of cancer-rewired GPCR signaling axes Affiong Ika Oqua, Dr. Alejandra Tomas, et al. for their study on Lipid regulation of the glucagon receptor family Drs. Naveen Thakur, Kenneth A Jacobson, Matthew T Eddy, et al. for their analysis on Membrane mimetic-dependence of GPCR energy landscapes Dr. GPCR University We successfully started our Dr.GPCR University workshop, 'Advanced Data Analysis for GPCR Pharmacology,’ led by Dr. Sam Hoare. Mark your calendar for September and October 2024. Dr. Kenakin will be back with two back-to-back classes. Stay tuned as we plan to open registrations for both classes in July 2024. Dr. GPCR Podcast Episode #151 is out! A special episode with our board, meet Drs. Maria Waldhoer, JoAnn Trejo, and Anne Marie Quinn. Did you watch Episode #150 of the Dr. GPCR Podcast? Join us in this episode to meet the team behind Dr. GPCR, hear anecdotes, and get important announcements. Tune in and be the first to know about the benefits coming your way! Dr. GPCR Matchmaking Mark Schmeizl, our Chief Matchmaker, can help you find your perfect match if you want to hire or be hired. Mark has experience connecting candidates with employers and will work with you to understand your needs and preferences to ensure a successful match. Contact Mark today to get started. Dr. GPCR Symposia Learn more about GPCRs by signing up for a Premium Membership to watch all the material recorded at our previous events, including the three editions of the Dr. GPCR Summit. We have postponed our symposium on Structural Insights into GPCR Activation to a later date. Stay tuned for our next symposium on GPCRs as Therapeutics Targets on October 11th, 2024. In the meantime, visit Dr. GPCR Symposia and learn from experts in the field. GPCR Event Highlight We are thrilled to partner with the Adhesion GPCR Consortium to organize our first Dr. GPCR in-person event. Mark your calendar for October 23 - 25, 2024, as we kick off the 11th Adhesion GPCR Workshop in Mexico City. Abstract submissions and registrations will open soon. Stay tuned We are also looking for sponsors to help support this fabulous event that brings together scientists worldwide working on all aspects of adhesion GPCR biology. Please reply to this email if you'd like to sponsor this event. Let’s dive into the Classified GPCR News from April 29th to May 12th, 2024 Adhesion GPCRs Essential Role of Latrophilin-1 Adhesion GPCR Nanoclusters in Inhibitory Synapses Embryonic spatiotemporal expression pattern of Folded gastrulation suggests roles in multiple morphogenetic events and regulation by AbdA GPCR Activation and Signaling The critical importance of conditions: Reconciling GPCR functionality and biophysical findings Adrenoceptor Desensitization: Current Understanding of Mechanisms Biased agonists of GPR84 and insights into biological control GPR84 in physiology-Many functions in many tissues Regulation of the pro-inflammatory G protein-coupled receptor GPR84 Function and regulation of GPR84 in human neutrophils Large-scale deorphanization of Nematostella vectensis neuropeptide G protein-coupled receptors supports the independent expansion of bilaterian and cnidarian peptidergic systems GPCR Binders, Drugs, and more A relaxin receptor gene RpGPCR41 is involved in the resistance of Rhopalosiphum padi to pyrethroids Discovering allatostatin type-C receptor specific agonists Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases MRGPRX4 mediates phospho-drug-associated pruritus in a humanized mouse model GPCRs in Cardiology, Endocrinology, and Taste The Genetic Pathophysiology and Clinical Management of the TADopathy, X-Linked Acrogigantism Thrombosis With Thrombocytopenia and Post-COVID-Vaccination Syndrome With Anti-G-Protein-Coupled Receptor (GPCR) Antibodies Treated With Therapeutic Plasma Exchange SUCNR1 regulates insulin secretion and glucose elevates the succinate response in people with prediabetes GPCRs in Neuroscience Spatiotemporal organization of prefrontal norepinephrine influences neuronal activity Transient cAMP production drives rapid and sustained spiking in brainstem parabrachial neurons to suppress feeding The C-terminus of the prototypical M2 muscarinic receptor localizes to the mitochondria and regulates cell respiration under stress conditions GPCRs in Oncology and Immunology Wnt pathway inhibition with the porcupine inhibitor LGK974 decreases trabecular bone but not fibrosis in a murine model with fibrotic bone The orphan