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The structure, function, and pharmacology of MRGPRs.
Cao C, Roth BL. Cao C, et al. Trends Pharmacol Sci. 2023 Apr;44(4):237-251. doi: 10.1016/j.tips.2023.02.002. Epub 2023 Mar 2. Trends Pharmacol Sci. 2023. PMID: 36870785 Free PMC article. Review.
Structure, function and pharmacology of human itch GPCRs.
Cao C, Kang HJ, Singh I, Chen H, Zhang C, Ye W, Hayes BW, Liu J, Gumpper RH, Bender BJ, Slocum ST, Krumm BE, Lansu K, McCorvy JD, Kroeze WK, English JG, DiBerto JF, Olsen RHJ, Huang XP, Zhang S, Liu Y, Kim K, Karpiak J, Jan LY, Abraham SN, Jin J, Shoichet BK, Fay JF, Roth BL. Cao C, et al. Nature. 2021 Dec;600(7887):170-175. doi: 10.1038/s41586-021-04126-6. Epub 2021 Nov 17. Nature. 2021. PMID: 34789874 Free PMC article.
AlphaFold2 structures guide prospective ligand discovery.
Lyu J, Kapolka N, Gumpper R, Alon A, Wang L, Jain MK, Barros-Álvarez X, Sakamoto K, Kim Y, DiBerto J, Kim K, Glenn IS, Tummino TA, Huang S, Irwin JJ, Tarkhanova OO, Moroz Y, Skiniotis G, Kruse AC, Shoichet BK, Roth BL. Lyu J, et al. Science. 2024 Jun 21;384(6702):eadn6354. doi: 10.1126/science.adn6354. Epub 2024 Jun 21. Science. 2024. PMID: 38753765
Structure-based design of bitopic ligands for the µ-opioid receptor.
Faouzi A, Wang H, Zaidi SA, DiBerto JF, Che T, Qu Q, Robertson MJ, Madasu MK, El Daibani A, Varga BR, Zhang T, Ruiz C, Liu S, Xu J, Appourchaux K, Slocum ST, Eans SO, Cameron MD, Al-Hasani R, Pan YX, Roth BL, McLaughlin JP, Skiniotis G, Katritch V, Kobilka BK, Majumdar S. Faouzi A, et al. Nature. 2023 Jan;613(7945):767-774. doi: 10.1038/s41586-022-05588-y. Epub 2022 Nov 30. Nature. 2023. PMID: 36450356 Free PMC article.
A neurodevelopmental disorder mutation locks G proteins in the transitory pre-activated state.
Knight KM, Krumm BE, Kapolka NJ, Ludlam WG, Cui M, Mani S, Prytkova I, Obarow EG, Lefevre TJ, Wei W, Ma N, Huang XP, Fay JF, Vaidehi N, Smrcka AV, Slesinger PA, Logothetis DE, Martemyanov KA, Roth BL, Dohlman HG. Knight KM, et al. Nat Commun. 2024 Aug 5;15(1):6643. doi: 10.1038/s41467-024-50964-z. Nat Commun. 2024. PMID: 39103320 Free PMC article.