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Gregory Tall and team's study on GPR114/ADGRG5, activated by tethered-peptide-agonist, a cleaved adhesion Submit poster abstracts here; short talks will be selected from Abstracts. substance use disorders Industry News Crinetics’ Once-Daily Oral Paltusotine Achieved The Primary And All Stephen Dowd As Chief Business Officer Septerna Announces Novel GPCR-targeted Program Acquired by Vertex Call

Kenakin’s latest lecture delivers a wake-up call for pharmacologists interpreting allosteric binding Batman ) and master the Hall model  to decode the thermodynamics behind complex binding behavior . residual signal effects ✅ Tools to model binding with cooperativity factors (α, β, γ, σ) using the Hall Thermodynamics > Intuition: Why the Hall Cube Matters To untangle complex binding behaviors, you need case study, Kenakin shows how G protein availability  determines whether you see “displacement” at all

August 2022 "GPCRs in Medicinal Chemistry Event 8th RSC / SCI symposium on GPCRs in Medicinal Chemistry Dates Wednesday-Friday, 5th-7th October 2022 Place Evotec Campus Levi-Montalcini, Verona, Italy Downloads and Links Registration closing dates: 6th September – registration against invoice (bank transfers): Tuesday, 6th September 30th September – online registration (card payments)" Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "WELCOME 4GPCRnet meeting bringing together four of the biggest GPCR networks in Europe for a joint meeting in Leipzig. Four of the biggest European networks on GPCR research (COST Actions Adher’n Rise and ERNEST plus DFG-funded SFB1423 and FOR2372) have joined forces to organize an international meeting, which will take place from 26th-29th September 2022 in the beautiful city of Leipzig in Germany. We aim to connect renowned international experts of the field with early career ‘rising stars’. The event will take place in the heart of Leipzig, which offers a colorful mixture of culture and vivid social life." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "Join Us in Boston for Discovery On Target 2022! Discovery on Target (DOT) highlights advances in current and emerging “hot” targets and technologies, as well as target validation strategies for the discovery and development of novel therapeutic agents ranging from biologics to small molecules." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 RAB-Symposium - Regulatory Autoantibodies Targeting GPCRs. September 15-16, 2022. Lübeck, Germany. Hybrid meeting. "Dear Sir or Madam, dear Colleagues, It gives me great pleasure to announce the fourth hybrid symposium on regulatory autoantibodies targeting G-protein-coupled receptors (GPCRs) in Lübeck. GPCRs are involved in a variety of physiological and pathophysiological processes. So far, numerous therapeutics targeting GPCRs have been developed, with a focus on small molecules and monoclonal antibodies for the treatment of cancer, infections, metabolic disorders or inflammatory diseases. Recently, functional autoantibodies targeting GPCRs have been associated with various disease-specific manifestations, highlighting a potential new area for therapeutic intervention. Therefore, the aim of this symposium is to bring together the current knowledge on the role of autoantibodies targeting GPCRs in various diseases, such as cardiovascular diseases, renal diseases, autoimmune diseases such as systemic sclerosis or systemic lupus erythematosus. In addition, one aim is to bring together the mode of action of autoantibodies in immune regulation and pathogenesis." Read more at the source #DrGPCR #GPCR #IndustryNews

August 2022 "We are happy to announce you our 2nd IRN i-GPCRnet meeting that will be held at the University of Wurzburg (Germany) from september 30th to october 1rst." Read more at the source #DrGPCR #GPCR #IndustryNews

Here, we provide evidence that distal carboxyl-terminal tail (C-tail), but not proximal, phosphorylation site-directed mutagenesis and bioluminescence resonance energy transfer approaches that distal, not proximal, C-tail In addition, we show that GPCRs that have similarly positioned C-tail phosphoresidues are also able to However, although necessary for some GPCRs, we found that distal C-tail sites might not be sufficient In conclusion, this study provides evidence that distal C-tail phosphorylation sites specify GRK-βarrestin-mediated

Bursicon receptor gene HLGR2 as a potential RNA interference target for control of the fall webworm Hyphantria

March 2022 "Geneva, Switzerland, March 7, 2022 – Addex Therapeutics (SIX: ADXN, Nasdaq: ADXN), a clinical-stage pharmaceutical company pioneering allosteric modulation-based drug discovery and development, announced today that it will issue its full-year 2021 financial results on Thursday, March 10, 2022. Tim Dyer, CEO, Roger Mills, CMO and Robert Lütjens, Head of Discovery Biology, will provide a business update and review its pipeline during a teleconference and webcast for investors, analysts and media at 16:00 CET (15:00 GMT / 10:00 EST / 07:00 PST) the same day. " Read more at the source #DrGPCR #GPCR #IndustryNews

