Health / Medical Topics

    DNA Methyltransferase Inhibitor SGI-110

    A dinucleotide antimetabolite of a decitabine linked via phosphodiester bond to a guanosine, with potential antineoplastic activity. Following metabolic activation by phosphorylation and incorporation into DNA, SGI-110 inhibits DNA methyltransferase, thereby causing genome-wide and non-specific hypomethylation, and inducing cell cycle arrest at S-phase. This agent is resistant to cytidine deaminase, hence may result in gradual release of decitabine both extra and intracellularly, leading to more prolonged exposures to decitabine. (NCI Thesaurus)




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