Structural basis for the inhibitor recognition of human Lyn kinase domain

被引：10
作者：
Miyano, Nao [1 ]
Kinoshita, Takayoshi [1 ]
Nakai, Ryoko [2 ]
Kirii, Yasuyuki [2 ]
Yokota, Koichi [2 ]
Tada, Toshiji [1 ]
机构：
[1] Osaka Prefecture Univ, Grad Sch Sci, Naka Ku, Osaka 5998531, Japan
[2] Carna Biosci Inc, BMA, Chuo Ku, Kobe, Hyogo 6500047, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 23期
关键词：
Lyn; Src family; Kinase; Structure; Inhibitor; SRC-FAMILY KINASES; CRYSTAL-STRUCTURES; ACTIVATION; COMPLEX; DESIGN; TARGET; CANCER; MICE; ABL;
D O I：
10.1016/j.bmcl.2009.10.038
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Human Lyn tyrosine kinase is expressed in hematopoietic tissues and plays crucial roles in the signal transduction of hematopoietic immune system. Its excess activity is involved in several tumors. The crystal structure has revealed that the potent inhibitor staurosporine binds to human Lyn kinase domain at the ATP-binding site. The remarkable structural features of the staurosporine-binding region will offer valuable structural insights for the structure-based design of novel Lyn-selective inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6557 / 6560
页数：4
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