Structure-based design of novel calcineurin (PP2B) inhibitors

被引：38

作者：

Tatlock, JH

Linton, MA

Hou, XJ

Kissinger, CR

Pelletier, LA

Showalter, RE

Tempczyk, A

Villafranca, JE

机构：

[1] Agouron Pharmaceuticals Inc., 3565 General Atomics Court, San Diego

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(97)00141-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design, synthesis, and evaluation of small molecule, in vitro, inhibitors of human calcineurin is described. These ligands were derived from the known nonspecific phosphatase inhibitor endothall, and were modified to enhance binding and selectivity toward calcineurin using protein crystal structure information. (C) 1997 Elsevier Science Ltd.

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页码：1007 / 1012

页数：6

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