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Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

dc.contributor.authorPors, Klaus*
dc.contributor.authorLoadman, Paul*
dc.contributor.authorShnyder, Steven*
dc.contributor.authorSutherland, Mark*
dc.contributor.authorSheldrake, Helen M.*
dc.contributor.authorGuino, M.*
dc.contributor.authorKiakos, K.*
dc.contributor.authorHartley, J.A.*
dc.contributor.authorSearcey, M.*
dc.contributor.authorPatterson, Laurence H.*
dc.date.accessioned2014-04-28T11:14:24Z
dc.date.available2014-04-28T11:14:24Z
dc.date.issued2011
dc.identifier.citationPors 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.
dc.identifier.urihttp://hdl.handle.net/10454/6138
dc.descriptionNo
dc.description.abstractThe 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.
dc.language.isoen
dc.subjectAlkylating agents
dc.subjectAnimals
dc.subjectBiotransformation
dc.subjectCHO cells
dc.subjectCricetinae
dc.subjectCricetulus
dc.subjectCytochrome P-450 CYP1A1
dc.subjectCytotoxins
dc.subjectHumans
dc.subjectIndoles
dc.subjectMolecular targeted therapy
dc.subjectOxidation-reduction
dc.subjectREF 2014
dc.titleModification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity
dc.typeArticle
dc.type.versionNo full-text in the repository
dc.identifier.doihttps://doi.org/10.1039/c1cc15638a
dc.openaccess.statusclosedAccess


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