Premium members can enjoy a 25% OFF early bird discount , but hurry - it's only available for a limited Special Offer for Scientists who work and live in developing countries If you live and work in a developing

novel ligands for the A 2A  adenosine receptor. function and ligand-receptor interactions. However, several challenges have limited the use of mutagenesis in drug discovery. Structure-based discovery of A2A adenosine receptor ligands. Molecular determinants of ligand efficacy and potency in GPCR signaling.

GPCR Activation and Signaling Homodimerization of CB2 cannabinoid receptor triggered by a bivalent ligand the GPR37-mTOR-S6K1 Signaling GPCRs in Neuroscience Astrocyte Gi-GPCR signaling corrects compulsive-like

member , you’re also unlocking over 500 minutes of exclusive, expert-led content from thought leaders like Don’t miss out on insightful resources like '   Applying Pharmacology to Drug Discovery ' and ' Advanced Sexton , Denise Wootten , et al., for their work on Isoquinoline small molecule ligands are agonists Positive Allosteric Modulators Enabling Optical Control of the M1 Receptor Isoquinoline small molecule ligands Insights into GPCR Function Monitoring GPCR conformation with GFP-inspired dyes Structural basis for the ligand

GPCR University offers two live courses this fall that you won’t want to miss. 5 to 26, 2024 What You’ll Learn during the four sessions: How to measure pharmacologic activity of ligands (affinity, efficacy, co-operativity) Determining mechanisms of action for new GPCR ligands Key elements 31, 2024 What You’ll Master during the five sessions: Utilizing new cellular assays to analyze GPCR ligand behavior Predicting activity and in vivo target coverage with real-time kinetics Discovering new ligands

(affinity, efficacy, co-operativity) Determining mechanisms of action for new GPCR ligands Elements and effective GPCR discovery Master advanced applications: Using new cellular assays to analyze GPCR ligand behavior Predicting activity and in vivo target coverage with real-time kinetics Discovering new ligands human G protein-coupled receptor biology and pharmacology Industry News Muscarinic drugs breathe new life into schizophrenia pipeline GPCR Dynamics Reveal Mechanisms for Drug Discovery DMS: Linking Protein

Gábor Turu , and László Hunyady  for their research on Functional consequences of spatial, temporal and ligand Kenakin Reading Materials Access to the private group Certificate Explore: Key metrics for assessing ligand pharmacology (affinity, efficacy, co-operativity) Mechanisms of action for new GPCR ligands Essentials for effective GPCR discovery Discover: Advanced cellular assays for GPCR ligand behavior Real-time kinetics for predicting activity Unique drug profiles from new ligands and GPCR behaviors GPCR Event

Application of this knowledge to determine the mechanism of action of new GPCR ligands. New ligands and new GPCR behaviors that produce unique drug profiles (i.e., intracellular ligands and Hosted by the Adhesion GPCR Consortium, this exciting event will occur in lively and culturally rich It is an opportunity to connect with like-minded scientists and researchers and gain valuable insights receptor subtypes Structural insights into ligand recognition, selectivity, and activation of bombesin

heterotrimeric G protein activity biosensors Marta Lopez-Balastegui , Antonella Di Pizio , Jiafei Mao  from July 8th to 14th, 2024 GPCR Activation and Signaling GPR116 alleviates acetaminophen-induced liver Receptor Influence of the Water Model on the Structure and Interactions of the GPR40 Protein with the Lipid Membrane and the Solvent: Rigid versus Flexible Water Models Probing the energy landscape of the lipid 2028 At Rate Of 6.5% Trevena Announces $2M Non-Dilutive Financing Tranche and Reduction in Outstanding Liabilities

Research Computational modelling of dynamic cAMP responses to GPCR agonists for exploration of GLP-1R ligand

Basis of MC1R Activation: Mutation-Induced Alterations in Structural Dynamics Structural insights into ligand Approach Redox-modulated SNX25 as a novel regulator of GPCR-G protein signaling from endosomes Cellular lipids Translation-independent association of mRNAs encoding protomers of the 5-HT 2A -mGlu2 receptor complex in living First R&D Milestone Tectonic bets on GPCR heart failure drug following reverse merger with Avrobio Lilly

However, the impact on structure-based ligand discovery remained uncertain due to the necessity for accurately Lyu et al. prospectively docked ultra-large libraries of molecules against unrefined AF2 models of the Moreover, advanced AI models like AlphaFold3, which can predict complex protein-molecule interactions This proprietary nature limits direct access to the model and imposes a cap on daily predictions. AlphaFold2 structures guide prospective ligand discovery.

