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, determin...

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Veröffentlicht in:	Chemical communications (Cambridge, England) England), 2017-05, Vol.53 (37), p.5087-5090
Hauptverfasser:	Yevglevskis, Maksims, Lee, Guat L, Nathubhai, Amit, Petrova, Yoana D, James, Tony D, Threadgill, Michael D, Woodman, Timothy J, Lloyd, Matthew D
Format:	Artikel
Sprache:	eng
Schlagworte:	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
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Beschreibung
Zusammenfassung:	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 IC and K values, reversibility and characterizing irreversible inhibition.
ISSN:	1359-7345 1364-548X
DOI:	10.1039/c7cc00476a