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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| Main Authors: | , |
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| Format: | Book |
| Published: |
MDPI AG,
2013-04-01T00:00:00Z.
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| Online Access: | Connect to this object online. |
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| Summary: | 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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| Item Description: | 10.3390/pharmaceutics5020220 1999-4923 |