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. 🚀 Develop New GPCR Skills Join Dr. Tune in to Ep.160 of the Dr.

🎓 Kicking Off Today: Dr. Watch Dr. Kenakin as he introduces the key concepts of this brand-new course.

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Home → Flash News → Exploring the combination of molecular simulation, pharmacological assays, and NMR to reveal the molecular mechanism of biased activation at the vasopressin V2 receptor. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! Published on December 10, 2024 Category GPCR Weekly News Exploring the combination of molecular simulation, pharmacological assays, and NMR to reveal the molecular mechanism of biased activation at the vasopressin V2 receptor. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/high-affinity-elr%2B-chemokine-ligands-show-g-protein-bias-over-%CE%B2-arrestin-recruitment-and-receptor-internalization-in-cxcr1-signalling #gpcr #drgpcr Previous Next Recent Articles

The Practical Assessment of Signaling Bias Dr. Terry Kenakin < Back Workshop Summary Join Dr. Dr. Dr. Dr. Terry Kenakin’s workshop offers a fresh perspective on drug discovery .

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Home → Flash News → Do you know we can discover allosteric modulators that bind to the intracellular allosteric binding site to better fine-tune the GPCRs’ activity? Check out the development of a NanoBRET assay platform to detect intracellular ligands for the chemokine receptors CCR6 and CXCR1. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! Published on October 29, 2024 Category GPCR Weekly News Do you know we can discover allosteric modulators that bind to the intracellular allosteric binding site to better fine-tune the GPCRs’ activity? Check out the development of a NanoBRET assay platform to detect intracellular ligands for the chemokine receptors CCR6 and CXCR1. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/methods-and-updates-in-gpcr-research/development-of-a-nanobret-assay-platform-to-detect-intracellular-ligands-for-the-chemokine-receptors-ccr6-and-cxcr1 Previous Next Recent Articles

Home → Flash News → A newly engineered biosensor reveals DNAJC13 as a key player in GPCR trafficking, shedding light on its role in DOR downregulation and endosomal regulation. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/an-engineered-trafficking-biosensor-reveals-a-role-for-dnajc13-in-dor-downregulation #gpcr #drgpcr Published on March 24, 2025 Category GPCR Weekly News A newly engineered biosensor reveals DNAJC13 as a key player in GPCR trafficking, shedding light on its role in DOR downregulation and endosomal regulation. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https:// www.ecosystem.drgpcr.com/receptor-activation-and-signaling/an-engineered-trafficking-biosensor-reveals-a-role-for-dnajc13-in-dor-downregulation #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! Cutting-edge cryo-EM reveals how LYCHOS, a lysosomal protein, senses cholesterol to regulate metabolism and cell growth ➡️https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/cryo-em-reveals-cholesterol-binding-in-the-lysosomal-gpcr-like-protein-lychos #gpcr #drgpcr Published on February 4, 2025 Category GPCR Weekly News Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! Cutting-edge cryo-EM reveals how LYCHOS, a lysosomal protein, senses cholesterol to regulate metabolism and cell growth ➡️ https:// www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/cryo-em-reveals-cholesterol-binding-in-the-lysosomal-gpcr-like-protein-lychos #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → New insights into FPR2 signaling! GRK5 drives FPR2 endocytosis, but β-arrestin plays a pivotal role in postendocytic trafficking, plasma membrane recycling, and regulating signal transduction. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/grk5-regulates-endocytosis-of-fpr2-independent-of-%CE%B2-arrestins #gpcr #drgpcr Published on January 30, 2025 Category GPCR Weekly News New insights into FPR2 signaling! GRK5 drives FPR2 endocytosis, but β-arrestin plays a pivotal role in postendocytic trafficking, plasma membrane recycling, and regulating signal transduction. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https:// www.ecosystem.drgpcr.com/receptor-activation-and-signaling/grk5-regulates-endocytosis-of-fpr2-independent-of-%CE%B2-arrestins #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → Check out the new optical BRET-based biosensor, Gαi bONE-GO! In neuronal cell lines, the use of Gαi bONE-GO revealed that several natural opioid neuropeptides act as partial agonists, contrary to their previous characterization as full agonists. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️https://buff.ly/e6gAlBv #gpcr#drgpcr Published on April 21, 2025 Category GPCR Weekly News Check out the new optical BRET-based biosensor, Gαi bONE-GO! In neuronal cell lines, the use of Gαi bONE-GO revealed that several natural opioid neuropeptides act as partial agonists, contrary to their previous characterization as full agonists. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https:// buff.ly/e6gAlBv #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → How does a superagonist activate M2 muscarinic receptors? New simulations reveal the conformational changes from inactive to active states to highlighting how ligand dynamics drive GPCR activation! Catch the full story in the Ecosystem! https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/visualizing-agonist-induced-m2-receptor-activation-regulated-by-aromatic-ring-dynamics #GPCR #drGPCR #M2R #drugdiscovery #moleculardynamics Published on March 31, 2025 Category GPCR Weekly News How does a superagonist activate M2 muscarinic receptors? New simulations reveal the conformational changes from inactive to active states to highlighting how ligand dynamics drive GPCR activation! Catch the full story in the Ecosystem! https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/visualizing-agonist-induced-m2-receptor-activation-regulated-by-aromatic-ring-dynamics #GPCR #drGPCR #M2R #drugdiscovery #moleculardynamics Previous Next Recent Articles

