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Inhibition of Humana-Methylacyl CoA Racemase(AMACR): a Target for Prostate Cancer

Carnell, A. J., Kirk, R., Smith, Matthew, McKenna, S., Lian, L-Y. and Gibson, R. (2013) Inhibition of Humana-Methylacyl CoA Racemase(AMACR): a Target for Prostate Cancer. ChemMedChem, 8. pp. 1643-1647. ISSN 1860-7179

Item Type: Article

Abstract

The enzyme α-methylacyl CoA racemase (AMACR) is involved in the metabolism of branched-chain fatty acids and has been identified as a promising therapeutic target for prostate cancer. By using the recently available human AMACR from HEK293 kidney cell cultures, we tested a series of new rationally designed inhibitors to determine the structural requirements in the acyl component. An N-methylthiocarbamate (Ki=98 nM), designed to mimic the proposed enzyme-bound enolate, was found to be the most potent AMACR inhibitor reported to date.

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More Information

Depositing User: Matt Smith

Identifiers

Item ID: 16335
Identification Number: https://doi.org/10.1002/cmdc.201300179
ISSN: 1860-7179
URI: http://sure.sunderland.ac.uk/id/eprint/16335
Official URL: https://chemistry-europe.onlinelibrary.wiley.com/d...

Users with ORCIDS

ORCID for Matthew Smith: ORCID iD orcid.org/0000-0003-1903-7607

Catalogue record

Date Deposited: 09 Aug 2023 13:04
Last Modified: 09 Aug 2023 13:04

Contributors

Author: Matthew Smith ORCID iD
Author: A. J. Carnell
Author: R. Kirk
Author: S. McKenna
Author: L-Y. Lian
Author: R. Gibson

University Divisions

Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences

Subjects

Sciences > Chemistry

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