Abstract
Alkylating agents such as temozolomide (TMZ) are effective anticancer drugs for treating a variety of solid tumors including melanoma, glioma, and astrocytoma. TMZ exerts its effects mainly via the mutagenic product O6-methylguanine, a cytotoxic DNA lesion. This damage may be repaired by the DNA repair enzyme O6-methylguanine DNA methyltransferase (MGMT), a key player in the resistance of cancers to TMZ. Several strategies are presently being pursued to improve the killing of tumor cells by TMZ, with inhibition of MGMT being the most promising. In this review, we provide an overview of recent advances in this field.
Keywords: Temozolomide, DNA repair, MGMT, cancer therapy, Alkylating agents, anticancer drugs, solid tumors, melanoma, glioma, astrocytoma
Current Medicinal Chemistry
Title:Strategies to Improve the Killing of Tumors Using Temozolomide: Targeting the DNA Repair Protein MGMT
Volume: 19 Issue: 23
Author(s): G. Jiang, L. -T. Li, Y. Xin, L. Zhang, Y. -Q. Liu and J. -N. Zheng
Affiliation:
Keywords: Temozolomide, DNA repair, MGMT, cancer therapy, Alkylating agents, anticancer drugs, solid tumors, melanoma, glioma, astrocytoma
Abstract: Alkylating agents such as temozolomide (TMZ) are effective anticancer drugs for treating a variety of solid tumors including melanoma, glioma, and astrocytoma. TMZ exerts its effects mainly via the mutagenic product O6-methylguanine, a cytotoxic DNA lesion. This damage may be repaired by the DNA repair enzyme O6-methylguanine DNA methyltransferase (MGMT), a key player in the resistance of cancers to TMZ. Several strategies are presently being pursued to improve the killing of tumor cells by TMZ, with inhibition of MGMT being the most promising. In this review, we provide an overview of recent advances in this field.
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Cite this article as:
Jiang G., -T. Li L., Xin Y., Zhang L., -Q. Liu Y. and -N. Zheng J., Strategies to Improve the Killing of Tumors Using Temozolomide: Targeting the DNA Repair Protein MGMT, Current Medicinal Chemistry 2012; 19 (23) . https://dx.doi.org/10.2174/092986712802002446
DOI https://dx.doi.org/10.2174/092986712802002446 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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