Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

Pors, Klaus; Loadman, Paul; Shnyder, Steven D.; Sutherland, Mark H.; Sheldrake, Helen M.; Guino, M.; Kiakos, K.; Hartley, J.A.; Searcey, M.; Patterson, Laurence H.

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.

URI

http://hdl.handle.net/10454/6138

Citation

Pors K, Loadman PM, Shnyder SD et al (2011) Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity. Chemical Communications 47(44): 12062-12064.

Link to publisher’s version

http://dx.doi.org/10.1039/c1cc15638a

Type

Article

Collections

Life Sciences Publications