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- encoding and decoding selectivity and promiscuity in the human chemokine GPCR interaction network | Dr. GPCR Ecosystem
Home → Flash News → encoding and decoding selectivity and promiscuity in the human chemokine GPCR interaction network Published on July 7, 2025 Category GPCR Weekly News How do chemokines and GPCRs decode selectivity? A landmark Cell paper delivers the answer—mapping how conserved and variable sequence–structure elements govern interaction logic across 46 chemokines and 23 GPCRs. The result: a framework for designing ligands with altered receptor preferences. ♦️ Defines “public” vs. “private” binding determinants ♦️ Highlights role of structured + unstructured regions ♦️ Includes a web tool + viral chemokine engineering demo This is a must-read for GPCR modelers, immunopharmacologists, and ligand engineers. ➡️ Read the paper: https://www.cell.com/cell/fulltext/S0092-8674(25)00398-8 #DrGPCR #GPCR #Chemokines #StructuralBiology #Pharmacology #ProteinEngineering #Immunology #DrugDiscovery Previous Next Recent Articles
- Biased agonism at the GLP-1 receptor: from structure to animal models of disease
Sexton is also a co-founder of Septerna Inc. " Patrick Sexton on the web CCeMMP Monash University Dr.
- Coffee Break with pastries announcement of the aGEM award | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Coffee Break with pastries announcement of the aGEM award Complimentary < Previous Session Next Session >
- Mexico City Nocturnal Tour, Food and drinks | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Mexico City Nocturnal Tour, Food and drinks Coming Soon < Previous Session Next Session >
- New biosensor technologies are shedding light on GPCR dynamics directly in cells, offering exciting possibilities for multiplexing and miniaturization! Curious about how these advances could impact drug discovery? Check out the latest review on GPCR biosensors. Check out the latest GPCR news in the Ecosystem today! You’ll need to register but don’t worry, it’s Free! | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- 📢 All 2025 Dr.GPCR Courses Are Open for Registration! Which one will you choose? 🚀 Whether you're diving into GPCR drug discovery, pharmacology, or advanced modeling, there's a course for you. 💡 Bonus: Premium Members enjoy 25% off on all courses! 🔗 Explore & register today: https://www.ecosystem.drgpcr.com/gpcr-courses #GPCR #DrGPCR #Biotech #DrugDiscovery #Pharmacology | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- Atypical Structure and Function of Typical Chemokine Receptors
The Ramsey Lab Amy Ramsey on the web University of Toronto Pubmed Google Scholar LinkedIn Twitter Dr.
- Did you know? 🌟 Researchers have developed reversibly photoswitchable allosteric modulators for Class A GPCRs! 🧬💡 These innovative compounds, “Photo-BQCisA” and “Photo-BQCtrAns,” offer subtype-selective precision by combining allosteric modulation with light control, paving the way for new therapeutic strategies targeting muscarinic receptors (M1-M5). 🔬✨ Learn more about this breakthrough in the Ecosystem! | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- GPCRs regulate key biological processes, but how exactly do inhibitory Gαi proteins control signal transduction beyond adenylyl cyclase suppression? New research sheds light on these pathways! ✨ Want to learn more? 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! | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- insights into g protein coupling preference from cryo em structures of gq bound PTH1R | Dr. GPCR Ecosystem
Home → Flash News → insights into g protein coupling preference from cryo em structures of gq bound PTH1R Published on July 14, 2025 Category GPCR Weekly News What drives Gq vs. Gs selectivity at PTH1R? This new Nature Chemical Biology paper reveals cryo-EM structures of Gq-bound PTH1R—highlighting how N-linked glycans and ICL2 interactions stabilize receptor conformations that favor Gq coupling. ♦️ Two distinct Gq-bound conformations ♦️ Comparison with Gs-bound PTH1R ♦️ Strategic implications for biased agonist design A critical advance for anyone working on class B1 GPCRs, bone biology, or biased signaling. ➡️ Read the paper: https://www.nature.com/articles/s41589-025-01957-6?utm_content=buffer3b1fa&utm_medium=social&utm_source=twitter.com&utm_campaign=buffer #DrGPCR #GPCR #PTH1R #BiasedAgonism #CryoEM #Pharmacology #Osteoporosis #DrugDiscovery Previous Next Recent Articles
