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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 → Did you know that GPR180 helps regulate lipid metabolism and may play a role in preventing obesity? recent study shows that overexpression of GPR180 in adipose tissue improves lipid metabolism and protects against HFD-induced obesity, while its knockout worsens lipid accumulation. This finding highlights GPR180 as a potential therapeutic target for metabolic disorders! Catch up on this exciting research in the Ecosystem today! 🏆📖 You’ll need to register, but don’t worry—it’s free! ➡️https://www.ecosystem.drgpcr.com/gpcrs-in-cardiology-endocrinology-and-taste/gpr180-reduces-adiposity-by-inhibiting-lipogenesis-and-fatty-acid-uptake-in-adipocytes #gpcr #drgpcr #metabolism #obesity Published on March 3, 2025 Category GPCR Weekly News Did you know that GPR180 helps regulate lipid metabolism and may play a role in preventing obesity? recent study shows that overexpression of GPR180 in adipose tissue improves lipid metabolism and protects against HFD-induced obesity , while its knockout worsens lipid accumulation . This finding highlights GPR180 as a potential therapeutic target for metabolic disorders! Catch up on this exciting research in the Ecosystem today! 🏆📖 You’ll need to register, but don’t worry—it’s free ! ➡️ https:// www.ecosystem.drgpcr.com/gpcrs-in-cardiology-endocrinology-and-taste/gpr180-reduces-adiposity-by-inhibiting-lipogenesis-and-fatty-acid-uptake-in-adipocytes #gpcr #drgpcr #metabolism #obesity 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 → 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