Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

Description

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.

Links & Downloads

1. 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.
2. http://hdl.handle.net/10454/6138
3. https://doi.org/10.1039/c1cc15638a

Tags

Alkylating agents

Animals

Biotransformation

CHO cells

Cricetinae

Cricetulus

Cytochrome P-450 CYP1A1

Cytotoxins

Humans

Indoles

Molecular targeted therapy

Oxidation-reduction

REF 2014

Additional Fields

Identifer	oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/6138
Date	January 2011
Creators	Pors, Klaus, Loadman, Paul, Shnyder, Steven, Sutherland, Mark, Sheldrake, Helen M., Guino, M., Kiakos, K., Hartley, J.A., Searcey, M., Patterson, Laurence H.
Source Sets	Bradford Scholars
Detected Language	English
Type	Article