Hello readers! Graham Ladds’ team refines AlphaFold models using binding calculations for human adenosine A3 receptor Kenakin in a small group setting, hurry and register today. Only three spots remain. May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2

Conformationally Selective 2-Aminotetralin Ligands Targeting the alpha2A- and alpha2C-Adrenergic Receptors Novel roles for G protein-coupled receptor kinases in cardiac injury and repair. and release of serotonin. RGS proteins and their roles in cancer: friend or foe?. (July 2 - 7, 2023). 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023) GPCR Jobs NEW Associate

ADX71149 is a selective metabotropic glutamate type 2 (mGlu2) receptor positive allosteric modulator Japan to be included in a potential global development of ADX71149 for the treatment of epilepsy. " Read

of receptor signaling Jiankun Lyu, Brian Shoichet, Bryan Roth, et al. for their research on AlphaFold2 Get ready to share your research with the global GPCR community! ligand discovery Industry News Roche reports positive Phase Ib results for its dual GLP-1/GIP receptor Events, Meetings, and Webinars May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2024 | Biologics US 2024 October 2

Warm greetings and a resounding welcome back to our GPCR Weekly Newsletter, rejuvenated after the festive Only 12 out of 20 spots remain. Registrations are open to Dr. GPCR Ecosystem Members! for CHHs in the mud crab, Scylla paramamosain Reshaping the yeast galactose regulon via GPCR signaling May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2

Hello Readers👋, Thank you for joining us this week. GPCR Activation and Signaling Coupling between GPR143 and dopamine D2 receptor is required for selective Gβγ subunits co-localize with RNA polymerase II and regulate transcription in cardiac fibroblasts. (March 2, 2023) GEM2023. (March 14-17, 2023). SLAS 2023 Building Biology in 3D Symposium. (July 2 - 7, 2023).

Hello readers! Check out our GPCR coverage for this week. Isabella Russell, Drs. After wounding, a G-protein coupled receptor promotes the restoration of tension in epithelial cells May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 NEW October 2024 | Biologics US 2024 October 2

October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system In the former, stimulation of Gs-coupled receptors leads to increases in contractility, whereas stimulation of Gq-coupled receptors modulates cellular survival and hypertrophic responses. We also review the hierarchy of signaling events driving the fibrotic response and the communications Read more at the source #DrGPCR #GPCR #IndustryNews

, the protein kinase mechanistic target of rapamycin complex 1 (mTORC1). Cholesterol bound to the amino-terminal permease-like region of LYCHOS, and mutating this site impaired LYCHOS bound to the GATOR1 complex, a guanosine triphosphatase (GTPase)-activating protein for the Rag By sequestering GATOR1, LYCHOS promotes cholesterol- and Rag-dependent recruitment of mTORC1 to lysosomes Read more at the source #DrGPCR #GPCR #IndustryNews

Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical Here, we review recent developments in single-molecule counting with a focus on photobleaching step counting of oligomerization in G-protein-coupled receptor signaling." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein or β-arrestin signaling pathways, are leading to the development of drugs with superior efficacy and reduced , Gpr3-deficient mice display several adverse phenotypes, including elevated anxiety-like behavior, reduced We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease Read more at the source #DrGPCR #GPCR #IndustryNews

have become immensely interested in predicting the drug target residence time. receptor (GPCR) protein family. contribution of the receptor. Our results build a strong foundation for further improvement of our approach by rationalizing the kinetics Read more at the source #DrGPCR #GPCR #IndustryNews

Such studies revealed that tissue response to a given dose of the hormone or its antagonist depends on receptors that engage the ligand. Thus, we need to know much more about the structures of receptor-ligand complexes at high resolution. Recently, X-ray structures of both AngII receptors (AT1 and AT2 receptors) bound to peptide and non-peptide , as the basis of ligand selectivity, efficacy, and regulation of the molecular functions of the receptors

