Inhibition of Human [alpha]-Methylacyl CoA Racemase (AMACR): a Target for Prostate Cancer
The enzyme [alpha]-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 ration...
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| Veröffentlicht in: | ChemMedChem 2013-10, Vol.8 (10), p.1643 |
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| creator | Carnell, Andrew J Kirk, Ralph Smith, Matthew McKenna, Shane Lian, Lu-Yun Gibson, Robert |
| description | The enzyme [alpha]-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=98nM), designed to mimic the proposed enzyme-bound enolate, was found to be the most potent AMACR inhibitor reported to date. [PUBLICATION ABSTRACT] |
| doi_str_mv | 10.1002/cmdc.201300179 |
| format | Article |
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| source | Wiley Online Library Journals Frontfile Complete |
| subjects | Enzymes Medical research Prostate cancer |
| title | Inhibition of Human [alpha]-Methylacyl CoA Racemase (AMACR): a Target for Prostate Cancer |
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