Issue 44, 2011
From the journal:

Chemical Communications

Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity†

Klaus Pors,a   Paul M. Loadman,a   Steven D. Shnyder,a   Mark Sutherland,a   Helen M. Sheldrake,a   Meritxell Guino,b   Konstantinos Kiakos,c   John A. Hartley,c   Mark Searceyb  and  Laurence H. Patterson*a  

* Corresponding authors

a Institute of Cancer Therapeutics, University of Bradford, West Yorkshire BD7 1DP, UK
E-mail: L.H.Patterson@Bradford.ac.uk

b Cancer Research UK Drug-DNA Interactions Research Group, UCL Cancer Institute, London, UK

c School of Pharmacy, University of East Anglia, Norwich, Norfolk NR4 7TJ, UK

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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Article information

DOI
https://doi.org/10.1039/C1CC15638A
Article type
Communication
Submitted
12 Sep 2011
Accepted
04 Oct 2011
First published
14 Oct 2011

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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