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- 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 >
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- 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
Home → Flash News → 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! Published on October 24, 2024 Category GPCR Weekly News 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! ➡️ https:// www.ecosystem.drgpcr.com/reviews/gpcr-biosensors-to-study-conformational-dynamics-and-signaling-in-drug-discovery #GPCR #DrGPCR #biosensor Recent Articles Previous Next
- 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 Recent Articles Previous Next
- 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 Recent Articles Previous Next
- 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 Recent Articles Previous Next
- 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
Home → Flash News → 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! Published on December 3, 2024 Category GPCR Weekly News 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! ➡️ buff.ly/4fgX4ZH #gpcr #drgpcr Recent Articles Previous Next
- 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 | Dr. GPCR Ecosystem
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 Recent Articles Previous Next
- 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 Recent Articles Previous Next
- 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
Home → Flash News → 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! Published on October 22, 2024 Category GPCR Weekly News 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! ➡️ https:// www.ecosystem.drgpcr.com/receptor-activation-and-signaling/germline-mutations-in-a-g-protein-identify-signaling-cross-talk-in-t-cells #GPCR #DrGPCR Recent Articles Previous Next
- 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 | Dr. GPCR Ecosystem
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 Recent Articles Previous Next
- 🚀 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 | Dr. GPCR Ecosystem
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 Recent Articles Previous Next
- 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 | Dr. GPCR Ecosystem
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 Recent Articles Previous Next
- 🔬 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
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 Recent Articles Previous Next
- 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 | Dr. GPCR Ecosystem
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 Recent Articles Previous Next
- 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 | Dr. GPCR Ecosystem
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 Recent Articles Previous Next
- 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
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 Recent Articles Previous Next

