Structure of human cytidine deaminase bound to a potent inhibitor

被引：63

作者：

Chung, SJ

Fromme, JC

Verdine, GL

机构：

[1] Harvard Univ, Dept Chem & Chem Biol, Cambridge, MA 02138 USA

[2] Harvard Univ, Dept Mol & Cellular Biol, Cambridge, MA 02138 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 03期

关键词：

D O I：

10.1021/jm0496279

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Human cytidine deaminase (CDA) is an enzyme prominent for its role in catalyzing metabolic processing of nucleoside-type anticancer and antiviral agents. It is thus a promising target for the development of small molecule therapeutic adjuvants. We report the first crystal structure of human CDA as a complex with a tight-binding inhibitor, diazepinone riboside 1. The structure reveals that inhibitor 1 is able to establish a canonical pi/pi-interaction with a key active site residue, Phe 137.

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页码：658 / 660

页数：3

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