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Receptor-Selective Fluorescent Probes and Applications in Single-Molecule Microscopy of Wild-Type Receptors Dr We’re thrilled to announce our upcoming courses with Dr. Terry Kenakin! Courses Schedule and Benefits Every Thursday at 10 am EST Online Lectures 1:1 meeting with Dr. Cryo-Electron Microscopy Postdoctoral Research Associate Senior Scientist - Discovery Biotherapeutics Join Dr

Episode 85 of the Dr. GPCR podcast is here! 🎧Hear Dr. Watch the full video with a paid Dr.

🎙️ Episode 87 of the @DrGPCR podcast with Dr. Bianca Plouffe is available!

November 2021 Dr. Kevin Pfleger and Dr. "Congratulations to Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of

📢 Did you know that this 3rd Edition of the Dr.

the kinetic factors that enhance in vivo efficacy beyond traditional potency metrics, as presented by Dr Dr. That's exactly what Dr. Dr. Submit your paper today to secure your work in Volume II ➤ Why Dr.

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🌟The Dr. GPCR event of the year is the 3rd edition of the Summit. Become a Dr. GPCR Ecosystem site member to attend the Summit, it’s free!

. 🔍 This Week in Dr. This week, Dr. Featured Talk: Dr. Terry Kenakin on The Kinetics of Allostery . Secure your seat today ➤ Why Dr. Read the Premium edition here ➤ What our members say 🗣️ "Dr.

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Join Dr. Here’s who we've talked to so far: 🎥 Check out the interview with Dr. . 🌐 Why Dr. GPCR Is in This Conversation At Dr.   📚 Terry’s Corner — The Only On-Demand Pharmacology Hub with Dr. Kenakin Himself If you’re part of the Dr.

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September 2022 "Phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2) lipids have been shown to stabilize an active conformation of class A G-protein coupled receptors (GPCRs) through a conserved binding site, not present in class B GPCRs. For class B GPCRs, previous molecular dynamics (MD) simulation studies have shown PI(4,5)P2 interacting with the Glucagon receptor (GCGR), which constitutes an important target for diabetes and obesity therapeutics. In this work, we applied MD simulations supported by native mass spectrometry (nMS) to study lipid interactions with GCGR. We demonstrate how tail composition plays a role in modulating the binding of PI(4,5)P2 lipids to GCGR. Specifically, we find the PI(4,5)P2 lipids to have a higher affinity toward the inactive conformation of GCGR. Interestingly, we find that in contrast to class A GPCRs, PI(4,5)P2 appear to stabilize the inactive conformation of GCGR through a binding site conserved across class B GPCRs but absent in class A GPCRs. This suggests differences in the regulatory function of PI(4,5)P2 between class A and class B GPCRs." Read more at the source #DrGPCR #GPCR #IndustryNews

July 2022 "I’m happy to share that I’m starting a new position as Scientific co-founder LASEREDD Therapeutics" Ross Bathgate Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "In the Wnt-β-catenin pathway, Wnt binding to Frizzled (Fzd) and LRP5 or LRP6 (LRP5/6) co-receptors inhibits the degradation of the transcriptional coactivator β-catenin by recruiting the cytosolic effector Dishevelled (Dvl). Polymerization of Dvl at the plasma membrane recruits the β-catenin destruction complex, enabling the phosphorylation of LRP5/6, a key step in inhibiting β-catenin degradation. Using purified Fzd proteins reconstituted in lipid nanodiscs, we investigated the factors that promote the recruitment of Dvl to the plasma membrane. We found that the affinity of Fzd for Dvl was not affected by Wnt ligands, in contrast to other members of the GPCR superfamily for which the binding of extracellular ligands affects the affinity for downstream transducers. Instead, Fzd-Dvl binding was enhanced by increased concentration of the lipid PI(4,5)P2, which is generated by Dvl-associated lipid kinases in response to Wnt and which is required for LRP5/6 phosphorylation. Moreover, binding to Fzd did not promote Dvl DEP domain dimerization, which has been proposed to be required for signaling downstream of Fzd. Our findings suggest a positive feedback loop in which Wnt-stimulated local PI(4,5)P2 production enhances Dvl recruitment and further PI(4,5)P2 production to support Dvl polymerization, LRP5/6 phosphorylation, and β-catenin stabilization." Read more at the source #DrGPCR #GPCR #IndustryNews

Dr. Register and join your colleagues in September ➤ Why Dr. GPCR Premium Membership Gives You an Edge In a world filled with noise, Dr. ” - DrGPCR University Course Attendee Get a competitive advantage—Join Dr.

Tomorrow is the day for another Dr. GPCR Virtual Cafe. This time with none other than Dr. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

June 2022 "We’re delighted to welcome Dr Ed Brennan as our new Vice President, Head of Clinical Development Dr Brennan has extensive experience across all phases of clinical development, and across multiple therapeutic

Dr. GPCR University Masterclass — Integrated GPCR Discovery in Practice Dr. Explore Dr. Prediction without validation creates risk. 👉 Listen to the Full Episode ➤ Why Dr. Dr. Join Dr. GPCR Premium — Build Your Structured Advantage ➤

November 2021 Read more at the source #DrGPCR #GPCR #IndustryNews

Excited to hear Dr. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe #drgpcr #gpcr #virtualcafe

Excited to hear Dr. automated micro-plate-based methods for quantifying #GPCR activation. https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe

Come attend this month's virtual café talk to see the awesome work of Dr. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #gpcr #drgpcr #virtualcafe

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Be sure to signup for the next Virtual Cafe of Dr. GPCR on the 24th of June! This time, the GPCRdb team ( Dr. David Gloriam , Dr. Reserve your spot for free at: https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe/ #GPCR #GPCRs #DrGPCR