The Two Faces of Potent Antitumor Duocarmycin‐Based Drugs: A Structural Dissection Reveals Disparate Motifs for DNA versus Aldehyde Dehydrogenase 1 Affinity | Zendy

Wirth Tanja | Zendy; Pestel Galina F. | Zendy; Ganal Vanessa | Zendy; Kirmeier Thomas | Zendy; Schuberth Ingrid | Zendy; Rein Theo | Zendy; Tietze Professor Lutz F. | Zendy; Sieber Professor Stephan A. | Zendy

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The Two Faces of Potent Antitumor Duocarmycin‐Based Drugs: A Structural Dissection Reveals Disparate Motifs for DNA versus Aldehyde Dehydrogenase 1 Affinity

Author(s) -

Wirth Tanja,

Pestel Galina F.,

Ganal Vanessa,

Kirmeier Thomas,

Schuberth Ingrid,

Rein Theo,

Tietze Professor Lutz F.,

Sieber Professor Stephan A.

Publication year - 2013

Publication title -

angewandte chemie international edition

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.831

H-Index - 550

eISSN - 1521-3773

pISSN - 1433-7851

DOI - 10.1002/anie.201208941

Subject(s) - moiety , aldehyde dehydrogenase , dna , chemistry , aldehyde , computational biology , stereochemistry , combinatorial chemistry , biochemistry , computer science , gene , biology , catalysis

Duocarmycin‐derived seco‐cyclopropabenzindole (CBI) drugs have been shown to bind DNA and an aldehyde dehydrogenase (ALDH1A1) in lung cancer cells. The removal of the DNA‐binding indole moiety results in a CBI compound that does not bind to DNA in whole cells but still exhibits remarkable cytotoxicity. This CBI compound has an increased affinity for ALDH1A1. Rh=rhodamine.

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