Title : Characterization of new potential anticancer drugs designed to overcome glutathione transferase mediated resistance.

Pub. Date : 2011 Oct 3

PMID : 21851097






5 Functional Relationships(s)
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1 Here we used novel strategies to target microsomal glutathione transferase 1 (MGST1) and glutathione transferase pi (GSTP) that are often overexpressed in tumors and confer resistance against a number of cytostatic drugs, including cisplatin and doxorubicin (DOX). Doxorubicin microsomal glutathione S-transferase 1 Homo sapiens
2 Here we used novel strategies to target microsomal glutathione transferase 1 (MGST1) and glutathione transferase pi (GSTP) that are often overexpressed in tumors and confer resistance against a number of cytostatic drugs, including cisplatin and doxorubicin (DOX). Doxorubicin microsomal glutathione S-transferase 1 Homo sapiens
3 Here we synthesized two derivatives of DOX, 2,4-dinitrobenzenesulfonyl doxorubicin (DNS-DOX) and 4-mononitrobenzenesulfonyl doxorubicin (MNS-DOX) and showed that they are substrates for MGST1 and GSTP (releasing DOX). Doxorubicin microsomal glutathione S-transferase 1 Homo sapiens
4 MGST1 overexpressing cells are resistant to DOX. Doxorubicin microsomal glutathione S-transferase 1 Homo sapiens
5 It would appear that, by controlling the reactivity of the prodrug, and thereby the DOX release rate, selective toxicity to MGST1 overexpressing cells can be achieved. Doxorubicin microsomal glutathione S-transferase 1 Homo sapiens