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article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian Bender , Chris De Graaf for their excellent work on Comparative Study of Allosteric GPCR Binding Sites

article Class B1 GPCR Dimerization: Unveiling Its Role in Receptor Function and Signaling Sonja Peter , Brian Bender , Chris De Graaf   for their excellent work on Comparative Study of Allosteric GPCR Binding Sites

September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular regions that bind to multiple ligands to regulate key biological functions including neurodevelopment and organogenesis. Modulating a single function of a specific aGPCR isoform while affecting no other function and no other receptor is not trivial. Here, we engineered an antibody, termed LK30, that binds to the extracellular region of the aGPCR ADGRL3, and specifically acts as an agonist for ADGRL3 but not for its isoform, ADGRL1. The LK30/ADGRL3 complex structure revealed that the LK30 binding site on ADGRL3 overlaps with the binding site for an ADGRL3 ligand – teneurin. In cellular-adhesion assays, LK30 specifically broke the trans-cellular interaction of ADGRL3 with teneurin, but not with another ADGRL3 ligand – FLRT3. Our work provides proof of concept for the modulation of isoform- and ligand specific aGPCR functions using unique tools, and thus establishes a foundation for the development of fine-tuned aGPCR-targeted therapeutics" Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing using ligands with differing levels of selectivity and affinity as GPR84 antagonists. Although blockade of GPR84 may potentially prove effective also in diseases associated with inflammation of the lower gut there is emerging interest in defining if agonists of GPR84 might find utility in conditions in which regulation of metabolism or energy sensing is compromised. Here, we consider the physiological and pathological expression profile of GPR84 and, in the absence of direct structural information, recent developments and use of GPR84 pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR #IndustryNews

Angiotensin-(1-7) improves cognitive function and reduces inflammation in mice following mild traumatic brain injury "Traumatic brain injury (TBI) is a leading cause of disability in the US.

Bryan Roth and Brian Krumm for their study on Molecular glues as potential GPCR therapeutics Drs. Extensive location bias of the GPCR-dependent translatome via site-selective activation of mTOR GPCR Binders

Structure-guided design of a peripherally restricted chemogenetic system Hye Jin Kang , Brian E Krumm , Adrien Tassou , Bryan L Roth , et al. 🕶 University CheatSheet is here! subtypes in rat pituitary Synthetic GPCRs for programmable sensing and control of cell behaviour GPCR Binders

Brian Krumm and Bryan Roth studied CryoEM structures of adhesion in GPCR CD97, filling gaps. biology β-arrestin1 is an E3 ubiquitin ligase adaptor for substrate linear polyubiquitination GPCR Binders

agonists reveal recognition motifs for the MRGPRD GPCR Chunyu Wang ,  Yongfeng Liu ,  Marion Lanier ,   Brian K Shoichet ,  Esther Martinborough ,  Jonathan F Fay ,  Can Cao ,   Bryan L Roth , et al. and spatial regulation of β-arrestin recruitment through Gβ5 and GRK3 at the μ-opioid receptor GPCR Binders

CUB domain of the adhesion GPCR ADGRG6/GPR126 is a key regulator of receptor signaling Jiankun Lyu, Brian Shoichet, Bryan Roth, et al. for their research on AlphaFold2 structures guide prospective ligand discovery extracellular CUB domain of the adhesion GPCR ADGRG6/GPR126 is a key regulator of receptor signaling GPCR Binders

fantastic paper on Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor Bryan Roth  and Brian Krumm  for their excellent study on Molecular glues as potential GPCR therapeutics Sabrina pro-resolving effects through positive allosteric modulation of the prostaglandin EP4 receptor GPCR Binders

Katharina Grotsch, Bryan L Roth, Valery V Fokin  et al. for their research on Virtual Screening of a Frizzleds act as dynamic pharmacological entities Marina Casiraghi, Robert J Lefkowitz, Peter Gmeiner, Brian peptide-induced relaxation of human coronary arteries: A key role for Gβγ subunit instead of cAMP GPCR Binders

Brian Arey is doing. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

Brian Arey, and Dr. J. Silvio Gutkind. adrenergic receptor Signal transduction at GPCRs: Allosteric activation of the ERK MAPK by β-arrestin GPCR Binders

Brian K. Shoichet, Dr. Luc Van Hijfte and Dr. Wendy Young.

This week's highlight includes congrats to: Makaía M Papasergi-Scott, Peter Gmeiner, Brian K Kobilka, in a High Fat Diet-induced Mouse Model of Obesity GPCRs in Neuroscience Xanthurenic acid: A role in brain

Franziska M Heydenreich, Michel Bouvier, Brian Kobilka, M Madan Babu, and their team's work on Molecular mud crab, Scylla paramamosain Reshaping the yeast galactose regulon via GPCR signaling cascade GPCR Binders

a Family A GPCR Jun Xu , Geng Chen , Haoqing Wang , Sheng Cao , Jie Heng , Xavier Deupi , Yang Du , Brian show G protein bias over β-arrestin recruitment and receptor internalization in CXCR1 signalling GPCR Binders

The blood-brain-barrier (BBB) and the complexity of the central nervous system (CNS) pose a challenge GPCR Structure, Activation, and Signaling Pathways in the Brain An understanding of GPCR structure is When the endogenous binder of the GPCR (which can be a neuromodulator, neurotransmitter, etc.), binds Greater specificity : allows for selective tracking of receptor subtypes in complex brain tissues.

This renders full-length recombinant GPCRs useless for analytical purposes, a problem that can be overcome quantitative Western blot analysis of CB1 receptor expression on crude synaptosomes of the adult rat brain

It wasn’t until his postdoctoral years at UCSF—under Brian Shoichet—that GPCRs entered his scientific

Action A non-pheromone GPCR is essential for meiosis and ascosporogenesis in the wheat scab fungus GPCR Binders Mouse Models of Social Interaction and Cognitive Impairment GPCRs in Neuroscience The Drosophila blood-brain

GPCR Binders, Drugs, and more Modelling altered signalling of G-protein coupled receptors in inflamed GPCRs in Cardiology, Endocrinology, and Taste Gender Differences in GRK2 in Cardiovascular Diseases and

Bryan Roth, Sudarshan Rajagopal, and Graeme Milligan. Save the date! Dr. GPCR Binders, Drugs, and more Development of a 5-HT7 receptor antibody for the rat: the good, the bad

signal through distinct β-arrestin 2-dependent pathways to regulate pancreatic β cell function GPCR Binders Neuroscience Dopaminergic Input Regulates the Sensitivity of Indirect Pathway Striatal Spiny Neurons to Brain-Derived

Live-tissue visualization Cell-type-specific receptor mapping Validation in both the periphery and brain effects are tied to where agonists bind Weight-loss and appetite effects often originate in precise brain This imaging tool is now being used to: Re-evaluate where GLP-1 and GIP receptors matter most Clarify brain

chromatography-mass spectrometry (LC-MS) based cell binding assay, using centrifugation to separate binders from non-binders.

Bryan Roth, Peter Gmeiner, and Thomas P. Sakmar this week. For Dr. GPCR Binders, Drugs, and more Design of Drug Efficacy Guided by Free Energy Simulations of the β2 -Adrenoceptor

GPCR Binders, Drugs, and more Novel targets for potential therapeutic use in Diabetes mellitus. Understanding Neuropeptide Transmission in the Brain by Optical Uncaging and Release.

Bryan L Roth study on Illuminating the understudied GPCR-ome Save the dates: February 8 - 29: Dr. Functional profiling of the G protein-coupled receptor C3aR1 reveals ligand-mediated biased agonism GPCR Binders