A novel colorimetric assay for α-methylacyl-CoA racemase 1A (AMACR; P504S) utilizing the elimination of 2,4-dinitrophenolate.
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 IC50and Kivalues, reversibility and characterizing irreversible inhibition.
Drug & Target Development, Department of Pharmacy & Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK. M.D.Lloyd@bath.ac.uk.
Maksims
M
Yevglevskis
Guat L
GL
Lee
Amit
A
Nathubhai
Yoana D
YD
Petrova
Tony D
TD
James
Michael D
MD
Threadgill
Timothy J
TJ
Woodman
Matthew D
MD
Lloyd
D003124:Colorimetry / Q000379:methods*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D062385:Hydroxybenzoates / Q000737:chemistry*; D015394:Molecular Structure; D009574:Nitro Compounds / Q000737:chemistry*; D019998:Racemases and Epimerases / Q000032:analysis* / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D062385:Hydroxybenzoates; D009574:Nitro Compounds; D019998:Racemases and Epimerases; C108352:alpha-methylacyl-CoA racemase; C017616:phenolic acid