Glutathione Transferase (GST)-Activated Prodrugs

Glutathione transferase (formerly GST) catalyzes the inactivation of various electrophile-producing anticancer agents via conjugation to the tripeptide glutathione. Moreover, several data link the overexpression of some GSTs, in particular GSTP1-1, to both natural and acquired resistance to various...

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Detalles Bibliográficos
Autores principales: Ruzza, Paolo, Calderan, Andrea
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3834953/
https://www.ncbi.nlm.nih.gov/pubmed/24300447
http://dx.doi.org/10.3390/pharmaceutics5020220
Descripción
Sumario:Glutathione transferase (formerly GST) catalyzes the inactivation of various electrophile-producing anticancer agents via conjugation to the tripeptide glutathione. Moreover, several data link the overexpression of some GSTs, in particular GSTP1-1, to both natural and acquired resistance to various structurally unrelated anticancer drugs. Tumor overexpression of these proteins has provided a rationale for the search of GST inhibitors and GST activated cytotoxic prodrugs. In the present review we discuss the current structural and pharmacological knowledge of GST-activated cytotoxic compounds.

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