About: DOT1L Inhibitor EPZ-5676     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • DOT1L Inhibitor EPZ-5676
rdfs:subClassOf
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • DOT1L Inhibitor EPZ-5676
NCI_META_CUI
  • CL437426
PDQ_Open_Trial_Search_ID
  • 740411
PDQ_Closed_Trial_Search_ID
  • 740411
FULL_SYN
  • DOT1L Inhibitor EPZ-5676PTNCI
  • EPZ-5676CNNCI
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.NCI
code
  • C103179
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