October 2022 "G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one Recent advances in the structure determination of GPCRs bound to different types of allosteric modulators In this review, we provide a systematic analysis of the currently available GPCR structures in complex with small-molecule allosteric ligands in terms of the location of allosteric pockets, receptor-ligand Read more at the source #DrGPCR #GPCR #IndustryNews

as a potential target in colorectal cancer using novel fluorescent GPCR ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of diseases, but few therapies have been directed We selected the adenosine receptor 2B (A2BAR), specifically expressed in cancer cell lines compared with As well, fluorescent ligands were effective at monitoring real-time A2BAR receptor labeling using live-imaging Read more at the source #DrGPCR #GPCR #IndustryNews

Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases "The chemokine receptor CXCR3 is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies, in particular autoimmune diseases. In a LPS-induced lung inflammation model in mice, ACT-660602 led to significantly reduced recruitment Read more at the source #DrGPCR #GPCR #IndustryNews

Hello readers! Check out our GPCR coverage for this week. official registrations open. and regulates GBP1 expression through GPCR receptor Mthl10 Methods & Updates in GPCR Research Engineering May 16 - 19, 2024 | ASPET 2024 May 27 - 29, 2024 | SLAS Europe 2024 Conference and Exhibition June 2 Phosphorylation and G-Protein Mediated Signaling Networks June 25 - 29, 2024 | FENS Forum 2024 October 2

Happy reading📚! sustained pain relief. by Regulating Ca2+ Flux. The role of G protein conformation in receptor-G protein selectivity. (July 2 - 7, 2023). 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023) GPCR Retreat (November 2

TRPM3's best understood function is its role as a peripheral noxious heat sensor in mice. Moreover, the mechanisms underlying regulation of TRPM3 are largely unexplored. In addition, a micro-RNA gene (miR-204) is located within the TRPM3 gene. The aim of this review is to highlight recent results and developments with particular focus on findings Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Psychedelic research across different disciplines and biological levels is growing at a remarkably fast pace. Considering the central role of the serotonin 5-HT2A receptor in the distinct effects of psychedelics previous preclinical models studying phenomena related to synaptic plasticity. Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "The common mechanisms by which members of the G protein-coupled receptor (GPCR) family respond Here we will discuss recent studies on the diversity of location, effectors, and signaling of GPCRs, Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "G protein-coupled receptors (GPCRs) are the largest family of membrane receptors that serve Classically, GPCR internalization has been considered to lead to receptor desensitization. However, many studies over the past decade have reported that internalized membrane receptors can trigger GPCR internalization dynamics, internalization routes, postinternalization fates, and related diseases Read more at the source #DrGPCR #GPCR #IndustryNews

(GPCRs) are an important receptor superfamily and common therapeutic targets. In this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling As well, it has not been reported whether the effects of temperature on biosensor activity are reversible We found that preincubation and luminescence reading at room temperature were optimal as compared to on biosensor activity was reversible.

to drug treatments in freely-moving adult rats. measuring behavioral responses. After several weeks to allow biosensor expression, fiber photometry is used in order to record drug responses in real time from freely-moving adult rats. Hence, it has wide applicability across a spectrum of neuroscience research, ranging from the study of

F-NMR and single-molecule fluorescence spectroscopy "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF For complete details on the use and execution of this protocol, please refer to Wei et al. (2022) and Read more at the source #DrGPCR #GPCR #IndustryNews

by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells transfected with their cognate receptor "Results of previous studies provided evidence for the existence of a functional gonadotropin-inhibitory However, GnIH peptides did not alter NFAT-RE-luc activity and ERK phosphorylation levels. Our results provide additional evidence for the understanding of signaling pathways activated by GnIH Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Fentanyl activates ovarian cancer and alleviates chemotherapy-induced toxicity via opioid receptor-dependent Although increasing evidence has suggested the direct role of fentanyl on cancer, little is known on Read more at the source #DrGPCR #GPCR #IndustryNews

We have previously reported that the MC4R forms homodimers, affecting receptor Gs signaling properties Recent studies introducing setmelanotide, a novel synthetic MC4R agonist, suggest a predominant role of the Gq/11 pathway regarding weight regulation. Gq/11 signaling of chimeric receptors was analyzed using luciferase-based reporter gene (NFAT) assays Results demonstrate an improvement of alpha-MSH-induced NFAT signaling of chimeras, reaching the level