8X6R

KRasG12C in complex with inhibitor

8X6R の概要

• エントリーDOI: 10.2210/pdb8x6r/pdb
• 分子名称: Isoform 2B of GTPase KRas, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... (5 entities in total)
• 機能のキーワード: gtp-binding, hydrolase-inhibitor complex, hydrolase/inhibitor
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 6
• 化学式量合計: 122700.78

構造登録者

Amano, Y.,Tateishi, Y. (登録日: 2023-11-21, 公開日: 2024-01-17)

• 主引用文献: Imaizumi, T.,Shimada, I.,Satake, Y.,Yamaki, S.,Koike, T.,Nigawara, T.,Kaneko, O.,Amano, Y.,Mori, K.,Yamanaka, Y.,Nakayama, A.,Nishizono, Y.,Shimazaki, M.,Nagashima, T.,Kuramoto, K.; Discovery of ASP6918, a KRAS G12C inhibitor: Synthesis and structure-activity relationships of 1-{2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one derivatives as covalent inhibitors with good potency and oral activity for the treatment of solid tumors.; Bioorg.Med.Chem., 98:117581-117581, 2023; PubMed: 38176113; DOI: 10.1016/j.bmc.2023.117581

実験手法

X-RAY DIFFRACTION (1.85 Å)