O-methylguanine-DNA-methyltransferase (MGMT) is a DNA repair enzyme, which
reverses the alkylation of guanine O through directtransfer of the methyl
group, maintains the gene stability and avoids tumor occurrence. Studies have
shown that MGMT gene methylation, polymorphism and protein expression are
involved in the process of various tumor development, such as colon cancer,
gastric carcinoma, etc. MGMT gene promotes methylation, protein
expression and enzyme activity from various tissues, which resultsin different
effects on the prognosis of patients. MGMT promoter methylation is a positive
factor for the prognosis of Glioblastoma (GBM), which can prolong overall
survival and progression-free survival, reduce the resistance of tumor cells to
temozolomide treatment, and improve the prognosis. The treatment of tumors based
on MGMT focuses on three aspects: targeting MGMT to increase the sensitivity of
alkylated drug therapy in tumors, immunotherapy combined with alkylated agents on
tumor treatment, and treatment for patients with MGMT promoter non-methylation.
Similarly, a number of studies have targeted MGMT to reduce alkylated agent
resistance in other systems. Although numerous studies on MGMT in tumors have
been reported, there are problems that need to be solved, such as selection and
consensus of MGMT promoter methylation detection methods (CpG detection sites,
cut-off value) and the treatment of MGMT non-methylated GBM patients, especially
elderly patients. In this review, we describe the regulation of MGMT expression
and its role inchemotherapy, especially in gliomas. Further studies exploring new
methods targeting MGMT with better curative effect and less toxicity are
advocated. We anticipate that these developments will be progressive and
sufficiently used for clinical application.