Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

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

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28 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)12062-12064
Number of pages3
JournalChemical Communications
Volume47
Issue number44
DOIs
Publication statusPublished - 2011

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