Mutation and inhibition studies of mevalonate 5-diphosphate decarboxylase

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6164-8. doi: 10.1016/j.bmcl.2007.09.033. Epub 2007 Sep 11.

Abstract

Mevalonate 5-diphosphate decarboxylase plays an important role in regulating cholesterol biosynthesis, which was studied through incubation with various synthetic substrate analogs and characterization of mutated enzymes. The results are potentially useful for further developing inhibitors that block the mevalonate pathway which is a drug target for treating cardiovascular disease and cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carboxy-Lyases / antagonists & inhibitors*
  • Carboxy-Lyases / chemistry*
  • Carboxy-Lyases / genetics
  • Cholesterol / metabolism
  • Drug Evaluation, Preclinical
  • Inhibitory Concentration 50
  • Kinetics
  • Liver / enzymology
  • Molecular Structure
  • Mutagenesis, Site-Directed
  • Rats
  • Signal Transduction / drug effects
  • Structure-Activity Relationship
  • Substrate Specificity / genetics
  • Yeasts / enzymology

Substances

  • Cholesterol
  • Carboxy-Lyases
  • pyrophosphomevalonate decarboxylase