Issue 29, 2010
From the journal:

Chemical Communications

Discovery of potent inhibitor for farnesyl pyrophosphate synthase in the mevalonate pathway†

Jinbo Gao,a   Xiusheng Chu,a   Yongge Qiu,a   Long Wu,a   Yuqin Qiao,a   Jiasheng Wua  and  Ding Li*b  

* Corresponding authors

a Department of Biology and Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Kowloon, Hong Kong, P. R. China

b School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou University City, Waihuan East Road 132, Guangzhou 510006, P. R. China
E-mail: liding@mail.sysu.edu.cn
Tel: +86 20 3994 3058

Abstract

The mevalonate pathway is an important drug target for the treatment of cancer and cardiovascular disease. We synthesized and studied a new type of nitrogen-containing bisphosphonate analogs and developed a sensitive end point assay method for enzyme FPPS, which was used for inhibitor screening. One potent FPPS inhibitor was discovered, and the structure–activity relationship of bisphosphonates for the enzyme inactivation was studied.

Graphical abstract: Discovery of potent inhibitor for farnesyl pyrophosphate synthase in the mevalonate pathway

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Article information

DOI
https://doi.org/10.1039/C0CC00992J
Article type
Communication
Submitted
17 Apr 2010
Accepted
20 May 2010
First published
14 Jun 2010

Chem. Commun., 2010,46, 5340-5342

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Discovery of potent inhibitor for farnesyl pyrophosphate synthase in the mevalonate pathway

J. Gao, X. Chu, Y. Qiu, L. Wu, Y. Qiao, J. Wu and D. Li, Chem. Commun., 2010, 46, 5340 DOI: 10.1039/C0CC00992J

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