NDLI: Studies of Glutathione Transferase P1-1 Bound to a Platinum(IV)-Based Anticancer Compound Reveal the Molecular Basis of Its Activation

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Studies of Glutathione Transferase P1-1 Bound to a Platinum(IV)-Based Anticancer Compound Reveal the Molecular Basis of Its Activation

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Studies of Glutathione Transferase P1-1 Bound to a Platinum(IV)-Based Anticancer Compound Reveal the Molecular Basis of Its Activation

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Hancock, Nancy C. De Luca, Anastasia Ascher, David B. Parker, Lorien J. Campomanes, Pablo Lo Bello, Mario Harris, Hugh H. Dyson, Paul J. Rothlisberger, Ursula Italiano, Louis C. Ang, Wee Han Aitken, Jade B. Parker, Michael W. Morton, Craig J.
Description	Author Affiliation: Parker LJ ( Biota Structural Biology Laboratory, St. Vincent's Institute of Medical Research, 41 Victoria Parade, Fitzroy, Victoria 3065, Australia.)
Abstract	Platinum-based cancer drugs, such as cisplatin, are highly effective chemotherapeutic agents used extensively for the treatment of solid tumors. However, their effectiveness is limited by drug resistance, which, in some cancers, has been associated with an overexpression of pi class glutathione S-transferase (GST P1-1), an important enzyme in the mercapturic acid detoxification pathway. Ethacraplatin (EA-CPT), a $trans-Pt^{IV}$ carboxylate complex containing ethacrynate ligands, was designed as a platinum cancer metallodrug that could also target cytosolic GST enzymes. We previously reported that EA-CPT was an excellent inhibitor of GST activity in live mammalian cells compared to either cisplatin or ethacrynic acid. In order to understand the nature of the drug–protein interactions between EA-CPT and GST P1-1, and to obtain mechanistic insights at a molecular level, structural and biochemical investigations were carried out, supported by molecular modeling analysis using quantum mechanical/molecular mechanical methods. The results suggest that EA-CPT preferentially docks at the dimer interface at GST P1-1 and subsequent interaction with the enzyme resulted in docking of the ethacrynate ligands at both active sites (in the H-sites), with the Pt moiety remaining bound at the dimer interface. The activation of the inhibitor by its target enzyme and covalent binding accounts for the strong and irreversible inhibition of enzymatic activity by the platinum complex.
ISSN	09476539
e-ISSN	15213765
Journal	Chemistry - A European Journal
Issue Number	28
Volume Number	17
Language	English
Publisher	Wiley-VCH;ChemPubSoc Europe
Publisher Date	2011-07-04
Publisher Place	Germany
Access Restriction	Open
Subject Keyword	Antineoplastic Agents Chemistry Metabolism Glutathione S-Transferase Pi Platinum Animals Therapeutic Use Cisplatin Crystallography, X-Ray Dimerization Enzyme Inhibitors Ethacrynic Acid Genetics Models, Molecular Molecular Dynamics Simulation Molecular Sequence Data Molecular Structure Neoplasms Drug Therapy Protein Binding Protein Conformation Recombinant Proteins Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S.
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Catalysis

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