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- NCIT_C173698 IAO_0000115 "An orally bioavailable inhibitor of the histone lysine methyltransferases enhancer of zeste homolog 1 (EZH1) and 2 (EZH2), with potential antineoplastic activity. Upon oral administration, EZH1/2 inhibitor HH2853 inhibits the activity of both wild-type and mutated forms of EZH1 and EZH2. Inhibition of EZH1/2 specifically prevents the methylation of lysine 27 on histone H3 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways, enhances transcription of certain target genes, and results in decreased proliferation of EZH1/2-expressing cancer cells. EZH1/2, histone lysine methyltransferase (HMT) class enzymes and catalytic subunits of the polycomb repressive complex 2 (PRC2), are overexpressed or mutated in a variety of cancer cells and play key roles in tumor cell proliferation, progression, stem cell self-renewal and migration." @default.
- NCIT_C173698 NCIT_A32 NCIT_C1909 @default.
- NCIT_C173698 NCIT_NHC0 "C173698" @default.
- NCIT_C173698 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C173698 NCIT_P107 "EZH1/2 Inhibitor HH2853" @default.
- NCIT_C173698 NCIT_P108 "EZH1/2 Inhibitor HH2853" @default.
- NCIT_C173698 NCIT_P208 "CL1407522" @default.
- NCIT_C173698 NCIT_P322 "CTRP" @default.
- NCIT_C173698 NCIT_P322 "GDC" @default.
- NCIT_C173698 NCIT_P329 "802064" @default.
- NCIT_C173698 NCIT_P330 "802064" @default.
- NCIT_C173698 NCIT_P375 "EZH1/2 Inhibitor HH2853" @default.
- NCIT_C173698 NCIT_P399 "802064" @default.
- NCIT_C173698 normalizedInformationContent "100" @default.
- NCIT_C173698 referenceCount "1" @default.
- NCIT_C173698 hasExactSynonym "EZH1 and EZH2 Inhibitor HH2853" @default.
- NCIT_C173698 hasExactSynonym "EZH1/2 Inhibitor HH2853" @default.
- NCIT_C173698 hasExactSynonym "HH 2853" @default.
- NCIT_C173698 hasExactSynonym "HH-2853" @default.
- NCIT_C173698 hasExactSynonym "HH2853" @default.
- NCIT_C173698 inSubset NCIT_C116977 @default.
- NCIT_C173698 inSubset NCIT_C116978 @default.
- NCIT_C173698 inSubset NCIT_C128784 @default.
- NCIT_C173698 inSubset NCIT_C157711 @default.
- NCIT_C173698 inSubset NCIT_C157712 @default.
- NCIT_C173698 inSubset NCIT_C176424 @default.
- NCIT_C173698 inSubset NCIT_C177537 @default.
- NCIT_C173698 type Class @default.
- NCIT_C173698 isDefinedBy ncit.owl @default.
- NCIT_C173698 label "EZH1/2 Inhibitor HH2853" @default.
- NCIT_C173698 subClassOf NCIT_C129824 @default.
- NCIT_C173698 subClassOf NCIT_C129825 @default.
- NCIT_C173698 subClassOf NCIT_C156804 @default.
- NCIT_C173698 subClassOf NCIT_C173698 @default.
- NCIT_C173698 subClassOf NCIT_C1908 @default.
- NCIT_C173698 subClassOf NCIT_C1909 @default.
- NCIT_C173698 subClassOf NCIT_C2189 @default.
- NCIT_C173698 subClassOf NCIT_C274 @default.
- NCIT_C173698 subClassOf NCIT_C471 @default.