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

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.
AuthorsJinbo Gao, Xiusheng Chu, Yongge Qiu, Long Wu, Yuqin Qiao, Jiasheng Wu, Ding Li
JournalChemical communications (Cambridge, England) (Chem Commun (Camb)) Vol. 46 Issue 29 Pg. 5340-2 (Aug 7 2010) ISSN: 1364-548X [Electronic] England
PMID20544107 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Enzyme Inhibitors
  • Alkyl and Aryl Transferases
  • Mevalonic Acid
  • Alkyl and Aryl Transferases (antagonists & inhibitors)
  • Biocatalysis
  • Enzyme Inhibitors (chemistry, pharmacology)
  • Inhibitory Concentration 50
  • Mevalonic Acid (metabolism)
  • Molecular Structure
  • Structure-Activity Relationship

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