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October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical Recent advances in X-ray crystallography and cryo-EM have resulted in a wealth of GPCR structures that adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source #DrGPCR #GPCR

October 2022 Identification of A2BAR 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 against GPCRs in the field of cancer, partly because of the lack Here, using colorectal cancer (CRC) as a model, we explored the gene expression of a panel of GPCRs in Read more at the source #DrGPCR #GPCR #IndustryNews

🧠Do you want to share your #GPCR knowledge? Come to Dr. GPCR Ecosystem and create a course on your favorite #GPCR research, technique and more… Available for GPCR Ecosystem paid memberships ➡️https://bit.ly/3R8ZZbo #gpcr #drgpcr

we explore how computational tools—especially AlphaFold —are helping crack the mystery of olfactory GPCRs The Problem: Hundreds of Receptors, Almost No Ligands Alessandro’s work focuses on olfactory GPCRs—nearly : Predicting the “Face” of a Receptor When Alessandro began his PhD, structural models of olfactory GPCRs —Alessandro Nicoli A New Era of GPCR Research AlphaFold didn’t just fill a gap—it shifted the focus of By iteratively refining the models with docking and mutagenesis data, they developed predictive pipelines

Hi GPCR Enthusiasts (and Arrestin Aficionados!)   This week at Dr. GPCR, we’re decoding arrestin-driven signaling and spotlighting the tools to match.   of GPCR-RAMP discovery. GPCR Updates   Advanced Methods for the Optimization of Candidate Selection  – Master GPCR behavior beyond From dual-epitope tagging to scalable multiplex assays, this conversation dives deep into the tools now

2022 "The very large G protein-coupled receptor (VLGR1, ADGRV1) is the largest member of the adhesion GPCR We confirmed the interaction of VLGR1 with key proteins of MAMs by pull-down assays in vitro complemented by in situ proximity ligation assays in cells. Read more at the source #DrGPCR #GPCR #IndustryNews

Welcome to the 4th official Adhesion GPCR Consortium newsletter! AB: I became aware of the existence of adhesion GPCRs while completing my graduate studies. to how pharmacological approaches will be developed, i.e., splice isoform-specific agonist/antagonist take place for the first time in a developing country like Mexico, is paramount. a suite of transcriptional reporter, G protein activation and B-arrestin recruitment assays.

assumption about how your molecule behaves in a living system can sink months of work and millions in development GPCR signaling almost never follows a straight path. This article is about one big idea: GPCRs don’t act in isolation—they respond to the system they’re in In this session, you’ll gain: ✅ A mental model you can trust  for predicting how GPCR ligands behave Constitutive Activity: When Doing Nothing Still Does Something Some GPCRs simply refuse to stay quiet

biosensors are based on the principle of Förster resonance energy transfer (FRET), and we have recently developed By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling neuroscience research, ranging from the study of neural circuits and behavior, to preclinical drug development Read more at the source #DrGPCR #GPCR #IndustryNews

The cross-talk between growth factor receptors and GPCRs is an intriguing area of study. They employed a series of phospho-mimicking mutants and assays such as linear ion trap mass spectrometry , BRET, pull down, and transwell cell migration assays to investigate the effects of these modifications , leading to segregation of RTK-to-Gαi pathways from canonical GPCR-to-Gαi pathways. This knowledge could inform the development of therapeutic strategies aimed at targeting specific phosphorylation

Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells GPCRs are present How Fluorescent Probes Enable High-Resolution Confocal Imaging of GPCRs To study the dynamics of GPCRs Ligand-directed labelling strategies  are a newly developed way to attach a fluorescent tag to a GPCR other ligands and are very interesting in TR-FRET (Time-Resolved Förster Energy Resonance Transfer) assays A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

GPCR Summit 2022 held between Oct. 10 - 16, it's FREE! Join the #GPCR movement by signing up now! ➡️ https://bit.ly/3cKMXlw #gpcr #drgpcr

GPCR event of the year is the 3rd edition of the Summit. Come join us from October 10 to 16 to hear about exciting #GPCR research from amazing speakers. GPCR Ecosystem site member to attend the Summit, it’s free! ➡️ https://bit.ly/3SUkB8D #gpcr #drgpcr

October 2022 Regulation of pulmonary surfactant by the adhesion GPCR GPR116/ADGRF5 requires a tethered activation mechanism "The mechanistic details of the tethered agonist mode of activation for the adhesion GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

