GPCR Store is live!   — A tale of detergent tails: GPCR activation beyond ligands .   A new commentary highlights how detergents and cholesterol shape mGluR2 activation—no ligand required

This week brings sharp new insights into how minor changes in ligand structure can flip GPCR function When someone signs up for a course, membership, or event through your referral link, you’ll receive a

Terry Kenakin, and catch up on cutting-edge insights through our full library of symposia recordings, Learn the fundamentals of ligand activity, mechanism of action, and GPCR discovery strategy—all at your Arrestin2 binds β₁AR without ligand-induced activation, reshaping our understanding of biased signaling A new cell-based tool detects receptor activity and reveals endogenous ligands.   Whether you're decoding a hidden receptor state or hunting for the next orphan GPCR ligand, we're here

It's starting to look a lot like Christmas at Dr. GPCR! Listen up, folks! VI drives arrestin-independent internalization and signaling of GPCRs Corticotropin-releasing factor-like learning GPCRs in Oncology and Immunology Short-chain fatty acids and cancer The path of GPR87: from a P2Y-like Insights into GPCR Function AlphaFold3 versus experimental structures: assessment of the accuracy in ligand-bound

’s Highlights: G protein-coupled receptor (GPCR) pharmacogenomics Miles D Thompson , David Reiner-Link Recorded GPCR Courses and Symposia / Summit 💲 Special Pricing on GPCR courses GPCR Forum Start a lively Direct line to the Dr. GPCR community members Join the GPCR fan club and geek out with fellows! It's like having a treasure map to academic success! receptors Structural insights into endogenous ligand selectivity and activation mechanisms of FFAR1

High-affinity agonists reveal recognition motifs for the MRGPRD GPCR Chunyu Wang ,  Yongfeng Liu ,  Marion 2025: adding odorant receptors, data mapper, structure similarity search and models of physiological ligand A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR Lior Peri ,   if you go for a Premium Membership , you'll not only back our mission but also snag fantastic perks like Direct line to the Dr.

It challenges you to push your limits, adapt to unforeseen challenges, and develop habits that will serve

a collection of titratable residues spans from the extracellular surface to the transmembrane area, linking strategies, where drugs are designed to target multiple sites or pathways simultaneously, reducing the likelihood Limitations Deep mutational scanning encounters several constraints that affect its broad applicability DMS requires considerable resources, including time, financial investment, and specialised expertise, limiting Future directions As deep mutational scanning continues to evolve, its future directions will likely

De Graaf   for their excellent work on Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability Targeting G Protein-Coupled Receptors Olfactive Biosolutions Establishes Scientific Advisory Board GLP-1s like signaling-competent receptors GPCRs in Neuroscience Astrocyte Gi-GPCR signaling corrects compulsive-like intestinal dendritic cells Methods & Updates in GPCR Research Generation of CRISPR/Cas9 modified human iPSC line Molecular Insights into GPCR Function Comparative Study of Allosteric GPCR Binding Sites and Their Ligandability

While GPCRs can exist as monomers, some types, like class C GPCRs, are obligate dimers, either as homodimers For example, dimerization has been shown to affect signaling pathways in class A dopamine receptors like both homodimers and heterodimers, which may play a crucial role in modulating receptor function and ligand These dimeric interactions may contribute to the phenomenon of biased agonism, where ligands produce Harikumar, K.G., et al., Impact of secretin receptor homo-dimerization on natural ligand binding.  

Apply unique pharmacologic assays and unconventional ligands to unveil GPCR activities. Adjust ligand kinetics and tissue disposition for optimal therapeutic activity. Environment Tailored to Your Needs Maximize your learning experience by accessing our comprehensive library Get ready to be blown away by our fantastic lineup of speakers HERE ! Let's make your brand shine like never before!

,  Andrea Vernall , et al. for their fantastic paper on Development of Putative Bivalent Dicovalent Ligands New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and November 14th : The Application of GPCR Ligand Kinetics to Candidate Design. November 21st : Unconventional GPCR Ligands as Drugs. December 5th : Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit.

New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and November 14th : The Application of GPCR Ligand Kinetics to Candidate Design. November 21st : Unconventional GPCR Ligands as Drugs. December 5th : Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit. 🌟 Get pumped up - the complete agenda is live; don't miss out HERE !

for predicting G protein-coupled receptor (GPCR) structures, especially when experimental data were limited However, this method has limitations: its accuracy is heavily dependent on the availability and quality In a recent study on TAAR1, a GPCR linked to central nervous system disorders, researchers compared the synthetic compounds, limiting its utility in drug discovery involving novel drug-like molecules. Ligand discovery from a dopamine D3 receptor homology model and crystal structure.

Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing 🌟 Exciting news - the complete agenda is live; check it out HERE ! GPCRs in Oncology and Immunology GPR37 promotes colorectal cancer against ferroptosis by reprogramming lipid metabolism via p38-SCD1 axis Methods & Updates in GPCR Research GPCRSPACE: A New GPCR Real Expanded Library Study Conformational Dynamics and Signaling in Drug Discovery Flavors of GPCR signaling bias Glucagon-like

Biased agonism is a phenomenon where different ligands acting on the same receptor trigger distinct signaling the glucagon-like peptide-1 receptor (GLP-1R). Compared to the endogenous ligand GLP-1, another endogenous ligand, oxyntomodulin, exhibits a bias towards In contrast, ligands like oxyntomodulin that preferentially activate ERK1/2 signaling interact more significantly Indeed, incretin-based drugs like Novo Nordisk's Wegovy and Eli Lilly's Zepbound are advancing diabetes

reproduction of C. elegans Alexei Sirbu , Paolo Annibale , et al., for their study on Cell swelling enhances ligand-driven But act fast – this offer is only available for a limited time. Not a premium member yet? Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing through IHH Signaling GPCR Activation and Signaling Illuminating GPCR trafficking Cell swelling enhances ligand-driven in Cardiology, Endocrinology, and Taste Role of G protein coupled receptors in acute kidney injury Ligand-Dependent

advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel biosensor shed light Therefore, it’s a great molecular tool for proximity labeling approaches in living cells. 

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

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 predicting activity Unique drug profiles from new ligands and GPCR behaviors GPCR Event Highlight GPCR oligomers in live cells Industry News Confo Therapeutics Announces EUR 60M Series B Financing to

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

News 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