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September 2022 "Morphine, the most widely used analgesic, relieves severe pain by activating the μ-opioid receptor (MOR), whereas naloxone, with only slight structural changes compared to morphine, exhibits inhibitory effect, and is used to treat opioid abuse. The mechanism by which the MOR distinguishes between the two is unclear. Molecular dynamics (MD) simulations on a 1-μs time scale and metadynamics-enhanced conformational sampling are used here to determine the different interactions of these two ligands with MOR: morphine adjusted its pose by continuously flipping deeper into the pocket, whereas naloxone failed to penetrate deeper because its allyl group conflicts with several residues of MOR. The endogenous peptide ligand endomorphin-1 (EM-1) underwent almost no significant conformational changes during the MD simulations. To validate these processes, we employed GIRK4S143T, a MOR-activated Gβγ-protein effector, in combination with mutagenesis and electrophysiological recordings. We verified the role of some key residues in the dynamic recognition of naloxone and morphine and identified the key residue I322, which leads to differential recognition of morphine and naloxone while assisting EM-1 in activating MOR. Reducing the side chain size of I322 (MORI322A) transformed naloxone from an inhibitor directly into an agonist of MOR, and I322A also significantly attenuated the potency of MOR on EM-1, confirming that binding deep in the pocket is critical for the agonistic effect of MOR. This finding reveals a dynamic mechanism for the response of MOR to different ligands and provides a basis for the discovery of new ligands for MOR at the atomic level." Read more at the source #DrGPCR #GPCR #IndustryNews

Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier Stuart Maudsley, Nicole Perry-Hauser, Lauren Slosky, Cesare Orlandi, and Simone Prömel. Dr. GPCR University Save the date for our upcoming workshop starting May 9th, 2024, featuring Dr. Dr. Terry Kenakin's "Applying Pharmacology to Drug Discovery" course at Dr. Dr.

Simone Prömel et al. for their study on the effect of Flamingo (FMI-1) on body size and extracellular Isabella Russell, Drs. Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier Dr. April 22 - 23, 2024 | Endocrine Metabolic GPCRs Join Dr. GPCR Founder Dr.

This week's highlight includes congrats to: Christina Katharina Kuhn, Drs. Howard Rockman, and Dr.  Franziska Heydenreich, Sudarshan Rajagopal, Graham Ladds, Cesare Orlandi, Simone Prömel and Michel Bouvier Dr. GPCR University Great News! The Dr. Dr.

This week's highlight includes congrats to: André Nguyen Dietzsch, Simone Prömel, et al. for their work We are pleased to announce five full scholarship opportunities for Dr. Join our upcoming Dr. GPCR University hands-on workshop with Dr.  The workshop includes: Four x 2-hour Zoom sessions One-on-one meeting with Dr. Hoare Access to Dr. Dr.

Weekly Highlights: Congrats to: Daniel Matúš , Simone Prömel , et al., for their work on The N terminus-only And access over 500 minutes of recorded classes in our  GPCR courses with Drs. Join us for an exciting discussion with Dr. live and work  in a developing country, please complete this form to enjoy complimentary access to Dr

It's spring break at Dr. Learn more about Live Masterclasses ➤ Partner Webinars Eurofins DiscoverX (Dr. GeneTex (Dr. Alex Ball)  — A reagent gap that holds back the biology. Details coming soon. Next Week in Boston The Dr. GPCR community gathers in person next week. Come find us ➤ About Dr. GPCR Dr. GPCR is the intelligence and community for GPCR scientists.

This week's GPCR papers feature publications from Drs. Vladimir Katanaev and Patrick Sexton. Remember to join us tomorrow, May 19th, for the highly anticipated Dr. To receive our monthly newsletter, please subscribe to Dr. GPCR News. Review Committee Recommends Continuing Study Addex Therapeutics in the 23rd BioEquity Europe Conference Simon Scientist—Immuno-Oncology Convergent Research - Senior Scientist, Cell-Based Assay Development Explore Dr

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In Episode 168 of the Dr. GPCR Podcast, Dr. And that mindset is precisely what makes their new partnership with Dr. GPCR so powerful. ” — Dr. That’s the mission. ” — Dr. Maria Majellaro Now, as official partners of the Dr. Keyword Cloud:   GPCR data platform , fluorescent ligands , assay development , GPCR research community , Dr

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The Corner comes will live monthly AMA sessions with Dr. Kenakin. GPCR Updates Learn Pharmacology That Drives Discovery  – From Dr. Explore Dr. This blog post breaks down Dr. Stay curious,   The Dr. GPCR Team

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In this Terry’s Corner lesson, Dr. Join before year-end to secure both. 👉   Join Terry's Corner Before Dec 31st, 2025 🎧 Dr. Hudson 🎧 Catch up on Part 2 with Dr. GPCR Year in Review: Carrying Better Experiments Into 2026 As 2025 closes, the Dr. Beyond access, Premium sustains the nonprofit mission behind Dr.

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Hello GPCR Innovators ,   We’re preparing to launch Terry’s Corner, a new knowledge hub shaped by Dr. Plus, Celtarys explores ligand selection for better assays, and co-founder Dr. pain relief in preclinical models Dr.GPCR Updates Terry’s Corner  – Build Better GPCR Screens with Dr Screening Strategy Leadership in Ligand Design  – The Celtarys Origin Story   In  this founder interview , Dr Best,   The Dr. GPCR Team