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.
Cryo-electron microscopy structures of the most potent bitopic ligands in complex with OR highlight the key interactions between the guanidine of the ligands and the key Asp(2.50) residue in the Na(+) site. Two bitopics (C5 and C6 guano) maintain nanomolar potency and high …
Cryo-electron microscopy structures of the most potent bitopic ligands in complex with OR highlight the key interactions between the guanidi …