Watch Episode 167 Today’s GPCR scientists don’t want to study one interaction, they want to model the Dual-epitope tagged constructs (N-term FLAG, C-term 1D4) Compatible with multiple readouts: proximity, immuno assays protein interactions  (e.g., 14-3-3) Heterodimerization Endogenous vs. overexpressed systems Orphan GPCR Listen to the complete episode to learn more. _________________ Keyword Cloud : GPCR scientist network , GPCR online course , GPCR data platform , multiplex assays , GPCR drug discovery

But what are the conformation changes that drive GPCR dimerization? How dynamic are GPCRs dimer interfaces? GPCRs constantly bind to form dimers and dissociate to form monomers. But how can we target GPCR dimers? via%3Dihub #GPCR #DrGPCR#Ecosystem

GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry In this session, you’ll gain: Why saturation and displacement assays fail when protein stoichiometry The midpoint and maximum—core parameters for downstream modeling—are only meaningful when the assay fully Displacement Curves and the Illusion of Potency Displacement assays measure affinity when no traceable Equilibration time:  Many assays stop before the system reaches equilibrium, especially with slow competitors

We found that some agonist-induced GPCR/14-3-3 signal intensities can rapidly decrease. could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach for GPCR drug development by modulating GPCR/14-3-3 signals temporally." Read more at the source #DrGPCR #GPCR #IndustryNews

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GPCRs have also been identified within the mitochondria. holds promise for the development of novel therapeutic interventions12. This may involve the development of specialized delivery vehicles, such as nanoparticles or liposomes Compartmentalized GPCR Signaling from Intracellular Membranes. Functional selectivity of GPCR-directed drug action through location bias.

July 2022 Confo Therapeutics receives €1.7 million VLAIO grant for further research on GPCR modulators The grant should help expand Confo Therapeutic’s research on G protein-coupled receptor (GPCR) drug candidates . " Read more at the source #DrGPCR #GPCR #IndustryNews

what would later become Blue Therapeutics, a startup he co-founded to develop non-addictive pain medications Superluminal Medicines: AI/ML Meets GPCR Pharmacology As Ajay continued to explore how GPCR signaling behavior computationally predictable, Ajay and his team are working to reduce the time and cost of developing early career redirection to startup setbacks, each step has added new layers to his thinking about drug development He also underscores the value of developing cross-functional skills — including communication, strategy

Tom Sakmar didn’t set out to map GPCR-RAMP interactions across hundreds of receptors. , multiplexed platform to investigate GPCR-RAMP biology  like never before. the help of Luminex technology and collaborators at SciLifeLab in Sweden , the lab built a multiplex assay interactions , Family B GPCRs , GPCR scientist network , GPCR data platform , Dr. GPCR ecosystem

Embark on this week’s thrilling updates in GPCR research, learning opportunities, and industry developments Topics: New cellular assays, real-time kinetics, and unique GPCR behaviors. Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing into the latest developments in adhesion GPCR biology. , and more Progress on the development of Class A GPCR-biased ligands GPCRs in Cardiology, Endocrinology

Affinity, Developability, and Serum Persistence Exhibits Excellent Antitumor Potency. GPCRs in Neuroscience Role of G-Proteins and GPCR-Mediated Signalling in Neuropathophysiology. BioSpace Sosei Heptares Notes its Partner Tempero Bio has Received FDA Clearance to Advance Clinical Development Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Ecosystem

Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE

GPCR Activation and Signaling Molecular Mechanisms of PTH/PTHrP class B GPCR Signaling and Pharmacological GPCR Binders, Drugs, and more Persistent challenges in the development of an mGlu7 PAM in vivo tool compound Papers GPCRs: Signal Transduction. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Ecosystem

, and more Life, death and resurrection of plant GPCRs Structural and Molecular Insights into GPCR Function Papers GPCRs: Signal Transduction. GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Summit | February 21-23, Boston. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. GPCR Ecosystem

'unproductive coupling'[1] and a fascinating phenomenon known as GPCR priming [2]. The enhanced signalling observed in GPCR priming is attributed to the formation of temporal non-cognate-GPCR GPCR priming opens new avenues for understanding the nuanced regulatory mechanisms governing GPCR signalling This has significant implications for drug development, as targeting these non-cognate interactions could lead to novel therapeutic strategies for modulating GPCR activity.