Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity
Publication date
2011Author
Pors, KlausLoadman, Paul
Shnyder, Steven
Sutherland, Mark
Sheldrake, Helen M.
Guino, M.
Kiakos, K.
Hartley, J.A.
Searcey, M.
Patterson, Laurence H.
Keyword
Alkylating agentsAnimals
Biotransformation
CHO cells
Cricetinae
Cricetulus
Cytochrome P-450 CYP1A1
Cytotoxins
Humans
Indoles
Molecular targeted therapy
Oxidation-reduction
REF 2014
Metadata
Show full item recordAbstract
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.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 Version of Record
https://doi.org/10.1039/c1cc15638aType
Articleae974a485f413a2113503eed53cd6c53
https://doi.org/10.1039/c1cc15638a