Long Dissociation of Bictegravir from HIV-1 Integrase-DNA Complexes

作者：Kirsten White, Nathan Osman, Ernesto Cuadra-Foy, Bluma Brenner, Devleena Shivakumar, Federico Campigotto, Manuel Tsiang, Philip Morganelli, Nikolai Novikov, Scott E. Lazerwith, Haolun Jin, Anita Niedziela‐Majka · 发表于：Antimicrobial Agents and Chemotherapy · 年份：2021 · DOI：10.1128/aac.02406-20 · 被引用次数：33 · 研究领域：HIV/AIDS drug development and treatment、Biochemical and Molecular Research、HIV Research and Treatment

and maintained longer antiviral activity after drug washout than DTG with the clinically relevant resistance IN mutant G140S+Q148H. Structural analyses indicate that BIC makes more contacts with the IN-DNA complex than DTG mainly via its bicyclic ring system which may contribute to more prolonged residence time and resilience against many resistance mutations.