Abstract
Temozolomide (TMZ) is an alkylating agent that is widely used in chemotherapy for cancer. A key mechanism of resistance to TMZ is the overexpression of O(6)-methylguanine-DNA methyltransferase (MGMT). MGMT specifically repairs the DNA O(6)-methylation damage induced by TMZ and irreversibly inactivates TMZ. Regulation of MGMT expression and research regarding the mechanism of TMZ resistance will help rationalize the clinical use of TMZ. In this review, we provide an overview of recent advances in the field, with particular emphasis on MGMT structure, function, expression regulation, and the association between MGMT and resistance to TMZ.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Antineoplastic Agents, Alkylating / pharmacology*
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Antineoplastic Agents, Alkylating / therapeutic use
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DNA Methylation
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Dacarbazine / analogs & derivatives*
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Dacarbazine / pharmacology
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Dacarbazine / therapeutic use
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Drug Resistance, Neoplasm / genetics*
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Gene Expression
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Gene Expression Regulation, Neoplastic
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Humans
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Neoplasms / drug therapy
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Neoplasms / genetics
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O(6)-Methylguanine-DNA Methyltransferase / antagonists & inhibitors
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O(6)-Methylguanine-DNA Methyltransferase / genetics*
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Promoter Regions, Genetic
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Research*
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Temozolomide
Substances
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Antineoplastic Agents, Alkylating
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Dacarbazine
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O(6)-Methylguanine-DNA Methyltransferase
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Temozolomide