G protein-coupled receptor 141 expressed in myeloid cells functions as an inflammation suppressor The landscape of cancer-rewired GPCR signaling axes Methods & Updates in GPCR Research ONE-GO: Direct detection of context-dependent GPCR activity Author Correction: GPCR molecular dynamics forecasting using recurrent neural networks Glycoprotein-glycoprotein receptor binding detection using bioluminescence resonance energy transfer Bayesian network models identify cooperative GPCR:G protein interactions that contribute to G protein coupling Reviews, GPCRs, and more Molecular adaptations in response to exercise training are associated with tissue-specific transcriptomic and epigenomic signatures Lipid regulation of the glucagon receptor family Technologies for the discovery of G protein-coupled receptor-targeting biologics Lipid mediators in neutrophil biology: inflammation, resolution and beyond Exploring GPCR signaling pathway networks as cancer therapeutic targets Generation of comprehensive GPCR-transducer-deficient cell lines to dissect complexity of GPCR signaling Structural and Molecular Insights into GPCR Function Membrane mimetic-dependence of GPCR energy landscapes Structural and Computational Insights into Dynamics and Intermediate States of Orexin 2 Receptor Signaling Industry News Addex Gets Creative To Secure Funding And Its Future Reunion Neuroscience Inc. Announces $103 Million Series A Financing Co-Led by MPM BioImpact and Novo Holdings Neurocrine Biosciences Announces Initiation of Phase 1 Clinical Study Evaluating Effects of NBI-1117567 in Healthy Adults Crinetics Pharmaceuticals Reports First Quarter 2024 Financial Results and Provides Business Update Nxera Pharma Operational Highlights and Consolidated Results for the First Quarter 2024 Crinetics Pharmaceuticals To Present Advancements From Atumelnant (Crn04894) And Paltusotine Development Programs At Endo 2024 Exscientia's CEO shares a pipeline overview and learnings from being one of the first AI companies out front and to go public GPCR Events, Meetings, and Webinars May 13 - 17, 2024 | 20th Annual PEGS Boston Summit May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 July 8 - 10, 2024 | 4th IRN i-GPCRnet Annual October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs Post Doctoral Fellow Postdoc Position Principal Scientist, In vitro Pharmacology Senior Associate Scientist - Global Research Technologies Novo Nordisk Scientist I - Global Research Technologies Novo Nordisk Postdoctoral Associate Research Technologist I Join Dr. GPCR Ecosystem

G protein-coupled receptors (GPCRs) are integral membrane proteins crucial for sensing extracellular signals, including hormones, neurotransmitters, and environmental cues. These receptors initiate intracellular signaling cascades upon activation, ultimately regulating a myriad of physiological processes. Central to GPCR function are G proteins, comprising subfamilies such as Gs, Gi/o, Gq/11, and G12/13, which orchestrate downstream signaling events, including the modulation of cyclic adenosine monophosphate (cAMP), calcium mobilization, and extracellular signal-regulated kinase (ERK) activation [1]. Traditionally, second messenger assays measuring cAMP accumulation, calcium mobilization, and ERK phosphorylation have been pivotal in deciphering GPCR activity, particularly in drug discovery endeavors [2]. However, these conventional assays often provide limited information on intermediate signaling events due to pathway crosstalk and signal amplification [3]. Also, most second messenger assays are primarily endpoint measurements and do not allow practical measurement of the kinetics of signaling. The emergence of resonance energy transfer (RET) techniques, notably Fluorescence Resonance Energy Transfer (FRET) and Bioluminescence Resonance Energy Transfer (BRET), has revolutionized the study of GPCRs by enabling real-time monitoring of protein-protein interactions and intracellular signaling dynamics[4]. FRET and BRET sensors operate on the principle of energy transfer between a fluorescent or luminescent donor and acceptor molecules within close proximity, typically within 100Å. These biosensors have facilitated the investigation of various aspects of GPCR signaling, including ligand binding (e.g NanoBRET ligand binding [5]), effector protein recruitment assays (e.g G protein recruitment assay [6], mini-G recruitment assay [7], GRK and β-arrestin recruitment assays [8]), G protein activation (e.g TRUPATH assay [9]), receptor trafficking ( e.g FYVE assay [10]),  β-arrestin dynamics ( e.g FLAsH biosensor [11]), cAMP production (e.g CAMYEL assay [12]) , and ERK activity (e.g YEN assay [13]), among others. One of the significant advantages of FRET and BRET-based sensors is their ability to provide real-time readouts of pharmacological activity, allowing for the determination of drug kinetics—a critical aspect in drug development [14]. Moreover, these experiments can be conducted in live cells, preserving the physiological context and minimizing artifacts associated with sample preparation for endpoint measurements. Despite their immense potential, utilizing FRET and BRET sensors in GPCR research comes with challenges, including expensive cost of reagents, optimizing sensor expression levels and adapting these systems to disease-relevant models. Addressing these hurdles is essential for translating findings from cellular models to clinically relevant scenarios. Some innovative solutions have been the development of the BERKY and the ONE-GO biosensors, designed to facilitate their application in disease models[3, 15]. BERKY consists of a membrane linker, a BRET donor, an ER/K α-helix linker, a BRET acceptor, and an active G protein detector. The ONE-GO biosensors, designed in a single vector, incorporate a G protein tagged with a YFP acceptor and a G protein detector tagged with an Nluc donor. Both BERKY and ONE-GO biosensors are engineered to detect the GTP-bound Gα subunit, serving as a proxy for G protein activation and have been optimized for use in detecting GPCR activity in primary cells. In conclusion, FRET and BRET-based sensors have transformed the landscape of GPCR research, offering unprecedented insights into the intricacies of GPCR signaling. These techniques not only enhance our understanding of fundamental cellular processes, but also hold immense promise in accelerating drug discovery efforts by enabling the precise characterization of pharmacological interventions in real time. As technology continues to advance, leveraging RET-based sensors will undoubtedly continue to propel our quest to unravel the complexities of GPCR signaling and pave the way for novel therapeutic strategies. 1.      Gilman, A.G., G proteins: transducers of receptor-generated signals. Annu Rev Biochem, 1987. 56: p. 615-49. 2.      Zhou, Y., et al., Multiple GPCR Functional Assays Based on Resonance Energy Transfer Sensors. Front Cell Dev Biol, 2021. 9: p. 611443. 3.      Maziarz, M., et al., Revealing the Activity of Trimeric G-proteins in Live Cells with a Versatile Biosensor Design. Cell, 2020. 182(3): p. 770-785.e16. 4.      Salahpour, A., et al., BRET biosensors to study GPCR biology, pharmacology, and signal transduction. Frontiers in Endocrinology, 2012. 3. 5.      Zhao, P., et al., Activation of the GLP-1 receptor by a non-peptidic agonist. Nature, 2020. 577(7790): p. 432-436. 6.      Galés, C., et al., Real-time monitoring of receptor and G-protein interactions in living cells. Nat Methods, 2005. 2(3): p. 177-84. 7.      Wan, Q., et al., Mini G protein probes for active G protein-coupled receptors (GPCRs) in live cells. J Biol Chem, 2018. 293(19): p. 7466-7473. 8.      McNeill, S.M., et al., The role of G protein-coupled receptor kinases in GLP-1R β-arrestin recruitment and internalisation. Biochemical Pharmacology, 2024. 222: p. 116119. 9.      Olsen, R.H.J., et al., TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome. Nat Chem Biol, 2020. 16(8): p. 841-849. 10.    Namkung, Y., et al., Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET. Nature Communications, 2016. 7(1): p. 12178. 11.    Strungs, E.G., L.M. Luttrell, and M.H. Lee, Probing Arrestin Function Using Intramolecular FlAsH-BRET Biosensors. Methods Mol Biol, 2019. 1957: p. 309-322. 12.    Jiang, L.I., et al., Use of a cAMP BRET sensor to characterize a novel regulation of cAMP by the sphingosine 1-phosphate/G13 pathway. J Biol Chem, 2007. 282(14): p. 10576-84. 13.    Goyet, E., et al., Fast and high resolution single-cell BRET imaging. Sci Rep, 2016. 6: p. 28231. 14.    Pfleger, K.D., R.M. Seeber, and K.A. Eidne, Bioluminescence resonance energy transfer (BRET) for the real-time detection of protein-protein interactions. Nat Protoc, 2006. 1(1): p. 337-45. 15.    Janicot, R., et al., Direct interrogation of context-dependent GPCR activity with a universal biosensor platform. bioRxiv, 2024.

