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- NCIT_C201128 IAO_0000115 "An orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon oral administration, CDK2 inhibitor ARTS-021 selectively targets, reversibly binds to and inhibits the activity of the CDK2/CyclinE1 (CCNE1; CCNE-1) complex. This inhibits retinoblastoma (Rb) phosphorylation and blocks G1/S transition, which leads to cell cycle arrest, the induction of apoptosis, and the inhibition of proliferation in CDK2 and/or CCNE1-overexpressing tumor cells. CDK2, a serine/threonine kinase that plays an important role in the regulation of cell cycle progression and cellular proliferation, is overexpressed in certain tumor cells. CCNE1, a regulatory factor and activator of CDK2 is overexpressed in various tumor cell types and CCNE1 overexpression elevates the activity of CDK2." @default.
- NCIT_C201128 NCIT_A7 NCIT_C25842 @default.
- NCIT_C201128 NCIT_NHC0 "C201128" @default.
- NCIT_C201128 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C201128 NCIT_P107 "CDK2 Inhibitor ARTS-021" @default.
- NCIT_C201128 NCIT_P108 "CDK2 Inhibitor ARTS-021" @default.
- NCIT_C201128 NCIT_P322 "CTRP" @default.
- NCIT_C201128 NCIT_P322 "GDC" @default.
- NCIT_C201128 normalizedInformationContent "100" @default.
- NCIT_C201128 referenceCount "1" @default.
- NCIT_C201128 hasExactSynonym "ARTS 021" @default.
- NCIT_C201128 hasExactSynonym "ARTS-021" @default.
- NCIT_C201128 hasExactSynonym "ARTS021" @default.
- NCIT_C201128 hasExactSynonym "CDK2 Inhibitor ARTS-021" @default.
- NCIT_C201128 inSubset NCIT_C116977 @default.
- NCIT_C201128 inSubset NCIT_C116978 @default.
- NCIT_C201128 inSubset NCIT_C128784 @default.
- NCIT_C201128 inSubset NCIT_C157711 @default.
- NCIT_C201128 inSubset NCIT_C157712 @default.
- NCIT_C201128 inSubset NCIT_C176424 @default.
- NCIT_C201128 type Class @default.
- NCIT_C201128 isDefinedBy ncit.owl @default.
- NCIT_C201128 label "CDK2 Inhibitor ARTS-021" @default.
- NCIT_C201128 subClassOf NCIT_C129824 @default.
- NCIT_C201128 subClassOf NCIT_C129825 @default.
- NCIT_C201128 subClassOf NCIT_C1404 @default.
- NCIT_C201128 subClassOf NCIT_C163758 @default.
- NCIT_C201128 subClassOf NCIT_C1908 @default.
- NCIT_C201128 subClassOf NCIT_C1909 @default.
- NCIT_C201128 subClassOf NCIT_C200052 @default.
- NCIT_C201128 subClassOf NCIT_C201128 @default.
- NCIT_C201128 subClassOf NCIT_C2185 @default.
- NCIT_C201128 subClassOf NCIT_C2189 @default.
- NCIT_C201128 subClassOf NCIT_C274 @default.
- NCIT_C201128 subClassOf NCIT_C471 @default.
- NCIT_C201128 subClassOf NCIT_C61074 @default.