HIV-1 Integrase Catalytic Core Domain Mutant (KGD) in Complex with Inhibitor GRL-142

HIV-1 Integrase Catalytic Core Domain Mutant (KGD) in Complex with Inhibitor GRL-142 Descriptor: (3S,3aR,5R,7aS,8S)-hexahydro-4H-3,5-methanofuro[2,3-b]pyran-8-yl [(2S,3R)-4-[{[2-(cyclopropylamino)-1,3-benzothiazol-6-yl]sulfonyl}(2-methylpropyl)amino]-1-(3,5-difluorophenyl)-3-hydroxybutan-2-yl]carbamate, Integrase, SULFATE ION Authors: Aoki, M, Aoki-Ogata, H, Bulut, H, Hayashi, H, Davis, D, Hasegawa, K, Yarchoan, R, Ghosh, A.K, Pau, A.K, Mitsuya, H. Deposit date: 2022-03-21 Release date: 2023-03-22 Last modified: 2024-04-24 Method: X-RAY DIFFRACTION (3 Å) Cite: GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants. Sci Adv, 9, 2023

与抑制剂GRL-142结合的HIV-1整合酶催化核心结构域突变体（KGD） 描述物：(3S,3aR,5R,7aS,8S)-六氢-4H-3,5-亚甲基呋喃并[2,3-b]吡喃-8-基 [(2S,3R)-4-[{[2-(环丙基氨基)-1,3-苯并噻唑-6-基]磺酰}(2-甲基丙基)氨基]-1-(3,5-二氟苯基)-3-羟基丁-2-基]氨基甲酸酯、整合酶、硫酸根离子 作者：Aoki, M、Aoki-Ogata, H、Bulut, H、Hayashi, H、Davis, D、Hasegawa, K、Yarchoan, R、Ghosh, A.K、Pau, A.K、Mitsuya, H 存放日期：2022-03-21 发布日期：2023-03-22 最后修改日期：2024-04-24 实验方法：X射线衍射（3 Å） 引用文献：GRL-142可结合并破坏HIV-1整合酶核定位信号，强效抑制对整合酶链转移抑制剂（INSTI）高度耐药的HIV-1变异株。《Science Advances》，9卷，2023年