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- NCIT_C162010 IAO_0000115 "An orally available, small-molecule, irreversible inhibitor of interleukin-2 inducible T-cell kinase (ITK) with potential immunomodulatory and antineoplastic activities. Upon oral administration, ITK inhibitor CPI-818 selectively and covalently binds to the cysteine residue at position 442 (CYS-442) of ITK, thereby disrupting ITK-mediated signal transduction, while sparing tyrosine-protein kinase TXK (resting lymphocyte kinase, RLK) activity. This may abrogate T-cell receptor (TCR) signaling through ITK and inhibit TCR-induced proliferation of malignant T-cells. Additionally, inhibiting ITK activation may prevent the upregulation of GATA-3, a transcription factor that drives T-helper 2 (Th2) cell differentiation and is overexpressed in certain T-cell lymphomas. Thus, selective inhibition of ITK may inhibit Th2 responses without affecting T-helper 1 (Th1)-dependent immunity. ITK, a member of the Tec family of non-receptor protein tyrosine kinases plays a significant role in the T-cell development, differentiation and production of pro-inflammatory cytokines." @default.
- NCIT_C162010 NCIT_A32 NCIT_C1909 @default.
- NCIT_C162010 NCIT_A7 NCIT_C29753 @default.
- NCIT_C162010 NCIT_NHC0 "C162010" @default.
- NCIT_C162010 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C162010 NCIT_P107 "ITK Inhibitor CPI-818" @default.
- NCIT_C162010 NCIT_P108 "ITK Inhibitor CPI-818" @default.
- NCIT_C162010 NCIT_P208 "CL970662" @default.
- NCIT_C162010 NCIT_P322 "CTRP" @default.
- NCIT_C162010 NCIT_P322 "GDC" @default.
- NCIT_C162010 NCIT_P329 "798593" @default.
- NCIT_C162010 NCIT_P330 "798593" @default.
- NCIT_C162010 NCIT_P375 "ITK Inhibitor CPI-818" @default.
- NCIT_C162010 NCIT_P399 "798593" @default.
- NCIT_C162010 normalizedInformationContent "100" @default.
- NCIT_C162010 referenceCount "1" @default.
- NCIT_C162010 hasExactSynonym "CPI 818" @default.
- NCIT_C162010 hasExactSynonym "CPI-818" @default.
- NCIT_C162010 hasExactSynonym "CPI818" @default.
- NCIT_C162010 hasExactSynonym "ITK Inhibitor CPI-818" @default.
- NCIT_C162010 hasExactSynonym "Interleukin-2 Inducible T-cell Kinase Inhibitor CPI-818" @default.
- NCIT_C162010 inSubset NCIT_C116977 @default.
- NCIT_C162010 inSubset NCIT_C116978 @default.
- NCIT_C162010 inSubset NCIT_C128784 @default.
- NCIT_C162010 inSubset NCIT_C157711 @default.
- NCIT_C162010 inSubset NCIT_C157712 @default.
- NCIT_C162010 inSubset NCIT_C176424 @default.
- NCIT_C162010 inSubset NCIT_C177537 @default.
- NCIT_C162010 type Class @default.
- NCIT_C162010 isDefinedBy ncit.owl @default.
- NCIT_C162010 label "ITK Inhibitor CPI-818" @default.
- NCIT_C162010 subClassOf NCIT_C129820 @default.
- NCIT_C162010 subClassOf NCIT_C129824 @default.
- NCIT_C162010 subClassOf NCIT_C129825 @default.
- NCIT_C162010 subClassOf NCIT_C1404 @default.
- NCIT_C162010 subClassOf NCIT_C156794 @default.
- NCIT_C162010 subClassOf NCIT_C162010 @default.
- NCIT_C162010 subClassOf NCIT_C1908 @default.
- NCIT_C162010 subClassOf NCIT_C1909 @default.
- NCIT_C162010 subClassOf NCIT_C1967 @default.
- NCIT_C162010 subClassOf NCIT_C2189 @default.
- NCIT_C162010 subClassOf NCIT_C274 @default.
- NCIT_C162010 subClassOf NCIT_C308 @default.
- NCIT_C162010 subClassOf NCIT_C471 @default.