Inactivation of thiolase by 2-alkynoyl-CoA via its intrinsic isomerase activity

Org Lett. 2007 Sep 27;9(20):3877-80. doi: 10.1021/ol0712677. Epub 2007 Sep 1.

Abstract

Selective inactivation of cytosolic thiolase by 2-alkynoyl-CoA via its intrinsic isomerase activity was studied, which provides an example for rationally developing mechanism-based inhibitors based on a side activity of the enzyme, and may become a supplemental method for better treatment of cardiovascular disease and cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetyl Coenzyme A / chemistry*
  • Acetyl Coenzyme A / metabolism*
  • Amino Acids / chemistry
  • Amino Acids / metabolism
  • Animals
  • Catalysis
  • Cell Line
  • Enzyme Activation
  • Isomerism
  • Kinetics
  • Liver / enzymology
  • Molecular Structure
  • Peptide Fragments / chemistry
  • Peptide Fragments / metabolism
  • Rats
  • Substrate Specificity
  • Sulfhydryl Compounds / metabolism*
  • Tandem Mass Spectrometry

Substances

  • Amino Acids
  • Peptide Fragments
  • Sulfhydryl Compounds
  • Acetyl Coenzyme A