Hello readers! We got a little busy with all the major events at Dr.GPCR, so our weekly news looks slightly different. We will be back next week with our regular weekly GPCR news digest. In the meantime, you can always check the  Classified GPCR News from the last weeks. Today, we celebrate a huge milestone by releasing Episode #150 of the Dr. GPCR Podcast. Join us in this wonderful episode to meet the team of volunteers behind the work you see. The story behind how Dr.GPCR came to be, the people behind the process, the great anecdotes, and what’s coming next. We also have some important announcements in today’s episode, so join us in this celebration and be the first to know about all the changes coming to Dr. GPCR. Today is also the first session of our hands-on workshop with Dr. Sam Hoare. If you aren't joining us this time, stay tuned for more Dr. GPCR University content coming soon.

Get the GPCR's news in your inbox Contributor Articles Dr. GPCR Monthly Newsletter Weekly GPCR News about the GPCR field Sign Up Latest Classified GPCR News Adhesion GPCRs May 7, 2024 Embryonic spatiotemporal expression pattern of Folded gastrulation suggests roles in multiple morphogenetic events and regulation by AbdA Read More April 29, 2024 Essential Role of Latrophilin-1 Adhesion GPCR Nanoclusters in Inhibitory Synapses Read More April 26, 2024 Dysfunction of the adhesion G protein-coupled receptor latrophilin 1 (ADGRL1/LPHN1) increases the risk of obesity Read More Read more Adhesion GPCR articles Articles from Ecosystem Contributors April 2, 2024 GPCRs are not simple on-off switches: deep dive into GPCR-ligand interactions Read More April 16, 2024 From DNA day to GPCR genomics Read More May 14, 2024 Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light on Cellular Signaling Read More Read more articles from our Contributors Call for GPCR papers September 6, 2023 opnMe GPCR Route 66+ project Read More October 1, 2022 GPCRs: Signal Transduction Read More October 1, 2022 Advances in Computational and Chemical Methods to study GPCR Signal Transduction. Read More GPCR Binders, Drugs, and More May 10, 2024 Discovering allatostatin type-C receptor specific agonists Read More May 10, 2024 Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases Read More May 8, 2024 MRGPRX4 mediates phospho-drug-associated pruritus in a humanized mouse model Read More Receptor Activation and Signaling in GPCRs May 2, 2024 Adrenoceptor Desensitization: Current Understanding of Mechanisms Read More May 1, 2024 Biased agonists of GPR84 and insights into biological control Read More May 1, 2024 GPR84 in physiology-Many functions in many tissues Read More UniversityPrice Premium Monthly $ 24.99 24.99$ Every month Immerse yourself into the GPCR World Valid for 12 months + 30 day free trial Start Free Trial Premium Yearly $ 249.99 249.99$ Every year Immerse yourself into the GPCR World 30 day free trial Start Free Trial Become Dr. GPCR Strategic Partner

