A rationally designed Pt(IV) anticancer compound is described, employing the novel concept of tethering an inhibitor of glutathione-S-transferase, an enzyme associated with Pt-based drug-resistance, to cisplatin. Its enzyme inhibition activity, investigated using spectrophotometric and mass spectrometry-based techniques, and cytotoxic profile in resistant cancer cells are described.
Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance. Publishing Authors By Initials
Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance. Journal Published:
PUBLICATION TYPE: Research Support, Non-U.S. Gov
Journal: Journal of the American Chemical Society
VOLUME: 127
Page Numbers: 1382-3
Journal Abbreviation: J. Am. Chem. Soc.
ISSN: 0002-7863
DAY: 9
MONTH: Feb
YEAR: 2005
Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance. Information
Number of References:
LANGUAGE: eng
NlmUniqueID: 7503056
Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance. Keywords Mesh Terms:
KEYWORDS: Organoplatinum Compounds
MESH TERMS: pharmacology
Chemical & Substance for Abstract: Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance. Information
Substance Name: Glutathione Transferase
Registry Number: EC 2.5.1.18
Grant and Affiliation Information for Rational design of platinum(IV) compounds to overcome glutathione-S-transferase mediated drug resistance.
AFFILIATION: Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne, EPFL-BCH, CH 1015 Lausanne, Switzerland.
Country: United States
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MEDLINETA: J Am Chem Soc
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