7KHK

Crystal structure of KIT kinase domain with a small molecule inhibitor, PLX9486 (bezuclastinib) in the DFG-in state

7KHK の概要

• エントリーDOI: 10.2210/pdb7khk/pdb
• 関連するPDBエントリー: 7KHG 7KHJ
• 分子名称: Mast/stem cell growth factor receptor Kit, 4,5-dimethyl-N-(2-phenyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazole-3-carboxamide (3 entities in total)
• 機能のキーワード: transferase, tyrosine-protein kinase, atp-binding, kinase-kinase inhibitor complex, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 76630.87

構造登録者

Zhang, Y. (登録日: 2020-10-21, 公開日: 2021-07-07, 最終更新日: 2023-10-18)

• 主引用文献: Wagner, A.J.,Severson, P.L.,Shields, A.F.,Patnaik, A.,Chugh, R.,Tinoco, G.,Wu, G.,Nespi, M.,Lin, J.,Zhang, Y.,Ewing, T.,Habets, G.,Burton, E.A.,Matusow, B.,Tsai, J.,Tsang, G.,Shellooe, R.,Carias, H.,Chan, K.,Rezaei, H.,Sanftner, L.,Marimuthu, A.,Spevak, W.,Ibrahim, P.N.,Inokuchi, K.,Alcantar, O.,Michelson, G.,Tsiatis, A.C.,Zhang, C.,Bollag, G.,Trent, J.C.,Tap, W.D.; Association of Combination of Conformation-Specific KIT Inhibitors With Clinical Benefit in Patients With Refractory Gastrointestinal Stromal Tumors: A Phase 1b/2a Nonrandomized Clinical Trial.; Jama Oncol, 7:1343-1350, 2021; PubMed: 34236401; DOI: 10.1001/jamaoncol.2021.2086

実験手法

X-RAY DIFFRACTION (2.34 Å)