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Issue 44, 2011
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Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

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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.

Graphical abstract: Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

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Supplementary files

Article information


Submitted
12 Sep 2011
Accepted
04 Oct 2011
First published
14 Oct 2011

Chem. Commun., 2011,47, 12062-12064
Article type
Communication

Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

K. Pors, P. M. Loadman, S. D. Shnyder, M. Sutherland, H. M. Sheldrake, M. Guino, K. Kiakos, J. A. Hartley, M. Searcey and L. H. Patterson, Chem. Commun., 2011, 47, 12062
DOI: 10.1039/C1CC15638A

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