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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 → 🔬 Enhance Your GPCR Expertise with Dr.GPCR University! Looking to sharpen your skills in GPCR pharmacology, drug discovery, data analysis, or project management? Dr.GPCR University offers industry-focused courses designed to help you stay ahead in the field. ✅ Comprehensive course library covering cutting-edge GPCR science ✅ Practical insights for real-world drug discovery challenges ✅ Flexible, on-demand learning to fit your schedule 🚀 Elevate your expertise today: Start learning now #GPCR #Pharmacology #DrugDiscovery #Biotech #DrGPCR Published on March 11, 2025 Category GPCR Weekly News 🔬 Enhance Your GPCR Expertise with Dr.GPCR University! Looking to sharpen your skills in GPCR pharmacology, drug discovery, data analysis, or project management ? Dr.GPCR University offers industry-focused courses designed to help you stay ahead in the field. ✅ Comprehensive course library covering cutting-edge GPCR science✅ Practical insights for real-world drug discovery challenges✅ Flexible, on-demand learning to fit your schedule 🚀 Elevate your expertise today: Start learning now #GPCR #Pharmacology #DrugDiscovery #Biotech #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

Home → Flash News → How do GRK-specific phosphorylation barcodes influence β-arrestin binding to GPCRs? New cryo-EM structures from Chen et al. (Nature, 2025) reveal that β-arrestin1 and β-arrestin2 form distinct complexes with ACKR3 depending on whether it's phosphorylated by GRK2 or GRK5, shaping arrestin conformation, complex stability, and engagement mode. Surprisingly, arrestin’s finger loop didn’t dive into the receptor core. Instead, it latched onto the micelle surface, breaking canonical expectations. Also, β-arrestin2 lacks a membrane anchor, making it more dynamic — a potential clue to its functional specialization. These findings underscore how barcode location + arrestin isoform = unique signaling outcomes. open book Read the full study: Inside Out: Mapping GPCRs from Membrane Codes to Market Moves #GPCRs #Arrestin #ACKR3 #GRKs #CryoEM #StructuralBiology #SignalingBias #Phosphorylation #DrGPCR Published on June 9, 2025 Category GPCR Weekly News How do GRK-specific phosphorylation barcodes influence β-arrestin binding to GPCRs? New cryo-EM structures from Chen et al. (Nature, 2025) reveal that β-arrestin1 and β-arrestin2 form distinct complexes with ACKR3 depending on whether it's phosphorylated by GRK2 or GRK5, shaping arrestin conformation, complex stability, and engagement mode. Surprisingly, arrestin’s finger loop didn’t dive into the receptor core. Instead, it latched onto the micelle surface, breaking canonical expectations. Also, β-arrestin2 lacks a membrane anchor, making it more dynamic — a potential clue to its functional specialization. These findings underscore how barcode location + arrestin isoform = unique signaling outcomes. Read the full study: Inside Out: Mapping GPCRs from Membrane Codes to Market Moves #GPCRs #Arrestin #ACKR3 #GRKs #CryoEM #StructuralBiology #SignalingBias #Phosphorylation #DrGPCR Previous Next Recent Articles