4MHA

Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC1817

4MHA の概要

• エントリーDOI: 10.2210/pdb4mha/pdb
• 関連するPDBエントリー: 2BRB 2POC 3BPR 3TCP 4M3Q 4MH7
• 分子名称: Tyrosine-protein kinase Mer, CHLORIDE ION, 2-(butylamino)-4-[(trans-4-hydroxycyclohexyl)amino]-N-(4-sulfamoylbenzyl)pyrimidine-5-carboxamide, ... (5 entities in total)
• 機能のキーワード: tyrosine kinase, acute lymphoblastic leukemia, rational structure-based drug design, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Membrane ; Single-pass type I membrane protein : Q12866
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 72969.07

構造登録者

Zhang, W.,Mciver, A.,Stashko, M.A.,Deryckere, D.,Branchford, B.R.,Hunter, D.,Kireev, D.B.,Miley, D.B.M.,Norris-Drouin, J.,Stewart, W.M.,Lee, M.,Sather, S.,Zhou, Y.,Dipaola, J.A.,Machius, M.,Janzen, W.P.,Earp, H.S.,Graham, D.K.,Frye, S.,Wang, X. (登録日: 2013-08-29, 公開日: 2014-05-21, 最終更新日: 2023-09-20)

• 主引用文献: Zhang, W.,McIver, A.L.,Stashko, M.A.,DeRyckere, D.,Branchford, B.R.,Hunter, D.,Kireev, D.,Miley, M.J.,Norris-Drouin, J.,Stewart, W.M.,Lee, M.,Sather, S.,Zhou, Y.,Di Paola, J.A.,Machius, M.,Janzen, W.P.,Earp, H.S.,Graham, D.K.,Frye, S.V.,Wang, X.; Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.; J.Med.Chem., 56:9693-9700, 2013; PubMed: 24219778; DOI: 10.1021/jm4013888

実験手法

X-RAY DIFFRACTION (2.59 Å)