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- Your GPCR Order Has Arrived! ❇ Feb 10 - 16, 2025 | Dr. GPCR Ecosystem
During these four sessions, you'll dive into: Advanced pharmacokinetic modeling The Druglike Quality ✅ Practical Quantification of Allosteric Modulation – May 1, 2025 ✅ Applying the Black/Leff Operational Model to Predict Agonism – October 2, 2025 Premium Members save 25% on enrollment. 2nd GPCR signaling and drug discovery Symposium & Workshop NEW April 2 - 3, 2025 | New therapeutic modalities
- Exploring Career Paths in GPCR Research with Dr. Jacek Mokrosiński | Dr. GPCR Ecosystem
Yamina will schedule a future talk with Jacek about GPCRs as therapeutic modalities. The discussion revealed their interest in GPCRs as therapeutic modalities and possible future collaborations
- Revvity | Dr. GPCR Ecosystem
All four formats are validated in well-established models like GLP1R and Mu opioid receptor (MOR), and
- Did you know allosteric modulators can change the GPCR G protein subtype selectivity? Have a look at this study to dive deep into its molecular mechanism. Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox. | Dr. GPCR Ecosystem
Home → Flash News → Did you know allosteric modulators can change the GPCR G protein subtype selectivity Published on December 12, 2024 Category GPCR Weekly News Did you know allosteric modulators can change to your inbox. ➡ https:// www.ecosystem.drgpcr.com/gpcr-binders-drugs-and-more/design-of-allosteric-modulators-that-change-gpcr-g-protein-subtype-selectivity
- 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
In neuronal cell lines, the use of Gαi bONE-GO revealed that several natural opioid neuropeptides act In neuronal cell lines, the use of Gαi bONE-GO revealed that several natural opioid neuropeptides act
- 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 Published on October 29, 2024 Category GPCR Weekly News Do you know we can discover allosteric modulators
- Game-changer for GPCR research! 🔬🧪 Molecular glues offer a new way to fine-tune receptor signaling, opening doors for next-gen drug discovery Subscribe to the Dr. GPCR Newsletter 📰 and get the latest GPCR News delivered to your inbox ➡️https://www.ecosystem.drgpcr.com/reviews/molecular-glues%3A-a-new-approach-to-modulating-gpcr-signaling-bias #gpcr #drgpcr | Dr. GPCR Ecosystem
delivered to your inbox ➡️https://www.ecosystem.drgpcr.com/reviews/molecular-glues%3A-a-new-approach-to-modulating-gpcr-signaling-bias delivered to your inbox ➡️ https:// www.ecosystem.drgpcr.com/reviews/molecular-glues%3A-a-new-approach-to-modulating-gpcr-signaling-bias
- 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
www.ecosystem.drgpcr.com/adhesion-gpcrs/conformational-coupling-between-extracellular-and-transmembrane-domains-modulates-holo-adhesion-gpcr-function www.ecosystem.drgpcr.com/adhesion-gpcrs/conformational-coupling-between-extracellular-and-transmembrane-domains-modulates-holo-adhesion-gpcr-function
- 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
🔬 On Ep.166 of the Dr.GPCR Podcast, Ben Clements shares how positive allosteric modulators (PAMs) at 🔬 On Ep.166 of the Dr.GPCR Podcast, Ben Clements shares how positive allosteric modulators (PAMs) at
- 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
🌟 This discovery reveals an unusual dual binding mode of FFA and offers tools for site-targeted compound 🌟 This discovery reveals an unusual dual binding mode of FFA and offers tools for site-targeted compound
- Fresh, Fresh, GPCR News ❇ Feb 17 - 23, 2025 | Dr. GPCR Ecosystem
April 1 - 3, 2025 | 2nd Peptide-Based Therapeutics Summit - USA April 2 - 3, 2025 | New therapeutic modalities larval growth and embryonic development in the multivoltine strain of Bombyx more Profiling Allosteric Modulators β-arrestin-1/endothelin axis in human ovarian fibroblasts Methods & Updates in GPCR Research Histamine-modulated
- 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
it's phosphorylated by GRK2 or GRK5, shaping arrestin conformation, complex stability, and engagement mode it's phosphorylated by GRK2 or GRK5, shaping arrestin conformation, complex stability, and engagement mode
- The Practical Assessment of Signaling Bias | Dr. GPCR Ecosystem
📌 Measuring Bias: A Quantitative Approach 🔹 The operational model provides a structured way to measure
