Search Results

GPCR Virtual Cafe with Matthew Eddy scheduled for tomorrow (Sep 29th, 2022) due to Hurricane Ian that #gpcr #drgpcr

What does DNA Day have to do with GPCRs? 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. Furthermore, computational genomics approaches, such as structural bioinformatics analysis, have facilitated drug discovery and design targeting GPCRs, leading to the development of novel therapeutics.

GPCR podcast! Give it a listen to hear from Dr. Thomas P. Sakmar on how the molecular studies of rhodopsin paved the way to understanding #GPCRs Be sure to subscribe https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #drgpcr #gpcr #podcast

Read more at the source #DrGPCR #GPCR #IndustryNews

GPCR podcast is now available! Our guest is Dr. Listen where you get your podcasts. https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ #gpcr #drgpcr #

GPCR Summit 2022 held between October 10th and 16th. Dr. GPCR Summit is FREE for all Ecosystem site members! Become a member today, it's also free! ➡️ https://bit.ly/3wKZmfR #gpcr #drgpcr

Joe Clayton from BioTek Instruments talk about automated micro-plate-based methods for quantifying #GPCR activation. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #drgpcr #gpcr #virtualcafe

Drum rolls, we’ve got 15 GPCR research papers, updates, industry news events, and GPCR ads curated just New ligands and new GPCR behaviors that produce unique drug profiles (i.e., intracellular ligands and Submit your design by August 15, 2024, and stand a chance to have your creation represent this prestigious phytochemical-based drug discovery approach for combating multi-drug resistant Staphylococcus aureus 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery October 2024 | Biologics

GPCR Summit is between October 10th to the 16th! ➡️ https://www.ecosystem.drgpcr.com/dr-gpcr-summit-2022 #gpcr #drgpcr

October 2022 GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral membrane and regulates epithelial apicobasal polarity "The adhesion family of G protein-coupled receptors (GPCRs GPR125 (ADGRA3), an orphan adhesion GPCR, has been shown to modulate planar cell polarity in gastrulating Thus, the basolateral protein GPR125, an autocleavable adhesion GPCR, appears to play a crucial role Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the newsletter HERE

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 have been used in drug design and formed the basis for mechanistic activation hypotheses. adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source #DrGPCR #GPCR

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

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

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that provided molecular insights into the functions and regulation of B2R, which shed light on structure-based drug design for the treatment of B2R-related diseases. In this review, we summarize the structure and function of B2R in relation to drug discovery and discuss Read more at the source #DrGPCR #GPCR #IndustryNews

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

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

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

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

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

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

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

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

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

Drug discovery does not move in fixed conclusions. It is designed as a continuous learning environment — supporting scientific reasoning as programs mature Each experimental decision — system sensitivity, assay configuration, kinetic design — carries strategic GPCR systems are sensitive and context-dependent. Advance promising hits into mechanistic evaluation quickly Use statistics to arbitrate interpretation Design

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

🧠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