Home → Flash News → 🚀 New Learning Opportunities at Dr.GPCR University! Expand your GPCR expertise with exclusive workshops, interactive courses, and an on-demand library—all in one place! ✅ Register for upcoming sessions ✅ Access expert-led content anytime ✅ Enjoy premium benefits & exclusive resources 📢 Don’t miss out—start your learning journey today! 🔗 https://www.ecosystem.drgpcr.com/gpcr-courses #GPCR #DrGPCR #LifelongLearning #drugdiscovery #pharmacology Published on February 25, 2025 Category GPCR Weekly News 🚀 New Learning Opportunities at Dr.GPCR University! Expand your GPCR expertise with exclusive workshops, interactive courses, and an on-demand library—all in one place! ✅ Register for upcoming sessions ✅ Access expert-led content anytime ✅ Enjoy premium benefits & exclusive resources 📢 Don’t miss out—start your learning journey today! 🔗 https://www.ecosystem.drgpcr.com/gpcr-courses #GPCR #DrGPCR #LifelongLearning #drugdiscovery #pharmacology Previous Next Recent Articles

Home → Flash News → Disrupting VIPR2 dimerisation halts breast cancer spread—could TM3-4 peptides be the next breakthrough in targeted cancer therapy? Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/gpcrs-in-oncology-and-immunology/dimerisation-of-the-vip-receptor-vipr2-is-essential-to-its-binding-vip-and-g%CE%B1i-proteins%2C-and-to-its-functions-in-breast-cancer-cells #gpcr#drgpcr Published on May 12, 2025 Category GPCR Weekly News Disrupting VIPR2 dimerisation halts breast cancer spread—could TM3-4 peptides be the next breakthrough in targeted cancer therapy? Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/gpcrs-in-oncology-and-immunology/dimerisation-of-the-vip-receptor-vipr2-is-essential-to-its-binding-vip-and-g%CE%B1i-proteins%2C-and-to-its-functions-in-breast-cancer-cells #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → This study adds a key piece to the puzzle of adhesion GPCR signaling. Understanding receptor-specific nuances, like the role of NTF cleavage, is crucial for decoding their functional outcomes. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️https://www.ecosystem.drgpcr.com/adhesion-gpcrs/n-terminal-fragment-shedding-contributes-to-signaling-of-the-full-length-adhesion-receptor-adgrl3 #gpcr #drgpcr Published on January 28, 2025 Category GPCR Weekly News This study adds a key piece to the puzzle of adhesion GPCR signaling. Understanding receptor-specific nuances, like the role of NTF cleavage, is crucial for decoding their functional outcomes. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️ https:// www.ecosystem.drgpcr.com/adhesion-gpcrs/n-terminal-fragment-shedding-contributes-to-signaling-of-the-full-length-adhesion-receptor-adgrl3 #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → Terry's Corner is Officially LIVE! 🎉 This is your new go-to for mastering drug discovery pharmacology. No fluff, just clear, on-demand insights from Terry Kenakin. Building core expertise? Master dose-response, binding, kinetics, and foundational models. Driving drug discovery? Apply pharmacology to selectivity, ADME, and strategic decision-making. An experienced drug hunter? Sharpen your edge with allosteric bias, residence time, and translational PK/PD. Learn on-demand, apply immediately: https://terrykenakin.com #DrGPCR #GPCR #pharmacology #TerrysCorner #DrugDiscovery Published on July 2, 2025 Category Terry's Corner Terry's Corner is Officially LIVE! 🎉 This is your new go-to for mastering drug discovery pharmacology. No fluff, just clear, on-demand insights from Terry Kenakin. Building core expertise? Master dose-response, binding, kinetics, and foundational models. Driving drug discovery? Apply pharmacology to selectivity, ADME, and strategic decision-making. An experienced drug hunter? Sharpen your edge with allosteric bias, residence time, and translational PK/PD. Learn on-demand, apply immediately: https://terrykenakin.com #DrGPCR #GPCR #pharmacology #TerrysCorner #DrugDiscovery Previous Next Recent Articles

