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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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Publication details

The article was received on 12 Sep 2011, accepted on 04 Oct 2011 and first published on 14 Oct 2011


Article type: Communication
DOI: 10.1039/C1CC15638A
Citation: Chem. Commun., 2011,47, 12062-12064
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    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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