Adhesion GPCR Workshop 2024 CINVESTAV , Mexico City, Mexico October 23-25, 2024 Register Welcome to the Adhesion GPCR Workshop 2024, hosted in the vibrant heart of Mexico City at the prestigious venue, CINVESTAV Centro de Investigación y de Estudios Avanzados del IPN (in English: Center for Research and Advanced Studies of the National Polytechnic Institute). Explore the latest Adhesion GPCR research, connect with experts, and ignite innovative discussions in this dynamic field. About the Venue Cinvestav: Centro de investigación y de Estudios Avanzados del IPN Av. Instituto Politécnico Nacional no 2508 Mexico City, C.P. 07360 Room: Auditorium Arturo Rosenblueth *Have an ID card ready (Passport, Driver's license, etc), as this will be required at the venue entrance Premilminary Program Layout October 23, 2024 09:00 AM Registration & Welcoming Remarks October 23, 2024 10:00 AM Flash Presentations October 23, 2024 11:30 AM Coffee Break October 23, 2024 12:00 PM Session I October 23, 2024 01:00 PM Plenary Lecture October 23, 2024 2:00 PM Lunch October 23, 2024 3:00 PM Session II October 23, 2024 7:00 PM Mexico City Nocturnal Tour October 24, 2024 09:00 AM Session III October 24, 2024 10:30 AM Coffee Break October 24, 2024 11:00 AM Session IV October 24, 2024 12:00 PM Plenary Lecture II October 24, 2024 1:00 PM Posters October 24, 2024 2:00 PM Lunch October 24, 2024 3:00 PM Session V October 24, 2024 4:30 PM Board Meeting October 24, 2024 5:00 PM Career Development October 24, 2024 6:00 PM Networking / Dinner / Reception October 25, 2024 09:00 AM Session VI October 25, 2024 10:30 AM Coffee Break October 25, 2024 11:00 AM Session VII October 25, 2024 12:00 PM Plenary Lecture III October 25, 2024 1:00 PM Session VIII October 25, 2024 2:00 PM Lunch October 25, 2024 3:00 PM Session IX October 25, 2024 4:30 PM Closing Remarks AdWork-Register Register for Adhesion GPCR Workshop 2024 Adhesion Workshop for Consortium Members $ 250 250$ Every year Adhesion GPCR Workshop 2024 + One Year Free Premium Membership Select Adhesion GPCR Workshop 2024 One Year Dr. GPCR Premium Membership Adhesion Workshop for Students $ 200 200$ Every year Adhesion GPCR Workshop 2024 + One Year Free Premium Membership Select Adhesion GPCR Workshop 2024 One Year Dr. GPCR Premium Membership Sponsor this event

Dr. GPCR Symposia Virtual - FREE - event series of 1-day. *Talks will be available for later viewing for the Ecosystem’s premium members. Become a Premium member Our Goal 1. Increase the number of events during the calendar year to meet more frequently. 2. Provide more topic-specific events to the GPCR community All Symposia Events are: 1. Virtual 2. Free for all members 3. Poster presentation 4. Networking Event schedule Session 1 - 8 am to 9:30 am EST 15 minutes break Session 2 - 9:45 am to 11: 15 am EST 15 minutes break Poster/Networking on Zoom Breakout Rooms Session 3 - 2 pm to 3: 30 pm EST 15 minutes break Session 4 - 3: 45 pm to 5:15 pm EST GPCRs in Immunology and Oncology November 17, 2023 Details GPCRs as Therapeutic Modalities September 22, 2023 Details Structural and Molecular Insights into GPCR Activation July 21, 2023 Details GPCR Activation and Signaling May 19, 2023 Details Recent Advances in Understanding Challenging GPCRs March 24, 2023 Details SymposiaPrice Premium Monthly $ 24.99 24.99$ Every month Immerse yourself into the GPCR World Valid for 12 months + 30 day free trial Start Free Trial Premium Yearly $ 249.99 249.99$ Every year Immerse yourself into the GPCR World 30 day free trial Start Free Trial Become Dr. GPCR Strategic Partner