Home → Flash News → How do GPCRs sense pH changes? New cryo-EM structures of GPR4 and GPR68 reveal how extracellular histidines act as proton sensors-trigger activation and biased G protein coupling! Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/structural-basis-and-biased-signaling-of-proton-sensation-by-gpcrs-mediated-by-extracellular-histidine-rearrangement #gpcr#drgpcr Published on May 26, 2025 Category GPCR Weekly News How do GPCRs sense pH changes? New cryo-EM structures of GPR4 and GPR68 reveal how extracellular histidines act as proton sensors-trigger activation and biased G protein coupling! Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️ https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/structural-basis-and-biased-signaling-of-proton-sensation-by-gpcrs-mediated-by-extracellular-histidine-rearrangement #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → Did you know that cell types can affect the GPCR-mediated signalling cascade? Check out this paper to know how different cell types affect the A2BR-mediated calcium signalling system. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/a2b-adenosine-receptor-triggered-intracellular-calcium-mobilization%3A-cell-type-dependent-involvement-of-gi%2C-gq%2C-gs-proteins-and-protein-kinase-c #gpcr #drgpcr Published on January 14, 2025 Category GPCR Weekly News Did you know that cell types can affect the GPCR-mediated signalling cascade? Check out this paper to know how different cell types affect the A2BR-mediated calcium signalling system. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https:// www.ecosystem.drgpcr.com/receptor-activation-and-signaling/a2b-adenosine-receptor-triggered-intracellular-calcium-mobilization%3A-cell-type-dependent-involvement-of-gi%2C-gq%2C-gs-proteins-and-protein-kinase-c #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → 10 GPCR pharmacology lessons. Zero fluff. Launching July 1, Terry’s Corner gives you the clarity and confidence to make better decisions—starting with: • The role of pharmacology in discovery strategy • Black & Leff’s operational model—finally made practical • Binding curves, orthosteric vs allosteric function, and real vs apparent affinity • Molecular dynamics and how they guide ligand design • Why Terry built this—and how it sharpens your next move 📅 Learn anytime. New course every week. 📬 Subscribe to The Kenakin Brief → https://www.terrykenakin.com #GPCRscience #drugdiscovery #TerrysCorner #GPCRpharmacology #ligandbinding Published on June 30, 2025 Category Terry's Corner 10 GPCR pharmacology lessons. Zero fluff. Launching July 1, Terry’s Corner gives you the clarity and confidence to make better decisions—starting with: 🟢 The role of pharmacology in discovery strategy 🟢 Black & Leff’s operational model—finally made practical 🟢 Binding curves, orthosteric vs allosteric function, and real vs apparent affinity 🟢 Molecular dynamics and how they guide ligand design 🟢 Why Terry built this—and how it sharpens your next move 📅 Learn anytime. New course every week. 📬 Subscribe to The Kenakin Brief → https://www.terrykenakin.com #GPCRscience #drugdiscovery #TerrysCorner #GPCRpharmacology #ligandbindingv Previous Next Recent Articles

