Development of selective RabGGTase inhibitors and crystal structure of a RabGGTase-inhibitor complex

被引：14

作者：

Guo, Zhong ^{[1
]}

Wu, Yao-Wen ^{[1
]}

Tan, Kui-Thong ^{[2
,3
]}

Bon, Robin S. ^{[2
,3
]}

Guiu-Rozas, Ester ^{[2
,3
]}

Delon, Christine ^{[1
]}

Nguyen, Uyen T. ^{[1
]}

Wetzel, Stefan ^{[2
,3
]}

Arndt, Sabine ^{[2
,3
]}

Goody, Roger S. ^{[1
]}

Blankenfeldt, Wulf ^{[1
]}

Alexandrov, Kirill ^{[1
]}

Waldmann, Herbert ^{[2
,3
]}

机构：

[1] Max Planck Inst Mol Physiol, Phys Biochem Abt, D-44227 Dortmund, Germany

[2] Max Planck Inst Mol Physiol, Abt Chem Biol, D-44227 Dortmund, Germany

[3] TU Dortmund, Fachbereich Chem, D-44227 Dortmund, Germany

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2008年 / 47卷 / 20期

关键词：

inhibitors; prenylation; protein modifications; protein structures; transferases;

D O I：

10.1002/anie.200705795

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Stopping the transfer: Based on the structure of pepticinnamin E, specific inhibitors of Rab geranylgeranyl transferase (RabGGTase) with activity in cells were developed, and the first crystal structure of the enzyme in complex with an inhibitor is reported (see inhibitor structure and positioning in the active site of the enzyme). The findings may have implications for the chemical-biological study of Rab prenylation and vesicular transport and the involvement of RabGGTase in the establishment of disease. (Chemical Equation Presented) © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：3747 / 3750

页数：4

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