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September 2022 "Class A (rhodopsin-like) G protein-coupled receptors (GPCRs) are constitutive phospholipid scrambling is not detectable in the resting plasma membrane of mammalian cells that is replete with GPCRs considered whether cholesterol, a prominent component of the plasma membrane, limits the ability of GPCRs This mechanism may explain the inability of GPCRs to scramble lipids at the plasma membrane." Read more at the source #DrGPCR #GPCR #IndustryNews

What does DNA Day have to do with GPCRs? This intersection of genomics and GPCR research sparked a new era of a comprehensive understanding of GPCR biology, the development of GPCR-targeted drugs, and the exploration of GPCRs as key regulators in the total count of GPCR genes in the human genome. Structural bioinformatics analysis of variants on GPCR function.

August 2022 "Emerging evidence suggests that G protein-coupled receptor (GPCR) kinases (GRKs) are associated reveal an interaction between the βarr2 finger loop domain and ICL2 and ICL3 of APH1A, similar to a GPCR-β-arrestin Read more at the source #DrGPCR #GPCR #IndustryNews

For Dr. GPCR News, please subscribe to your monthly newsletter. Papers GPCRs: Signal Transduction. Deadline extended to March 31st, 2023 GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery Research Fellow - School of Physics and Astronomy Postdoctoral Research Associate (Fixed Term) Explore Dr GPCR Ecosystem

Join us for a fantastic introduction to GPCRdb with Dr. David Gloriam and Dr. Albert Kooistra. Register today: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

September 2022 "G protein-coupled receptor (GPCR) kinases (GRKs) and arrestins mediate GPCR desensitization The spatial pattern of GPCR phosphorylation is predicted to trigger these discrete GRK and arrestin-mediated However, although necessary for some GPCRs, we found that distal C-tail sites might not be sufficient to specify recruitment of STAM1 to βarr1 for other GPCRs. Read more at the source #DrGPCR #GPCR #IndustryNews

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

For drug hunters working at the GPCR interface, the difference between a successful lead and a dead-end For GPCR drug discovery, those hidden details can determine whether a compound advances or stalls. The Hidden Lever in GPCR Research In GPCR pharmacology, the conversation often centers on ligand properties—affinity your topic suggestions Weekly new releases — always fresh, always relevant Live monthly AMA with Dr biotech, pharma & academia 💎 $2999/year — one conference cost = a full year of expert training  (Premium Dr

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

September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular Modulating a single function of a specific aGPCR isoform while affecting no other function and no other Here, we engineered an antibody, termed LK30, that binds to the extracellular region of the aGPCR ADGRL3 Our work provides proof of concept for the modulation of isoform- and ligand specific aGPCR functions therapeutics" Read more at the source #DrGPCR #GPCR #IndustryNews

Unlocking the Puzzle: The Importance of Precision in GPCR Programs and the Hidden Costs of Overlooking A GPCR program can have world-class science, top-tier talent, and millions in funding — and still fail Hiring Won’t Save Your GPCR Drug Discovery Program When a drug discovery program stalls, the default Bad Data Management Is Undermining Your GPCR Drug Discovery Team The real problem isn’t competence. Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn

Did you register for our next Dr. GPCR Virtual Cafe? Register today! Addgene's Dr. research or you want to share your materials, this is the place to go. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe / #gpcr #drgpcr #virtualcafe #addgene

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 Start with our GPCR training program and get hands-on with virtual tools shaping the future of drug discovery

Hi GPCR Enthusiasts (and Arrestin Aficionados!)   This week at Dr. Dr. Led by Dr. Dr. Tom Sakmar and Dr.

By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling Read more at the source #DrGPCR #GPCR #IndustryNews

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

Welcome aboard, GPCR Crew! live and work  in a developing country, please complete this form to enjoy complimentary access to Dr GPCR Event Spotlight 11th Adhesion GPCR Workshop    📍  Mexico City 📅 October 23 - 25, 2024 Get ready Emerging Voices in GPCR Biology in Special Issue of Molecular Pharmacology GPCR Events, Meetings, and November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug

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

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 Internalized Signaling: Same Receptor, Different Story A GPCR response isn’t always over when the receptor Constitutive Activity: When Doing Nothing Still Does Something Some GPCRs simply refuse to stay quiet

But for Ajay Yekkirala, that closed door lit the fuse for a career that would reimagine GPCR therapeutics postdoctoral training at Boston Children’s Hospital and Harvard Medical School, he joined the lab of Dr This environment helped him see science as an ecosystem, where collaboration and interdisciplinary thinking Superluminal Medicines: AI/ML Meets GPCR Pharmacology As Ajay continued to explore how GPCR signaling Takeaway: Ajay Yekkirala’s story is not just about GPCR science or startup success.

Welcome to the 4th official Adhesion GPCR Consortium newsletter! de Investigación y de Estudios Avanzados del IPN (Cinvestav) How did you become involved in adhesion GPCR AB: I became aware of the existence of adhesion GPCRs while completing my graduate studies. The family of adhesion GPCRs called the Latrophilins or ADGRLs first captured my attention due to their postdoctoral training, I joined one of the labs that participated in Latrophilins’ discovery, the lab of Dr

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

Fine-tuning GPCR signaling: conformational dynamics and intracellular responses GPCR signaling is a complex Apart from G proteins, GPCRs engage other effectors for signaling modulation. GPCR kinases (GRKs) and β-arrestins are activated by agonist-bound GPCRs and interact with the receptor Recent years have seen cryo-EM dominate new GPCR structure determinations, offering insight into GPCR-effector Check the original article at https://pubmed.ncbi.nlm.nih.gov/37259558/ #GPCR #DrGPCR #Ecosystem

What if the way we've been studying GPCRs—arguably the most important drug targets in pharmacology—has In the foundational lesson of Terry’s Corner , Dr. Here’s the surprising truth: up to 80% of GPCR-targeted drugs fail—not because of poor chemistry, but Join Terry’s Corner and stay updated on the latest in GPCR research—delivered in a format that’s as approachable

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

I wish Dr. field” — Dr. GPCR University Learner Dr. GPCR Podcast - Surviving Discovery’s Gauntlet Dr. Listen Now – Real Lessons from a GPCR Expert ➤ The future of GPCR isn’t waiting. The Dr. GPCR Team Read Full Edition ➤

The Dr. GPCR Virtual Cafe is back! Our first guest speaker is none other than Dr. Ben Myers! Learn about communication between GPCRs and PKA, Class F GPCR Smoothened & the Hedgehog signaling pathway https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe

Traditionally, GPCR signaling was believed to primarily occur at the plasma membrane. GPCRs have also been identified within the mitochondria. Another challenge is the potential interference of tagging molecules with GPCR function. Compartmentalized GPCR Signaling from Intracellular Membranes. Functional selectivity of GPCR-directed drug action through location bias.

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

cooperative interaction between G βγ subunits and GIRK channels determines both the amplitude and kinetics of GPCR-dependent Read more at the source #DrGPCR #GPCR #IndustryNews