A novel colorimetric assay for α-methylacyl-CoA racemase 1A (AMACR; P504S) utilizing the elimination of 2,4-dinitrophenolate

Chem Commun (Camb). 2017 May 4;53(37):5087-5090. doi: 10.1039/c7cc00476a.

Abstract

α-Methylacyl-CoA racemase (AMACR; P504S) regulates branched-chain fatty acid degradation, activates Ibuprofen and is a recognised cancer drug target. A novel, facile colorimetric assay was developed based on elimination of 2,4-dinitrophenolate. The assay was used to test 5 known inhibitors, determining IC50 and Ki values, reversibility and characterizing irreversible inhibition.

MeSH terms

  • Colorimetry / methods*
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Hydroxybenzoates / chemistry*
  • Molecular Structure
  • Nitro Compounds / chemistry*
  • Racemases and Epimerases / analysis*
  • Racemases and Epimerases / antagonists & inhibitors
  • Racemases and Epimerases / metabolism
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Hydroxybenzoates
  • Nitro Compounds
  • Racemases and Epimerases
  • alpha-methylacyl-CoA racemase
  • phenolic acid