Numerous in vitro, in vivo, and ex vivo studies have revealed multiple molecular fingerprints of gliomas, such as methylation of the O(6)-methylguanine-DNA methyltransferase (MGMT) promoter, mutant isocitrate dehydrogenase (IDH), platelet-derived growth factor receptor (PDGFR), vascular endothelial growth factor receptor (VEGFR), integrin αvβ3 receptor, epidermal growth factor receptor (EGFR), c-Met, etc. These tumor-specific molecules can be used not only as targets for diagnosis and therapeutic response assessment, but also as potential targets for glioma treatment. Here, MGMT is linked to central nervous system cancer.