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Version: 17.06d (Release date: 2017-06-26)
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DOT1L Inhibitor EPZ-5676 (Code C103179)

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Terms & Properties

Preferred Name: DOT1L Inhibitor EPZ-5676

Definition: A small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Upon intravenous administration, EPZ-5676 specifically blocks the activity of the histone lysine-methyltransferase DOT1L, thereby inhibiting the methylation of nucleosomal histone H3 on lysine 79 (H3K79) that is bound to the mixed lineage leukemia (MLL) fusion protein which targets genes and blocks the expression of leukemogenic genes. This eventually leads to an induction of apoptosis in the leukemic cells bearing the MLL gene translocations. DOT1L, a non-SET domain-containing histone methyltransferase, specifically methylates H3K79 and plays a key role in normal cell differentiation and in the development of leukemia with MLL gene rearrangement on chromosome 11 and promotes the expression of leukemia-causing genes.

Display Name: DOT1L Inhibitor EPZ-5676

Label: DOT1L Inhibitor EPZ-5676

NCI Thesaurus Code: C103179 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3641112  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
DOT1L Inhibitor EPZ-5676
EPZ-5676

External Source Codes: 
PDQ Closed Trial Search ID 740411
PDQ Open Trial Search ID 740411 (check for NCI PDQ open clinical trial info)
UMLS CUI C3641112

Other Properties:
     Name Value (qualifiers indented underneath)
code C103179
Contributing_Source CTRP
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C103179

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