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 |
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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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| 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... |
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| Date Deposited: 09 Aug 2023 13:04 |
| Last Modified: 09 Aug 2023 13:04 |
| Author: |
Matthew Smith
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| Author: | A. J. Carnell |
| Author: | R. Kirk |
| Author: | S. McKenna |
| Author: | L-Y. Lian |
| Author: | R. Gibson |
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