Jürgen Wess and Liu Liu for their study on A novel function of the M2 muscarinic receptor Drs. vivo via differential phosphorylation Increased transcriptional elongation and RNA stability of GPCR ligand -PH domain-based fluorescent reporters for visualizing phosphatidylinositol 4-phosphate dynamics in living

Suchismita Roy et al. have explored how growth factors can modulate canonical G protein signaling, shedding light They employed a series of phospho-mimicking mutants and assays such as linear ion trap mass spectrometry Key findings include: Phosphorylation Hotspots: P Loop (Ser44, Ser47, Thr48): Impairs ligand-stimulated Interdomain Cleft (Ser151, Tyr154, Tyr155): Phosphorylation at Tyr154 and Tyr155 impaired ligand-stimulated C Terminus (Tyr320): Phosphorylation at Tyr320 disrupted Gβγ binding, receptor coupling, and ligand-stimulated

Brendan Creemer, Thomas Gardella, and Ross Cheloha for their work on Highly biased agonism for GPCR ligands Badr Sokrat is live! You can now watch podcast episodes in video format on our website. GPCR Activation and Signaling Highly biased agonism for GPCR ligands via nanobody tethering Mechanistic orientation using a neurotensin receptor 1 peptide Illuminating the neuropeptide Y4 receptor and its ligand asthma GPCR Events, Meetings, and Webinars June 2 - 7, 2024 | Chemotactic Cytokines June 4, 2024 | Live

receptors (CKRs) that signal via Gαi and 4 official atypical chemokine receptors (ACKRs) which engage in ligand Indeed, ACKRs behave as scavenging “decoys” in order to either limit chemokines spatial availability sites, while maintaining the responsiveness of canonical G protein-coupled CKRs that bind to the same ligand inflammatory response when needed; and it may interfere with other chemokine receptors which share the ligands CKRs should be considered when evaluating the safety and therapeutic efficacy of blocking receptor-ligand

Jacek Mokrosiński is live! Development of Selective Cannabinoid Receptor 2 Inverse Agonists Development of Putative Bivalent Dicovalent Ligands prospects, and pathophysiological perspectives Structural and Molecular Insights into GPCR Function Bilayer lipids modulate ligand binding to atypical chemokine receptor 3 Industry News New cannabinoid CB1 receptor | ENDO 2024 NEW June 3 - 6, 2024 | BIO 2024 June 2 - 7, 2024 | Chemotactic Cytokines June 4, 2024 | Live

To my surprise and delight, the neurexins happened to be ligands for one isoform of the Latrophilins. AB: The next workshop will likely bring together some of the hottest adhesion GPCR research going on community, added to the fact that this will all take place for the first time in a developing country like The food: While in Mexico, eat like one. The diversity is humongous. What mariachi song are you most likely to shout along to at 3 AM?

Initially, the activation of small GTPases like RAS leads to the activation of the MAP kinase kinase

Azietaku for his first contributor article on Illuminating GPCR Research: FRET and BRET-Based Sensors Shed Light Lyu, Brian Shoichet, Bryan Roth, et al. for their research on AlphaFold2 structures guide prospective ligand Arthur Christopoulos is now live, titled "A Brief History of Allosteric Modulators."  of the Prototypic G Protein-Coupled Adenosine A2A Receptor AlphaFold2 structures guide prospective ligand SLAS Europe 2024 Conference and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines NEW June 4, 2024 | Live

This highlights the power of advanced imaging techniques like cryo-EM in solving complex biological puzzles

Alejandra Tomas, et al. for their study on Lipid regulation of the glucagon receptor family Drs. Please reply to this email if you'd like to sponsor this event. response to exercise training are associated with tissue-specific transcriptomic and epigenomic signatures Lipid glucagon receptor family Technologies for the discovery of G protein-coupled receptor-targeting biologics Lipid pathway networks as cancer therapeutic targets Generation of comprehensive GPCR-transducer-deficient cell lines

We got a little busy with all the major events at Dr.GPCR, so our weekly news looks slightly different

Hoare's workshop for individuals who live and work in developing countries.  mapping G-protein-coupled receptor agonists Development of a synthetic relaxin-3/INSL5 chimeric peptide ligand for NanoBiT complementation binding assays Generation of a deep mouse brain spectral library for transmembrane Structural and Molecular Insights into GPCR Function Fungal alkaloid malbrancheamide reorients the lipid

Hoare's workshop for individuals who live and work in developing countries.  protein signalling and modulates excitability of human induced pluripotent stem cell-derived nociceptive-like Methods & Updates in GPCR Research Alared: Solvatochromic and Fluorogenic Red Amino Acid for Ratiometric Live-cell United With or Without an Additional Transmembrane Sequence Indicate Classification into Three Groups of Linkers

Valery V Fokin  et al. for their research on Virtual Screening of a Chemically Diverse "Superscaffold" Library Enables Ligand Discovery for a Key GPCR Target Gunnar Schulte, Lukas Grätz, Pawel Kozielewicz, et al Hoare's workshop for individuals who live and work in developing countries. If you have any research you would like to showcase to our community, you can submit a poster presentation Enables Ligand Discovery for a Key GPCR Target GPCRs in Cardiology, Endocrinology, and Taste Orphan

Advances in structural genomics, coupled with techniques like X-ray crystallography and cryo-electron The genetic variation in GPCRs is extensive; databases like GPCRdb provide a large database of genetic

Hoare's workshop for individuals who live and work in developing countries. If you have any research you would like to showcase to our community, you can submit a poster presentation Classified GPCR News from April 1st to 7th, 2024 GPCR Activation and Signaling GPRASP1 loss-of-function links Hepatic extracellular ATP/adenosine dynamics in zebrafish models of alcoholic and metabolic steatotic liver