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- A high-resolution deep mutational scan of MC4R reveals how thousands of genetic variants impact obesity-linked signaling pathways and highlights new opportunities for precision drug discovery Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️ https://www.ecosystem.drgpcr.com/receptor-activation-and-signaling/high-resolution-deep-mutational-scanning-of-the-melanocortin-4-receptor-enables-target-characterization-for-drug-discovery #gpcr#drgpcr | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- 📢 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Did you know registrations are already open for all our 2025 Dr.GPCR University Courses? Check out what you can learn this year from the master, Dr. Terry Kenakin 😉and save your spot soon! Remember Premium Members get a 25% discount 🙌 ✳️Click here and start your next learning experience https://www.ecosystem.drgpcr.com/gpcr-courses #gpcr #drgpcr | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Can we preserve opioid pain relief without the side effects? 🔬 On Ep.166 of the Dr.GPCR Podcast, Ben Clements shares how positive allosteric modulators (PAMs) at the mu-opioid receptor could revolutionize treatment —with a 10x boost in methadone efficacy. Tune in for a masterclass on translational pharmacology, curiosity-driven science, and meaningful mentorship. 🎧 Full episode: Ep 166 with Dr. Ben Clements #GPCRresearch #DrGPCR #GPCRpodcast #OpioidPharmacology #DrugDiscovery | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- A large-scale analysis of GPCR molecular dynamics reveals hidden allosteric sites and lateral gateways, unlocking new possibilities for drug discovery. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️https://www.ecosystem.drgpcr.com/structural-and-molecular-insights-into-gpcr-function/large-scale-investigation-of-gpcr-molecular-dynamics-data-uncovers-allosteric-sites-and-lateral-gateways #gpcr#drgpcr | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Scientific careers are not just built on brilliance | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- "Solving financial puzzles feels just like solving scientific ones," says Joe St. Germain from Company Launch Partners. Behind every successful research organization, there is a rock-solid operations team. Don’t miss this rare conversation bridging science, structure, and strategy with Chuck DeWeese & Joe St. Germain. ✳️ Tune in now: Ep 165 with Chuck DeWeese & Joe St. Germain #gpcr #DrGPCR #ScienceStartup | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- New Episode Alert! 🎙️ Ep. 163 of the Dr. GPCR Podcast is here! 🚀 This time, we sit down with Dr. Dmitry Veprintsev to discuss the importance of asking the right GPCR questions. Whether you're a researcher, student, or GPCR enthusiast, this episode is packed with insights that will challenge how you think about your experiments. ✳️Tune in at https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/ep-163-with-dr.-dmitry- #DrGPCR #GPCRPodcast #Pharmacology #DrugDiscovery #Biotech #GPCRs | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- New cryo-EM insights reveal how extracellular domains communicate with transmembrane regions in holo-adhesion GPCRs, uncovering mechanisms behind receptor activation. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️https://www.ecosystem.drgpcr.com/adhesion-gpcrs/conformational-coupling-between-extracellular-and-transmembrane-domains-modulates-holo-adhesion-gpcr-function #gpcr #drgpcr | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- A GPCR imaging breakthrough that didn’t start in a grant proposal | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Weekly News October 16 | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- How GPCR Spatial Signaling Sparked a Scientific Journey | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- 🔬 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Visualizing GPCRs in their native environment changes everything | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- How GPCR Collaboration Built an Innovation Engine | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Flash News: Your Hub for GPCR Insights and Scientific Conference Programs
Michelle Halls unpacks how GPCR signaling isn’t just about ligand–receptor interaction. For decades, molecular modeling focused on explaining — rationalizing why a ligand binds, why a mutation A good model doesn’t just match published structures; it forecasts new biology, new ligands, and new By integrating molecular docking, molecular dynamics, and machine learning, they design ligands with Get it wrong, and the best molecule on paper stalls in development.
- Dr. GPCR Team | Dr. GPCR Ecosystem
She developed expertise over the past two decades studying structure/function relationships of GPCRs Her research centers on developing nanobody-ligand conjugates to target GPCRs, with a focus on receptors Driven by a passion for advancing drug development, John is committed to leveraging his expertise to Further down the track, he aims to apply this knowledge to develop novel chemical treatments for neuronal
- Session VIII * | Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
receptor 110 (ADGRF1, GPR110), an adhesion GPCR recently deorphanized, plays an important role in in the development Synaptamide, an endogenous ligand for GPR110, binds to the N-terminal G-protein autoproteolysis-inducing activation promotes neurogenic differentiation of neural stem cells, neurite growth, and synaptogenesis of developing Regulates Mating In The Closest Relatives Of Animals Alain Garcia De Las Bayonas Abstract "All animals develop
- irreversible drugs post 3 | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Lighting up a native pancreatic islet isn’t just a technical win it’s a shift in what GPCR imaging can reveal | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Dr. Gregory Tall | Dr. GPCR Ecosystem
Mechanical dissociation of the two fragments aided by protein binding ligands and cell movement serves
- 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
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- ama session sept 18 post 1 | Dr. GPCR Ecosystem
affinity experiments are interpreted—and how those interpretations quietly shape SAR, lead selection, and development Experiments: How to Avoid the Most Common Data Pitfalls Binding affinity appears straightforward: add ligand
- Full Agenda for Adhesion GPCR Workshop 2024 | Dr. GPCR Ecosystem
Extracellular Region with Transmembrane Domain in a Holo-Adhesion GPCR Yuling Feng Localization of putative ligands Approach for Drug Discovery for Human Adhesion GPCRs Anne Bormann Intricacies Of Complex Assembly And Ligand
- Your GPCR Order Has Arrived! ❇ Feb 10 - 16, 2025 | Dr. GPCR Ecosystem
. 🗓️ Upcoming 4-Week Course: Development of GPCR Ligands as Therapeutic Drugs starting March 20 – April Highlights of the Week How Ligands Achieve Biased Signaling toward Arrestins Stéphanie Gaillard , Neha A combined in silico approach to design peptide ligands with increased receptor-subtype selectivity Adam Structural and Molecular Insights into GPCR Function A combined in silico approach to design peptide ligands with increased receptor-subtype selectivity Ligand-Independent Spontaneous Activation of Purinergic