- Session IX / Technology capsule: Light on aGPCR signaling and function | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Full Agenda Adhesion GPCR workshop 2024 CINVESTAV, Mexico City, Mexico October 23-25 Download PDF Program HERE < Back to Full Agenda Session IX / Technology capsule: Light on aGPCR signaling and function NovoiSMART - A new platform for GPCR antibody drug discovery Abstract Developing monoclonal antibody drugs against GPCRs and other multi-pass transmembrane targets, such as ion channels, remains a significant challenge. Novoprotein developed a NovoiSMART technology, utilizing mRNA-based immunization, which can overcome these obstacles by producing high-quality antibodies that more accurately mimic natural protein structures. This approach contrasts with other antigen forms like peptides or DNA, which face limitations in structural integrity and immunogenicity. mRNA technology, demonstrated in the success of COVID-19 vaccines, is emerging as a promising method for antibody discovery. Several case studies of GPCR and other multi-pass transmembrane targets are presented, including GPRC5D, Claudin 6 and Napi2b. These studies show that mRNA immunization yields higher antibody titers and greater epitope diversity compared to other methods. These examples underscore the potential of NovoiSMART technology in developing highly specific antibodies for complex targets, with implications for overcoming challenges like drug resistance and tumor escape. About Gavin Zhang Gavin is a currently a director of business and operations at Novoprotein Scientific. His research experience includes phylogenetics and cancer epigenetics. Gavin Zhang on the web LinkedIn < Previous Session Next Session >
- 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 | Dr. GPCR Ecosystem
Master dose-response, binding, kinetics, and foundational models. Driving drug discovery? Master dose-response, binding, kinetics, and foundational models. Driving drug discovery?
- Ever wondered how we perceive bitterness? 👅🔬 Researchers have unveiled the cryo-EM structure of TAS2R14, the most promiscuous bitter taste receptor, bound to the drug flufenamic acid (FFA) and its signaling partner gustducin! 🌟 This discovery reveals an unusual dual binding mode of FFA and offers tools for site-targeted compound design. 🧪✨ Learn more about this exciting breakthrough in bitter taste signaling. | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- Did you know that GPR20, a potential therapeutic target to treat gastrointestinal stromal tumours, performs high constitutive activity when coupling with Gi? Check out this paper to see how molecular dynamics simulation can be used to explore its constitutive activation mechanism. 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/exploring-the-constitutive-activation-mechanism-of-the-class-a-orphan-gpr20 #gpcr #drgpcr | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- 🔬 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 | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- error | Dr. GPCR Ecosystem
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- 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 | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- 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 | Dr. GPCR Ecosystem
Dr. GPCR News Dec 18, 2025 Scientific Isolation: The Real Reason Early Biotechs Lose Traction The Quiet Drift Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves
- Fresh, Fresh, GPCR News ❇ Feb 17 - 23, 2025 | Dr. GPCR Ecosystem
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- Your GPCR Order Has Arrived! ❇ Feb 10 - 16, 2025 | Dr. GPCR Ecosystem
🎓 Kicking Off Today: Dr. Watch Dr. Kenakin as he introduces the key concepts of this brand-new course.
- error | Dr. GPCR Ecosystem
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- 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! | Dr. GPCR Ecosystem
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. GPCR Ecosystem
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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- 500 | Dr. GPCR Ecosystem
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- 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! | Dr. GPCR Ecosystem
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
- 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 | Dr. GPCR Ecosystem
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
- 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 | Dr. GPCR Ecosystem
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
- 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 | Dr. GPCR Ecosystem
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
- 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 | Dr. GPCR Ecosystem
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
