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

Maksims Yevglevskis; Guat L Lee; Amit Nathubhai; Yoana D Petrova; Tony D James; Michael D Threadgill; Timothy J Woodman; Matthew D Lloyd

doi:10.1039/c7cc00476a

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

Maksims Yevglevskis
, Guat L Lee
, Amit Nathubhai
, Yoana D Petrova
, Tony D James
, Michael D Threadgill
, Timothy J Woodman
, Matthew D Lloyd

Science

Research output: Contribution to Journal › Article › peer-review

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.

Original language	English
Pages (from-to)	5087-5090
Number of pages	4
Journal	ChemComm
Volume	53
Issue number	37
DOIs	https://doi.org/10.1039/c7cc00476a
Publication status	Published - 4 May 2017

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Colorimetry/methods
Dose-Response Relationship, Drug
Enzyme Inhibitors/chemical synthesis
Humans
Hydroxybenzoates/chemistry
Molecular Structure
Nitro Compounds/chemistry
Racemases and Epimerases/analysis
Structure-Activity Relationship

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10.1039/c7cc00476aLicence: CC BY

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

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.",

keywords = "Colorimetry/methods, Dose-Response Relationship, Drug, Enzyme Inhibitors/chemical synthesis, Humans, Hydroxybenzoates/chemistry, Molecular Structure, Nitro Compounds/chemistry, Racemases and Epimerases/analysis, Structure-Activity Relationship",

author = "Maksims Yevglevskis and Lee, \{Guat L\} and Amit Nathubhai and Petrova, \{Yoana D\} and James, \{Tony D\} and Threadgill, \{Michael D\} and Woodman, \{Timothy J\} and Lloyd, \{Matthew D\}",

year = "2017",

month = may,

day = "4",

doi = "10.1039/c7cc00476a",

language = "English",

volume = "53",

pages = "5087--5090",

journal = "ChemComm",

issn = "1364-548X",

publisher = "Royal Society of Chemistry",

number = "37",

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T1 - A novel colorimetric assay for α-methylacyl-CoA racemase 1A (AMACR; P504S) utilizing the elimination of 2,4-dinitrophenolate

AU - Yevglevskis, Maksims

AU - Lee, Guat L

AU - Nathubhai, Amit

AU - Petrova, Yoana D

AU - James, Tony D

AU - Threadgill, Michael D

AU - Woodman, Timothy J

AU - Lloyd, Matthew D

PY - 2017/5/4

Y1 - 2017/5/4

N2 - 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.

AB - 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.

KW - Colorimetry/methods

KW - Dose-Response Relationship, Drug

KW - Enzyme Inhibitors/chemical synthesis

KW - Humans

KW - Hydroxybenzoates/chemistry

KW - Molecular Structure

KW - Nitro Compounds/chemistry

KW - Racemases and Epimerases/analysis

KW - Structure-Activity Relationship

U2 - 10.1039/c7cc00476a

DO - 10.1039/c7cc00476a

M3 - Article

C2 - 28338138

SN - 1364-548X

VL - 53

SP - 5087

EP - 5090

JO - ChemComm

JF - ChemComm

IS - 37

ER -

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

Abstract

UN SDGs

Keywords

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