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
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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Date Deposited: 09 Aug 2023 13:04 |
Last Modified: 04 Jun 2025 16:06 |