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

doi:10.1039/C1CC15638A

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 Searcey^b and Laurence H. Patterson*^a

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* 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.

Chemical Communications

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

Abstract

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Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

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