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J Med Chem. 2008 Aug 28;51(16):5118-20. doi: 10.1021/jm800496s. Epub 2008 Aug 6.

Reductive heme-dependent activation of the n-oxide prodrug AQ4N by nitric oxide synthase.

Author information

1
Department of Pharmaceutical Chemistry, University of California, 600 16th Street, San Francisco, California 94158-2517, USA.

Abstract

Anaerobic reduction of anticancer prodrugs is a promising route to achieve targeting and selectivity in anticancer drug design. Most reductive prodrug activations involve simple electron transfer from a flavoprotein and are not amenable to specific targeting. Here, we report that the N-oxide AQ4N is reduced by a nitric oxide synthase. This reduction involves interaction with the heme iron atom in the active site and is thus subject to specific protein constraints.

PMID:
18681417
PMCID:
PMC2730118
DOI:
10.1021/jm800496s
[Indexed for MEDLINE]
Free PMC Article

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