8X6R

KRasG12C in complex with inhibitor

Summary for 8X6R

• Entry DOI: 10.2210/pdb8x6r/pdb
• Descriptor: Isoform 2B of GTPase KRas, GUANOSINE-5'-DIPHOSPHATE, MAGNESIUM ION, ... (5 entities in total)
• Functional Keywords: gtp-binding, hydrolase-inhibitor complex, hydrolase/inhibitor
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 6
• Total formula weight: 122700.78

Authors

Amano, Y.,Tateishi, Y. (deposition date: 2023-11-21, release date: 2024-01-17)

• Primary citation: 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

Experimental method

X-RAY DIFFRACTION (1.85 Å)