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Target intelligence / Profile preview
Tumor Suppressor Gene Promoter Methylation
- Molecular classification
- Epigenetic Modification, DNA Methylation
01
Overview
Tumor suppressor gene promoter methylation refers to the addition of methyl groups to cytosine residues within CpG islands located in the promoter regions of tumor suppressor genes. This epigenetic modification leads to transcriptional silencing of these genes, thereby preventing their normal function in regulating cell growth, apoptosis, and DNA repair. The loss of tumor suppressor gene activity through promoter hypermethylation is a well-established mechanism contributing to cancer initiation and progression.
- Other names
- Tumor Suppressor Gene Promoter HypermethylationTSG Promoter MethylationPromoter Methylation of Tumor Suppressor Genes
02
Mechanism of action
Reversal of DNA methylation by inhibiting DNA methyltransferases (DNMTs)
03
Biological functions
Transcriptional silencingGene regulationChromatin modificationEpigenetic regulation of gene expression
04
Disease associations
Cancer initiationCancer progressionTumorigenesisLoss of tumor suppressor function
05
Safety considerations
Off-target effects of demethylating agentsToxicity associated with demethylating agentsPotential for reactivation of oncogenes
06
Interacting drugs
Azacitidine
1 more in the full profile.
07
Biomarkers
MGMT promoter methylation (gliomas, colorectal cancer)RASSF1A promoter methylation (endometrial carcinoma)GSTP1 promoter methylation (endometrial carcinoma)CDH1 promoter methylation (endometrial carcinoma)p15/CDKN2B promoter methylation (leukemia)p16/CDKN2A promoter methylation (leukemia)RB1 promoter methylation (retinoblastoma, breast, bladder cancer)
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