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. 2011 Nov 28;47(44):12062-4.
doi: 10.1039/c1cc15638a. Epub 2011 Oct 14.

Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

Klaus Pors  1 , Paul M Loadman, Steven D Shnyder, Mark Sutherland, Helen M Sheldrake, Meritxell Guino, Konstantinos Kiakos, John A Hartley, Mark Searcey, Laurence H Patterson
Affiliations

Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

Klaus Pors et al. Chem Commun (Camb). .

Abstract

The identification of an agent that is selectively activated by a cytochrome P450 (CYP) has the potential for tissue specific dose intensification as a means of significantly improving its therapeutic value. Towards this goal, we disclose evidence for the pathway of activation of a duocarmycin analogue, ICT2700, which targets CYP1A1 for biological activity.

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