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Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

; ; ; ; 
Sheldrake, Helen M.
; 
Guino, M.
; 
Kiakos, K.
; 
Hartley, J.A.
; 
Searcey, M.
; 
Patterson, Laurence H.
Publication Date
2011
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Keywords
Alkylating agents, Animals, Biotransformation, CHO cells, Cricetinae, Cricetulus, Cytochrome P-450 CYP1A1, Cytotoxins, Humans, Indoles, Molecular targeted therapy, Oxidation-reduction, REF 2014
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Peer-Reviewed
Yes
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closedAccess
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Life Sciences Publications
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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
https://bradscholars.brad.ac.uk/handle/10454/6138.2
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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.
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https://doi.org/10.1039/c1cc15638a
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Article
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