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- NCIT_C156743 IAO_0000115 "An orally available selective inhibitor of the histone lysine methyltransferase (HMT) enhancer of zeste homolog 2 (EZH2), with potential antineoplastic activity. Upon oral administration, EZH2 inhibitor PF-06821497 selectively targets, binds to and inhibits the activity of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 on lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased proliferation of EZH2-expressing cancer cells. EZH2, an HMT class enzyme and the catalytic subunit of the polycomb repressive complex 2 (PRC2), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation; its expression is correlated with tumor initiation, progression, stem cell self-renewal, migration and angiogenesis." @default.
- NCIT_C156743 NCIT_A32 NCIT_C1909 @default.
- NCIT_C156743 NCIT_NHC0 "C156743" @default.
- NCIT_C156743 NCIT_P106 "Organic Chemical" @default.
- NCIT_C156743 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C156743 NCIT_P108 "EZH2 Inhibitor PF-06821497" @default.
- NCIT_C156743 NCIT_P208 "CL935894" @default.
- NCIT_C156743 NCIT_P210 "1844849-10-0" @default.
- NCIT_C156743 NCIT_P319 "S4L4MM20B6" @default.
- NCIT_C156743 NCIT_P322 "FDA" @default.
- NCIT_C156743 NCIT_P322 "GDC" @default.
- NCIT_C156743 NCIT_P329 "795703" @default.
- NCIT_C156743 NCIT_P330 "795703" @default.
- NCIT_C156743 NCIT_P375 "EZH2 Inhibitor PF-06821497" @default.
- NCIT_C156743 NCIT_P399 "795703" @default.
- NCIT_C156743 normalizedInformationContent "100" @default.
- NCIT_C156743 referenceCount "1" @default.
- NCIT_C156743 hasExactSynonym "1(2H)-Isoquinolinone, 5,8-Dichloro-2-((1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl)-3,4-dihydro-7-((R)-methoxy-3-oxetanylmethyl)-" @default.
- NCIT_C156743 hasExactSynonym "EZH2 Inhibitor PF-06821497" @default.
- NCIT_C156743 hasExactSynonym "PF 06821497" @default.
- NCIT_C156743 hasExactSynonym "PF-06821497" @default.
- NCIT_C156743 hasExactSynonym "PF06821497" @default.
- NCIT_C156743 inSubset NCIT_C128784 @default.
- NCIT_C156743 inSubset NCIT_C157711 @default.
- NCIT_C156743 inSubset NCIT_C157712 @default.
- NCIT_C156743 inSubset NCIT_C176424 @default.
- NCIT_C156743 inSubset NCIT_C177537 @default.
- NCIT_C156743 inSubset NCIT_C63923 @default.
- NCIT_C156743 type Class @default.
- NCIT_C156743 isDefinedBy ncit.owl @default.
- NCIT_C156743 label "EZH2 Inhibitor PF-06821497" @default.
- NCIT_C156743 subClassOf NCIT_C129824 @default.
- NCIT_C156743 subClassOf NCIT_C129825 @default.
- NCIT_C156743 subClassOf NCIT_C156743 @default.
- NCIT_C156743 subClassOf NCIT_C156804 @default.
- NCIT_C156743 subClassOf NCIT_C1908 @default.
- NCIT_C156743 subClassOf NCIT_C1909 @default.
- NCIT_C156743 subClassOf NCIT_C2189 @default.
- NCIT_C156743 subClassOf NCIT_C274 @default.
- NCIT_C156743 subClassOf NCIT_C471 @default.