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- NCIT_C134448 IAO_0000115 "A specific inhibitor of heat shock protein 90 (Hsp90) subtypes alpha and beta, with potential antineoplastic and chemo/radiosensitizing activities. Upon oral administration, pimitespib specifically binds to and inhibits the activity of Hsp90 alpha and beta; this results in the proteasomal degradation of oncogenic client proteins, which inhibits client protein dependent-signaling, induces apoptosis, and inhibits the proliferation of cells overexpressing HSP90alpha/beta. Hsp90, a family of molecular chaperone proteins that are upregulated in a variety of tumor cells, plays a key role in the conformational maturation, stability, and function of "client" proteins within the cell,; many of which are involved in signal transduction, cell cycle regulation and apoptosis, including kinases, cell-cycle regulators, transcription factors and hormone receptors. As TAS-116 selectively inhibits cytosolic HSP90alpha and beta only and does not inhibit HSP90 paralogs, such as endoplasmic reticulum GRP94 or mitochondrial TRAP1, this agent may have less off-target toxicity as compared to non-selective HSP90 inhibitors." @default.
- NCIT_C134448 NCIT_A32 NCIT_C1909 @default.
- NCIT_C134448 NCIT_A7 NCIT_C97588 @default.
- NCIT_C134448 NCIT_A7 NCIT_C97591 @default.
- NCIT_C134448 NCIT_NHC0 "C134448" @default.
- NCIT_C134448 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C134448 NCIT_P107 "Pimitespib" @default.
- NCIT_C134448 NCIT_P108 "Pimitespib" @default.
- NCIT_C134448 NCIT_P207 "C4044757" @default.
- NCIT_C134448 NCIT_P210 "1260533-36-5" @default.
- NCIT_C134448 NCIT_P319 "PLO044MUDZ" @default.
- NCIT_C134448 NCIT_P322 "CTRP" @default.
- NCIT_C134448 NCIT_P322 "FDA" @default.
- NCIT_C134448 NCIT_P322 "GDC" @default.
- NCIT_C134448 NCIT_P329 "788861" @default.
- NCIT_C134448 NCIT_P330 "788861" @default.
- NCIT_C134448 NCIT_P375 "HSP90alpha/beta Inhibitor TAS-116" @default.
- NCIT_C134448 NCIT_P375 "Pimitespib" @default.
- NCIT_C134448 NCIT_P399 "788861" @default.
- NCIT_C134448 NCIT_R125 NCIT_C17828 @default.
- NCIT_C134448 NCIT_R125 NCIT_C20150 @default.
- NCIT_C134448 NCIT_R125 NCIT_C20480 @default.
- NCIT_C134448 NCIT_R125 NCIT_C40715 @default.
- NCIT_C134448 NCIT_R125 NCIT_C41515 @default.
- NCIT_C134448 NCIT_R125 NCIT_C51037 @default.
- NCIT_C134448 normalizedInformationContent "100" @default.
- NCIT_C134448 referenceCount "1" @default.
- NCIT_C134448 hasExactSynonym "3-Ethyl-4-(3-(1-methylethyl)-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo(3,4-b)pyridin-1-yl)benzamide" @default.
- NCIT_C134448 hasExactSynonym "HSP90alpha/beta Inhibitor TAS-116" @default.
- NCIT_C134448 hasExactSynonym "Heat Shock Protein 90 alpha/beta Inhibitor TAS-116" @default.
- NCIT_C134448 hasExactSynonym "PIMITESPIB" @default.
- NCIT_C134448 hasExactSynonym "Pimitespib" @default.
- NCIT_C134448 hasExactSynonym "TAS-116" @default.
- NCIT_C134448 hasExactSynonym "TAS116" @default.
- NCIT_C134448 inSubset NCIT_C116977 @default.
- NCIT_C134448 inSubset NCIT_C116978 @default.
- NCIT_C134448 inSubset NCIT_C128784 @default.
- NCIT_C134448 inSubset NCIT_C157711 @default.
- NCIT_C134448 inSubset NCIT_C157712 @default.
- NCIT_C134448 inSubset NCIT_C176424 @default.
- NCIT_C134448 inSubset NCIT_C177537 @default.
- NCIT_C134448 inSubset NCIT_C63923 @default.
- NCIT_C134448 type Class @default.
- NCIT_C134448 isDefinedBy ncit.owl @default.
- NCIT_C134448 label "Pimitespib" @default.
- NCIT_C134448 subClassOf NCIT_C129824 @default.
- NCIT_C134448 subClassOf NCIT_C134448 @default.
- NCIT_C134448 subClassOf NCIT_C156880 @default.
- NCIT_C134448 subClassOf NCIT_C1908 @default.
- NCIT_C134448 subClassOf NCIT_C1909 @default.
- NCIT_C134448 subClassOf NCIT_C2189 @default.
- NCIT_C134448 subClassOf NCIT_C274 @default.
- NCIT_C134448 subClassOf NCIT_C74526 @default.