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- NCIT_C185593 IAO_0000115 "A third-generation, reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon administration, BTK inhibitor HMPL-760 non-covalently binds to and inhibits the activity of both wild-type and the C481S mutated form of BTK, a resistance mutation in the BTK active site in which cysteine is substituted for serine at residue 481. This prevents the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B-cells that overexpress BTK or the C481S mutated form. BTK C481S mutation plays an important role in resistance to certain BTK inhibitors; HMPL-760 may be able to overome this resistance. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B-lymphocytes." @default.
- NCIT_C185593 NCIT_A7 NCIT_C75017 @default.
- NCIT_C185593 NCIT_NHC0 "C185593" @default.
- NCIT_C185593 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C185593 NCIT_P107 "BTK Inhibitor HMPL-760" @default.
- NCIT_C185593 NCIT_P108 "BTK Inhibitor HMPL-760" @default.
- NCIT_C185593 NCIT_P208 "CL1773932" @default.
- NCIT_C185593 NCIT_P322 "CTRP" @default.
- NCIT_C185593 NCIT_P322 "GDC" @default.
- NCIT_C185593 NCIT_P399 "808293" @default.
- NCIT_C185593 normalizedInformationContent "100" @default.
- NCIT_C185593 referenceCount "1" @default.
- NCIT_C185593 hasExactSynonym "BTK Inhibitor HMPL-760" @default.
- NCIT_C185593 hasExactSynonym "Bruton's Tyrosine Kinase Inhibitor HMPL760" @default.
- NCIT_C185593 hasExactSynonym "HMPL 760" @default.
- NCIT_C185593 hasExactSynonym "HMPL-760" @default.
- NCIT_C185593 hasExactSynonym "HMPL760" @default.
- NCIT_C185593 inSubset NCIT_C116977 @default.
- NCIT_C185593 inSubset NCIT_C116978 @default.
- NCIT_C185593 inSubset NCIT_C128784 @default.
- NCIT_C185593 inSubset NCIT_C157711 @default.
- NCIT_C185593 inSubset NCIT_C157712 @default.
- NCIT_C185593 inSubset NCIT_C176424 @default.
- NCIT_C185593 type Class @default.
- NCIT_C185593 isDefinedBy ncit.owl @default.
- NCIT_C185593 label "BTK Inhibitor HMPL-760" @default.
- NCIT_C185593 subClassOf NCIT_C124801 @default.
- NCIT_C185593 subClassOf NCIT_C129824 @default.
- NCIT_C185593 subClassOf NCIT_C129825 @default.
- NCIT_C185593 subClassOf NCIT_C1404 @default.
- NCIT_C185593 subClassOf NCIT_C163758 @default.
- NCIT_C185593 subClassOf NCIT_C163774 @default.
- NCIT_C185593 subClassOf NCIT_C185593 @default.
- NCIT_C185593 subClassOf NCIT_C1908 @default.
- NCIT_C185593 subClassOf NCIT_C1909 @default.
- NCIT_C185593 subClassOf NCIT_C1967 @default.
- NCIT_C185593 subClassOf NCIT_C2189 @default.
- NCIT_C185593 subClassOf NCIT_C274 @default.
- NCIT_C185593 subClassOf NCIT_C471 @default.