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
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Colorimetry / methods*
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Humans
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Hydroxybenzoates / chemistry*
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Molecular Structure
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Nitro Compounds / chemistry*
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Racemases and Epimerases / analysis*
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Racemases and Epimerases / antagonists & inhibitors
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Racemases and Epimerases / metabolism
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Hydroxybenzoates
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Nitro Compounds
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Racemases and Epimerases
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alpha-methylacyl-CoA racemase
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phenolic acid