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A µ-opioid receptor modulator that works cooperatively with naloxone.
O'Brien ES, Rangari VA, El Daibani A, Eans SO, Hammond HR, White E, Wang H, Shiimura Y, Krishna Kumar K, Jiang Q, Appourchaux K, Huang W, Zhang C, Kennedy BJ, Mathiesen JM, Che T, McLaughlin JP, Majumdar S, Kobilka BK. O'Brien ES, et al. Nature. 2024 Jul;631(8021):686-693. doi: 10.1038/s41586-024-07587-7. Epub 2024 Jul 3. Nature. 2024. PMID: 38961287 Free PMC article.
Structure-Guided Design of Partial Agonists at an Opioid Receptor.
Che T, Varga B, Bernhard SM, El Daibani A, Zaidi S, Lam J, Aguilar J, Appourchaux K, Nazarova A, Kouvelis A, Eans S, Margolis E, Fay J, Pradhan A, Katritch V, McLaughlin J, Majumdar S. Che T, et al. Res Sq [Preprint]. 2024 Jul 16:rs.3.rs-4664764. doi: 10.21203/rs.3.rs-4664764/v1. Res Sq. 2024. Update in: Nat Commun. 2025 Mar 13;16(1):2518. doi: 10.1038/s41467-025-57734-5. PMID: 39070616 Free PMC article. Updated. Preprint.
Signaling Modulation Mediated by Ligand Water Interactions with the Sodium Site at μOR.
Ople RS, Ramos-Gonzalez N, Li Q, Sobecks BL, Aydin D, Powers AS, Faouzi A, Polacco BJ, Bernhard SM, Appourchaux K, Sribhashyam S, Eans SO, Tsai BA, Dror RO, Varga BR, Wang H, Hüttenhain R, McLaughlin JP, Majumdar S. Ople RS, et al. ACS Cent Sci. 2024 Jul 17;10(8):1490-1503. doi: 10.1021/acscentsci.4c00525. eCollection 2024 Aug 28. ACS Cent Sci. 2024. PMID: 39220695 Free PMC article.
Advances in the structural understanding of opioid allostery.
Ramos-Gonzalez N, Varga BR, Majumdar S. Ramos-Gonzalez N, et al. Trends Pharmacol Sci. 2025 Feb;46(2):98-101. doi: 10.1016/j.tips.2024.12.007. Epub 2025 Jan 17. Trends Pharmacol Sci. 2025. PMID: 39827063 Free PMC article. Review.
Molecular mechanisms of inverse agonism via κ-opioid receptor-G protein complexes.
Tyson AS, Khan S, Motiwala Z, Han GW, Zhang Z, Ranjbar M, Styrpejko D, Ramos-Gonzalez N, Woo S, Villers K, Landaker D, Kenakin T, Shenvi R, Majumdar S, Gati C. Tyson AS, et al. Nat Chem Biol. 2025 Jul;21(7):1046-1057. doi: 10.1038/s41589-024-01812-0. Epub 2025 Jan 7. Nat Chem Biol. 2025. PMID: 39775170 Free PMC article.