Title : Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription.

Pub. Date : 2016 Apr 28

PMID : 27088648






4 Functional Relationships(s)
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1 Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription. Cyproheptadine SET domain containing 7, histone lysine methyltransferase Homo sapiens
2 Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription. Cyproheptadine SET domain containing 7, histone lysine methyltransferase Homo sapiens
3 We identified cyproheptadine, a clinically approved antiallergy drug, as a Set7/9 inhibitor in a high-throughput screen using a fluorogenic substrate-based HMT assay. Cyproheptadine SET domain containing 7, histone lysine methyltransferase Homo sapiens
4 Kinetic and X-ray crystallographic analyses revealed that cyproheptadine binds in the substrate-binding pocket of Set7/9 and inhibits its enzymatic activity by competing with the methyl group acceptor. Cyproheptadine SET domain containing 7, histone lysine methyltransferase Homo sapiens