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Version: 17.06d (Release date: 2017-06-26)
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Histone-Lysine N-Methyltransferase EZH2 Inhibitor GSK2816126 (Code C113334)

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Terms & Properties

Preferred Name: Histone-Lysine N-Methyltransferase EZH2 Inhibitor GSK2816126

Definition: 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.

Display Name: Histone-Lysine N-Methyltransferase EZH2 Inhibitor GSK2816126

Label: Histone-Lysine N-Methyltransferase EZH2 Inhibitor GSK2816126

NCI Thesaurus Code: C113334 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL458162  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
EZH2 Inhibitor GSK2816126
Histone-Lysine N-Methyltransferase EZH2 Inhibitor GSK2816126

External Source Codes: 
PDQ Closed Trial Search ID 756211
PDQ Open Trial Search ID 756211 (check for NCI PDQ open clinical trial info)

Other Properties:
     Name Value (qualifiers indented underneath)
code C113334
Contributing_Source CTRP
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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