Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative

被引：35

作者：

Kinoshita, T

Warizaya, M

Ohori, M

Sato, K

Neya, M

Fujii, T

机构：

[1] Fujisawa Pharmaceut Co Ltd, Exploratory Res Labs, Tsukuba, Ibaraki 3002698, Japan

[2] Fujisawa Pharmaceut Co Ltd, Med Chem Res Labs, Tsukuba, Ibaraki 3002698, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 01期

关键词：

ERK2; X-ray; structural change;

D O I：

10.1016/j.bmcl.2005.09.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyrazolopyridazine compounds were briefly investigated as ERK2 inhibitors. The crystal structure of ERK2 complexed with an allyl derivative was determined. The compound induces structural change including movement of the glycine-rich loop and peptide flip between Met108-Glu109. As a result, the newly formed subsite can recognize small hydrophobic substituents but not hydrophilie ones. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：55 / 58

页数：4

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