title: Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity.
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.
authors: Institute of Cancer Therapeutics, University of Bradford, West Yorkshire BD7 1DP, UK.
authors: Klaus
authors: K
authors: Pors
authors: Paul M
authors: PM
authors: Loadman
authors: Steven D
authors: SD
authors: Shnyder
authors: Mark
authors: M
authors: Sutherland
authors: Helen M
authors: HM
authors: Sheldrake
authors: Meritxell
authors: M
authors: Guino
authors: Konstantinos
authors: K
authors: Kiakos
authors: John A
authors: JA
authors: Hartley
authors: Mark
authors: M
authors: Searcey
authors: Laurence H
authors: LH
authors: Patterson
mesh_terms: D000477:Alkylating Agents / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001711:Biotransformation; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D019363:Cytochrome P-450 CYP1A1 / Q000235:genetics / Q000378:metabolism*; D003603:Cytotoxins / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology*; D058990:Molecular Targeted Therapy; D010084:Oxidation-Reduction
chemical_list: D000477:Alkylating Agents; D003603:Cytotoxins; D007211:Indoles; D019363:Cytochrome P-450 CYP1A1