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

Chem Commun (Camb). 2010 Aug 7;46(29):5340-2. doi: 10.1039/c0cc00992j. Epub 2010 Jun 14.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

  • Enzyme Inhibitors
  • Alkyl and Aryl Transferases
  • Mevalonic Acid