REVIEW An alkylating agent used for the treatment of Grade IV astrocytoma and melanoma. The therapeutic benefit of temozolomide depends on its ability to alkylate/methylate DNA, which most often occurs at the N-7 or O-6 positions of guanine residues. This methylation damages the DNA and triggers the death of tumor cells. However, some tumor cells are able to repair this type of DNA damage, and therefore diminish the therapeutic efficacy of temozolomide, by expressing a protein called O-6-methylguanine-DNA methyltransferase (MGMT) or O-6-alkylguanine-DNA alkyltransferase (AGT or AGAT).
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Algharabil J, Kintner DB, Wang Q, Begum G, Clark PA, Yang SS, Lin SH, Kahle KT, Kuo JS, Sun D (2012). Inhibition of Na(+)-K(+)-2Cl(-) cotransporter isoform 1 accelerates temozolomide-mediated apoptosis in glioblastoma cancer cells. Cell Physiol Biochem. 30(1):33-48. PMID 22759954.
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