Crystal structure of KRAS G12A in a transition state mimetic complex with CYPA and RMC-7977

Crystal structure of KRAS G12A in a transition state mimetic complex with CYPA and RMC-7977 Descriptor: (1R,5S,6r)-N-[(1P,7S,9S,13S,20M)-20-{5-(4-cyclopropylpiperazin-1-yl)-2-[(1S)-1-methoxyethyl]pyridin-3-yl}-21-ethyl-17,17-dimethyl-8,14-dioxo-15-oxa-4-thia-9,21,27,28-tetraazapentacyclo[17.5.2.1~2,5~.1~9,13~.0~22,26~]octacosa-1(24),2,5(28),19,22,25-hexaen-7-yl]-3-oxabicyclo[3.1.0]hexane-6-carboxamide, ALUMINUM FLUORIDE, GUANOSINE-5'-DIPHOSPHATE, ... Authors: Pourfarjam, Y, Goldgur, Y, Cuevas-Navarro, A, Lito, P. Deposit date: 2024-04-21 Release date: 2024-11-06 Last modified: 2026-08-12 Method: X-RAY DIFFRACTION (1.9 Å) Cite: Pharmacological restoration of GTP hydrolysis by mutant RAS. Nature, 637, 2025KRAS G12A与亲环素A（CYPA）及RMC-7977形成的过渡态模拟复合物的晶体结构 描述物：(1R,5S,6r)-N-[(1P,7S,9S,13S,20M)-20-{5-(4-环丙基哌嗪-1-基)-2-[(1S)-1-甲氧基乙基]吡啶-3-基}-21-乙基-17,17-二甲基-8,14-二氧代-15-氧杂-4-硫杂-9,21,27,28-四氮杂五环[17.5.2.1~2,5~.1~9,13~.0~22,26~]二十八碳-1(24),2,5(28),19,22,25-六烯-7-基]-3-氧杂双环[3.1.0]己烷-6-甲酰胺、氟化铝、鸟苷-5'-二磷酸等 作者：普尔加法姆, Y、戈德古尔, Y、奎瓦斯-纳瓦罗, A、利托, P 入库日期：2024-04-21 发布日期：2024-11-06 最后修改日期：2025-01-29 实验方法：X射线衍射（分辨率1.9 Å） 引用文献：《突变型RAS的GTP水解药理学恢复》，《自然》，637卷，2025年