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

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.

SUBMITTER: Nishida CR 

PROVIDER: S-EPMC2730118 | biostudies-literature | 2008 Aug

REPOSITORIES: biostudies-literature