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

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.

• Authors: Jinbo Gao, Xiusheng Chu, Yongge Qiu, Long Wu, Yuqin Qiao, Jiasheng Wu, Ding Li
• Journal: Chemical communications (Cambridge, England) (Chem Commun (Camb)) Vol. 46 Issue 29 Pg. 5340-2 (Aug 07 2010) ISSN: 1364-548X [Electronic] England
• PMID: 20544107 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Enzyme Inhibitors
• Alkyl and Aryl Transferases
• Mevalonic Acid

Topics

• Alkyl and Aryl Transferases (antagonists & inhibitors)
• Biocatalysis
• Enzyme Inhibitors (chemistry, pharmacology)
• Inhibitory Concentration 50
• Mevalonic Acid (metabolism)
• Molecular Structure
• Structure-Activity Relationship