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October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system In VSMCs, stimulation of GPCRs also modulates contractile and cell growth phenotypes. Here, we will focus on the relatively less well-studied effects of GPCRs in cardiac fibroblasts, focusing We discuss how such events may be distinct depending on where the GPCRs and their associated signaling Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Dimerization of GPCRs: Novel insight into the role of FLNA and SSAs regulating SST2 and SST5 homo- and hetero-dimer formation "The process of GPCR dimerization can have profound effects on GPCR activation, signaling, and intracellular trafficking. Somatostatin receptors (SSTs) are class A GPCRs abundantly expressed in pituitary tumors where they represent Read more at the source #DrGPCR #GPCR #IndustryNews

December 2021 "Drug development is rarely trivial. Drugs that do make it to clinical trials have major hurdles to clear—not the least of which is safety It is necessary for drugs to evaluated for potential toxicities and side effects, and these key factors must be deemed tolerable before investigators can assess drug potency. Read more at the source #DrGPCR #GPCR #IndustryNews

function and expression landscape Odorant receptors (ORs) belong to the G protein-coupled receptor (GPCR compounds, there has been a growing interest from the scientific community to target this class of GPCRs (for drug repurposing) and endogenous ligands. design. Check the original article at https://pubmed.ncbi.nlm.nih.gov/35999088/ #GPCR #DrGPCR#Ecosystem

August 2022 "Several G-protein coupled receptors (GPCR) are upregulated in Alzheimer's Disease (AD), This article focuses on the role of Aβ granules and their possible interaction with GPCRs that modulate Read more at the source #DrGPCR #GPCR #IndustryNews

2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor (GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

Hello Sweet GPCR Enthusiasts, This week at Dr. GPCR: a new podcast episode with Dr. GPCR Store is live! Rock your favorite design, spark conversations in the lab, and help power everything we build—one mug   — A tale of detergent tails: GPCR activation beyond ligands .   GPCR Team

2022 Fly casting with ligand sliding and orientational selection supporting complex formation of a GPCR simulation was conducted to elucidate binding mechanisms of a middle-sized flexible molecule, bosentan, to a GPCR Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

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 That meant simulations, ligand screening, and experimental design could move forward with confidence. —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

Win on kinetics, not just Kd:  Dynamic binding means “affinity” moves—design readouts and decisions that Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters From Bench Frustrations to Breakthrough Design For decades, GPCR trafficking research relied on overexpression It's designed to help GPCR scientists and teams move faster by consolidating scattered updates into a field 🧠 Designed for researchers at every career stage

By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling pathways over time, and in response to drug treatments in freely-moving adult rats. After several weeks to allow biosensor expression, fiber photometry is used in order to record drug responses spectrum of neuroscience research, ranging from the study of neural circuits and behavior, to preclinical drug Read more at the source #DrGPCR #GPCR #IndustryNews

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. November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug potential agonists of orphan receptor GPR78 targeting CNS disorders Predicting biological activity and design

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

2022 Sosei Heptares and Kallyope Enter Collaboration to Identify and Validate Novel Gastrointestinal GPCR programs in key therapeutic areas Kallyope, pioneers in drug discovery involving the gut-brain axis, the Sosei Heptares compound library for its industry-leading biology platform to identify potential GPCR entered a strategic research collaboration to identify and validate novel G protein-coupled receptor (GPCR . " 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

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

Step into the world of drug discovery with Dr. In this foundational-level  lesson, Terry unpacks the real-life process behind discovering new drugs, with the language, logic, and big-picture view that underpins all future learning in pharmacology and drug Don’t miss your chance to learn from one of the best: Unlock “Introduction to Drug Discovery" now

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

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

What if the way we've been studying GPCRs—arguably the most important drug targets in pharmacology—has Terry Kenakin invites us to challenge outdated assumptions and step into a new era of drug discovery. Here’s the surprising truth: up to 80% of GPCR-targeted drugs fail—not because of poor chemistry, but It’s 40 years of hard-won insight distilled into accessible, high-impact content designed for learners Join Terry’s Corner and stay updated on the latest in GPCR research—delivered in a format that’s as approachable

He has led teams that have filed more than 10 Investigational New Drug Applications (IND), as well as multiple New Drug (NDA) and Supplemental New Drug Applications (SNDA). #biotech #lifesciences #appointment #GPCR #Oncology" Read more at the source #DrGPCR #GPCR #IndustryNews

GPCRs have also been identified within the mitochondria. Therefore, it is essential to design tagging strategies that minimize interference with GPCR function Compartmentalized GPCR Signaling from Intracellular Membranes. Drug discovery today, 24(11), 2192–2201. https://doi.org/10.1016/j.drudis.2019.09.003 Ferrandon, S., Functional selectivity of GPCR-directed drug action through location bias.

July 2022 "Orion Biotechnology and Peptilogics are pursuing AI-driven drug discovery to explore new functional and precision-engineer therapeutics with enhanced potency and tailored signaling against an undrugged GPCR #ai #drugdiscovery #gpcr" Read more at the source #DrGPCR #GPCR #IndustryNews

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 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 Binders, Drugs, and more Persistent challenges in the development of an mGlu7 PAM in vivo tool compound GPCR Industry News Septerna Announces the Formation of a Cross-Functional Scientific and Drug Discovery 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

Watch Episode 167 Some GPCR-targeting antibodies don’t inhibit receptors. They activate them. GPCRs, are likely targets for antibody-based immune responses. This is the future of GPCR immunology . ________________ Keyword Cloud : GPCR autoantibodies , GPCR immunology , GPCR diagnostics , Dr. GPCR ecosystem , multiplex assays

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