April 2022 John Streicher talks about his work on terpenes found in cannabis as these may be a novel with cannabis, but John Streicher, PhD, takes a closer look at the plant’s aromatic chemical compounds called

Did you register for our next Dr. GPCR Virtual Cafe? Register today! Addgene's Dr. Joanne Kamens is our guest. If you need a plasmid for your 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

Toll-like receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent

protein constructs GST-CB1414-472 and GST-CB1414-442 containing much of the human CB1 receptor C-terminal tail To this end we used three different antibodies, all raised against a peptide comprising the C-terminal

The all-atom MD simulations reveal that CBD induces conformational changes linked with agonist-bound

Targeted Drug Design through GPCR Mutagenesis: Insights from β2AR China M Payne ,   Cam Sinh Lu ,   Karen Gregory We aim to make education accessible to all! behavior in important human cell regulator, opening up a new drug target for cancer, other diseases Call

L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A., & May, L. T. (2016).

The GPCR rocket is all fueled and ready to blast off into a galaxy of incredible advancements, now powered activity-modifying proteins in obesity and diabetes mellitus Maleesha Ubhayarathna , Christopher Langmead , Gregory disorders: Opportunities and hurdles for clinical development 👨‍💻 Why would you want to miss out on all Being a premium member means you get to enjoy all the freebies plus: Access to the recorded classes Exclusive access to private groups  Over 30 recorded talks from Symposia - that's a lot of brain food

of GPCR-G protein selectivity revealed by structural pharmacology Yao Lu, Drs Christopher Langmead,  Gregory

a single compound, resulting in a novel category of GPCR ligands referred to as 'bitopic' (Valant, Gregory

Most teams don’t stall because the science is weak. They stall because the data becomes a mess. I call it the Lego Bucket Problem : You’ve got CRO output, internal assay data, maybe even some promising Decisions stall. And momentum quietly dies. True Embedded Partnership I review CRO scopes, flag risks early, and sit in on your strategic calls. Let’s talk through your program—no pitch, just clarity.

All of the talks were fantastic, but Maria would love to highlight these three: -            First, Prof Wendy Young’s talk, during session 3 on day 2, was also incredible. Katerina Leftheris’ talk, which talked about new and innovative technologies used to overcome peptides Also, there was a great balance between academic and industrial talks. Session 8 on Thursday was Maria’s turn to give a talk.

talent:  When senior leaders spend nights copy-pasting data, your burn rate accelerates while innovation stalls Featured Talk: Dr. Terry Kenakin on The Kinetics of Allostery . signals today will lead tomorrow’s breakthroughs—and avoid delays others won’t see coming. 👉 Don’t Fall Kenakin is a masterful teacher and communicator." — DrGPCR University Attendee The difference between stalled

  — A tale of detergent tails: GPCR activation beyond ligands .   A structural cautionary tale for all of us.  Want the full breakdown? From sugar-sensing structures to strategic partnerships—GPCRs remain at the center of it all.

Breakthroughs this week:  Why Everyone’s Talking About Metabolic GPCRs; GPS for proteins: Tracking the Power analysis tells you exactly how many replicates you need for 95% confidence. Eliminate subjective calls:  From t-tests to ANOVA and F-tests, know which tool to apply when, so debates Whether you’re in discovery, translation, or strategic leadership, Premium ensures you never fall behind signals today will lead tomorrow’s breakthroughs—and avoid delays others won’t see coming. 👉 Don’t Fall

The assays are running, data is flowing in from your CROs or your internal labs , yet progress stalls drawn to the same critical challenges: missed opportunities, misaligned systems, and promising programs stalling I call this the Lego Bucket Problem . You have the data, but not the definitive direction. 📌 Learn more about my services: Yamina.org 📅 Book a 30-minute strategy call: https://calendly.com

For GPCR drug discovery, those hidden details can determine whether a compound advances or stalls. By increasing sensitivity, so-called “silent” antagonists reveal themselves as weak agonists. of accelerated GPCR-targeting innovation, these advantages define which programs advance and which stall orthosteric and allosteric interactions as interchangeable, you’re leaving precision (and money) on the table

Drugs that look great in vitro fall apart in humans. A Call for Patient-First Science Serafini’s strategy isn’t just about method — it’s about mindset.

Terry Kenakin to elevate your science and sharpen your calls. But kinetics tells the truth. signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming. 👉 Don’t Fall Everything you need to master GPCR science — in one membership. 🎓 Full GPCR University + 🔬 200+ expert talks

This week, we focus on how to convert ambiguous data into confident, defensible Mechanism of Action calls—before druggability 🔹 The role of cryo-EM in capturing fully activated GPCR complexes 📅 Catch Aaron’s full talk signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming. 👉 Don’t Fall