Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

Klaus Pors; Paul M. Loadman; Steven D. Shnyder; Mark Sutherland; Helen M. Sheldrake; Meritxell Guino; Konstantinos Kiakos; John A. Hartley; Mark Searcey; Laurence H. Patterson

doi:10.1039/C1CC15638A

Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

Klaus Pors, Paul M. Loadman, Steven D. Shnyder, Mark Sutherland, Helen M. Sheldrake, Meritxell Guino, Konstantinos Kiakos, John A. Hartley, Mark Searcey, Laurence H. Patterson

Research output: Contribution to journal › Article › peer-review

35 Citations (Scopus)

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.

Original language	English
Pages (from-to)	12062-12064
Number of pages	3
Journal	Chemical Communications
Volume	47
Issue number	44
DOIs	https://doi.org/10.1039/C1CC15638A
Publication status	Published - 2011

Access to Document

10.1039/C1CC15638A

Cite this

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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.",

author = "Klaus Pors and Loadman, {Paul M.} and Shnyder, {Steven D.} and Mark Sutherland and Sheldrake, {Helen M.} and Meritxell Guino and Konstantinos Kiakos and Hartley, {John A.} and Mark Searcey and Patterson, {Laurence H.}",

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T1 - Modification of the duocarmycin pharmacophore enables CYP1A1 targeting for biological activity

AU - Pors, Klaus

AU - Loadman, Paul M.

AU - Shnyder, Steven D.

AU - Sutherland, Mark

AU - Sheldrake, Helen M.

AU - Guino, Meritxell

AU - Kiakos, Konstantinos

AU - Hartley, John A.

AU - Searcey, Mark

AU - Patterson, Laurence H.

PY - 2011

Y1 - 2011

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AB - 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.

U2 - 10.1039/C1CC15638A

DO - 10.1039/C1CC15638A

M3 - Article

VL - 47

SP - 12062

EP - 12064

JO - Chemical Communications

JF - Chemical Communications

SN - 1359-7345

IS - 44

ER -