| Health / Medical Topics |
Histone-Lysine N-Methyltransferase EZH2 Inhibitor GSK2816126
A small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone-lysine N-methyltransferase EZH2, with potential antineoplastic activity. Upon administration, histone-lysine N-methyltransferase EZH2 inhibitor GSK2816126 inhibits the activity of EZH2 and specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in cancer cells that overexpress this enzyme. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancers and plays a key role in tumor cell proliferation. (NCI Thesaurus)
YOU MAY ALSO LIKE
Histone-lysine N-methyltransferase EZH2 (746 aa, ~85 kDa) is encoded by the human EZH2 gene. This protein is involved in the regulation of…
Histone-lysine N-methyltransferase EHMT1 (1298 aa, ~141 kDa) is encoded by the human EHMT1 gene. This protein plays a role in histone…
Histone-binding protein RBBP4 (425 aa, ~48 kDa) is encoded by the human RBBP4 gene. This protein is involved in transcriptional regulation, cell…
Histone-arginine methyltransferase CARM1 (585 aa, ~63 kDa) is encoded by the human CARM1 gene. This protein is involved in the mediation of…
A substance that blocks certain enzymes involved in gene expression and cell division. These enzymes may be found in a mutated (changed)…
An orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon…
