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Different reviews have extensively described the success and failure in drug discovery on chemokine receptors This redundancy can be seen as problematic in drug discovery as blocking a single receptor might not Another important aspect in CKRs targeted drug discovery is the concept of biased agonism/antagonism, Drug discovery is shifting towards the development of biased ligands, which promote the engagement of Further difficulties arise from the existence of cross-reactivity with other GPCRs and differences in

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 #

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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

April is the month of DNA Day, a special day commemorating the discovery of the DNA double helix structure The discovery of DNA's double helical structure was a scientific milestone that revolutionized molecular Genomics, in turn, played a crucial role in the discovery and sequencing of the beta-adrenergic receptor GPCR biology, the development of GPCR-targeted drugs, and the exploration of GPCRs as key regulators discovery and design targeting GPCRs, leading to the development of novel therapeutics.

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

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

Course Schedule and Details Every Thursday at 10 am EST Principles of Pharmacology in Drug Discovery The required elements of a comprehensive and effective GPCR Discovery. 2. Principles of Pharmacology in Drug Discovery II - Advanced Methods for the Optimization of Candidate 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

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

As researchers, we all understand the importance of data in driving meaningful discoveries  and advancing unanswered questions about blockbuster weight-loss drugs Transforming Drug Discovery: Insights from Drug Discovery February 15 - 19, 2025 | BPS 2025 February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28 Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR

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

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

Development and challenges in the discovery of 5-HT1A and 5-HT7 receptor ligands. IPO: A star scientist, GPCR drug discovery and a plan to challenge pharma in diabetes TGA’s approval Endocrine Society Awards Baxter Prize to Innovator in Endocrine Drug Discovery Upstream Bio Announces Deadline extended to March 31st, 2023 GPCR Events, Meetings, and Webinars 2nd GPCR-Targeted Drug Discovery GPCR Jobs Computational drug design PhD student at the Department of Drug Design and Pharmacology Computational

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

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 Updates   New Podcast Episode  - When to Walk, When to Run with Dr. GPCR Store is live!   — A tale of detergent tails: GPCR activation beyond ligands .   GPCR Team

GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled and complex drug targets, remain central in modern targeted drug discovery. The 19th Annual GPCR-Based Drug Discovery conference (October 2-3, 2024, in Boston and online) gathers Join us October 2-3 at the GPCR Drug Discovery Conference . Webinar - The value of GPCR cell-based assays in drug discovery September 30 - October 3, 2024 | 22nd

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

we explore how computational tools—especially AlphaFold —are helping crack the mystery of olfactory GPCRs More accurate hypotheses, faster ligand discovery, and new strategies to tackle one of biology’s most From Prediction to Discovery One of Alessandro’s projects focused on receptor R5VK1 , where his team This case study highlights why computational chemistry is no longer a side tool—it’s a driver of discovery Start with our GPCR training program and get hands-on with virtual tools shaping the future of drug discovery

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

October 2022 "While the role of G-protein-coupled receptors (GPCR) in cancer is acknowledged, their underlying Protease-activated receptors (PAR), a subgroup of GPCRs, form a family of four members (PAR1-4) centrally We propose that Pc(4-4) may serve as a powerful drug not only toward PAR-expressing tumors but also for Read more at the source #DrGPCR #GPCR #IndustryNews

Let's set sail towards exciting discoveries and groundbreaking achievements together! Highlights: Our fearless leader, Yamina Berchiche , is gearing up to rock the mic today at the 22nd Discovery November 21st : Unconventional GPCR Ligands as Drugs. Webinars September 30 - October 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024   26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress

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

If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is assumptions to interpret allosteric binding data, you're likely missing critical insights—or mislabeling your drug Unlock “Allosteric Binding” Now Only in Terry’s Corner Why Terry’s Corner Drug discovery isn’t slowing built for scientists who want to move faster , think sharper , and make smarter decisions  in early discovery Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology

Watch Episode 169 What if you could earn a PhD while supporting a family and working full time in drug discovery? Pin proves it’s possible to have it all, if you design it yourself. _________________ Keyword Cloud: GPCR training program , GPCR scientist network , GPCR drug discovery , G protein-coupled receptors , GPCR

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

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide Extensive efforts of structural biology have been made on the study of GPCRs. Herein we evaluated the accuracy of GPCR structure models predicted by AlphaFold2. differences impeded the use of predicted structure models in the functional study and structure-based drug Read more at the source #DrGPCR #GPCR #IndustryNews