Home → Flash News → GPCR activation is well-known to be a multi-step process. However, current molecular structures only capture the fully activated complex. Check out this paper to see how scientists combine different techniques to elucidate the intermediate GPCR-mini-Gαsβγ complex at 2.6 Å. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/structure-and-function-of-a-near-fully-activated-intermediate-gpcr-g%CE%B1%CE%B2%CE%B3-complex #gpcr #drgpcr Published on February 11, 2025 Category GPCR Weekly News GPCR activation is well-known to be a multi-step process. However, current molecular structures only capture the fully activated complex. Check out this paper to see how scientists combine different techniques to elucidate the intermediate GPCR-mini-Gαsβγ complex at 2.6 Å. Did you know that we work hard to bring you the most recent GPCR News, weekly? Catch up today in the Ecosystem using your free site membership! ➡️ https:// www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/structure-and-function-of-a-near-fully-activated-intermediate-gpcr-g%CE%B1%CE%B2%CE%B3-complex #gpcr #drgpcr Previous Next Recent Articles

Home → Flash News → Did you know that certain ergot derivatives can produce wash-resistant signalling through the 5-HT2B receptor persisting for many hours without losing potency or efficacy? By using signalling assays, radioligand binding assay, and microscopy, Gaidarov et al. suggested that this phenomenon results from persistently/irreversibly internalised signalling receptor complexes. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/mechanisms-of-constitutive-and-agonist-induced-5-ht2b-internalization%2C-persistent-endosomal-signaling-and-paradoxical-regulation-of-agonist-pharmacology #gpcr#drgpcr Published on May 19, 2025 Category GPCR Weekly News Did you know that certain ergot derivatives can produce wash-resistant signalling through the 5-HT2B receptor persisting for many hours without losing potency or efficacy? By using signalling assays, radioligand binding assay, and microscopy, Gaidarov et al. suggested that this phenomenon results from persistently/irreversibly internalised signalling receptor complexes. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/mechanisms-of-constitutive-and-agonist-induced-5-ht2b-internalization%2C-persistent-endosomal-signaling-and-paradoxical-regulation-of-agonist-pharmacology #gpcr#drgpcr Previous Next Recent Articles

Home → Flash News → Think βCGRP is just αCGRP’s understudy? Think again. New research shows that βCGRP triggers distinct receptor signaling profiles across the CGRP receptor family, challenging the long-held assumption of redundancy. 🔬 A closer look reveals differences in G protein coupling, second messenger production, and receptor trafficking. 📊 This could reshape how we understand CGRP-related physiology—and how we target it in drug design. 🧠 Pain, inflammation, metabolism: the implications go far beyond signaling bias. 🔗 Read the full paper in Biochemistry: Unique Biased Agonism Profile of βCGRP on CGRP Family Receptors #GPCR #CGRP #DrugDiscovery #Pharmacology #SignalTransduction #Neuropeptides Published on June 16, 2025 Category GPCR Weekly News Think βCGRP is just αCGRP’s understudy? Think again. New research shows that βCGRP triggers distinct receptor signaling profiles across the CGRP receptor family, challenging the long-held assumption of redundancy. 🔬 A closer look reveals differences in G protein coupling, second messenger production, and receptor trafficking. 📊 This could reshape how we understand CGRP-related physiology—and how we target it in drug design. 🧠 Pain, inflammation, metabolism: the implications go far beyond signaling bias. 🔗 Read the full paper in Biochemistry : Unique Biased Agonism Profile of βCGRP on CGRP Family Receptors #GPCR #CGRP #DrugDiscovery #Pharmacology #SignalTransduction #Neuropeptides Previous Next Recent Articles