Ontology highlight
ABSTRACT:
SUBMITTER: Liu F
PROVIDER: S-EPMC5216742 | biostudies-literature | 2016 Jul
REPOSITORIES: biostudies-literature
Liu Feiyang F Wang Beilei B Wang Qiang Q Qi Ziping Z Chen Cheng C Kong Lu-Lu LL Chen Ji-Yun JY Liu Xiaochuan X Wang Aoli A Hu Chen C Wang Wenchao W Wang Huiping H Wu Fan F Ruan Yanjie Y Qi Shuang S Liu Juan J Zou Fengming F Hu Zhenquan Z Wang Wei W Wang Li L Zhang Shanchun S Yun Cai-Hong CH Zhai Zhimin Z Liu Jing J Liu Qingsong Q
Oncotarget 20160701 29
BCR gene fused ABL kinase is the critical driving force for the Philadelphia Chromosome positive (Ph+) Chronic Myeloid Leukemia (CML) and has been extensively explored as a drug target. With a structure-based drug design approach we have discovered a novel inhibitor CHMFL-074, that potently inhibits both the native and a variety of clinically emerged mutants of BCR-ABL kinase. The X-ray crystal structure of CHMFL-074 in complex with ABL1 kinase (PDB ID: 5HU9) revealed a typical type II binding m ...[more]