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- NCIT_C182615 IAO_0000115 "An orally bioavailable, targeted degrader of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase) by using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. BGB-16673 is comprised of an E3 ubiquitin ligase binding moiety conjugated, via a linker, to a BTK-binding moiety. Upon oral administration, BTK degrader BGB-16673 targets and binds to BTK with its BTK-targeting moiety, thereby inhibiting its activity. Upon binding, the E3 ligase-binding moiety binds to cereblon (CRBN), a component of the CRL4-CRBN E3 ubiquitin ligase complex. This catalyzes ubiquitination and proteasome-mediated degradation of BTK, and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B-cells that overexpress BTK. 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 B-lymphocyte development, activation, signaling, proliferation and survival. Compared to BTK inhibitors, BGB-16673 may overcome tumor resistance associated with BTK inhibitor-induced resistance mutations, including the BTK C481S mutation, a resistance mutation in the BTK active site in which cysteine is substituted for serine at residue 481." @default.
- NCIT_C182615 NCIT_A7 NCIT_C104142 @default.
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- NCIT_C182615 NCIT_NHC0 "C182615" @default.
- NCIT_C182615 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C182615 NCIT_P107 "BTK Degrader BGB-16673" @default.
- NCIT_C182615 NCIT_P108 "BTK Degrader BGB-16673" @default.
- NCIT_C182615 NCIT_P208 "CL1770940" @default.
- NCIT_C182615 NCIT_P322 "CTRP" @default.
- NCIT_C182615 NCIT_P322 "GDC" @default.
- NCIT_C182615 NCIT_P399 "806209" @default.
- NCIT_C182615 NCIT_R125 NCIT_C17828 @default.
- NCIT_C182615 NCIT_R125 NCIT_C20150 @default.
- NCIT_C182615 NCIT_R125 NCIT_C20480 @default.
- NCIT_C182615 NCIT_R125 NCIT_C40715 @default.
- NCIT_C182615 NCIT_R125 NCIT_C41515 @default.
- NCIT_C182615 NCIT_R125 NCIT_C51037 @default.
- NCIT_C182615 normalizedInformationContent "100" @default.
- NCIT_C182615 referenceCount "1" @default.
- NCIT_C182615 hasExactSynonym "BGB 16673" @default.
- NCIT_C182615 hasExactSynonym "BGB-16673" @default.
- NCIT_C182615 hasExactSynonym "BGB16673" @default.
- NCIT_C182615 hasExactSynonym "BTK Degrader BGB-16673" @default.
- NCIT_C182615 hasExactSynonym "BTK Protein Degradation Agent BGB-16673" @default.
- NCIT_C182615 hasExactSynonym "BTK-Protac BGB-16673" @default.
- NCIT_C182615 inSubset NCIT_C116977 @default.
- NCIT_C182615 inSubset NCIT_C116978 @default.
- NCIT_C182615 inSubset NCIT_C128784 @default.
- NCIT_C182615 inSubset NCIT_C157711 @default.
- NCIT_C182615 inSubset NCIT_C157712 @default.
- NCIT_C182615 inSubset NCIT_C176424 @default.
- NCIT_C182615 type Class @default.
- NCIT_C182615 isDefinedBy ncit.owl @default.
- NCIT_C182615 label "BTK Degrader BGB-16673" @default.
- NCIT_C182615 subClassOf B2ca78872e385c1894c2eed0c6c33bc4c @default.
- NCIT_C182615 subClassOf Bc98a7c8dc254bf215a269150a35d9356 @default.
- NCIT_C182615 subClassOf NCIT_C182615 @default.
- NCIT_C182615 subClassOf NCIT_C1908 @default.
- NCIT_C182615 subClassOf NCIT_C1909 @default.
- NCIT_C182615 subClassOf NCIT_C200055 @default.
- NCIT_C182615 subClassOf NCIT_C2189 @default.
- NCIT_C182615 subClassOf NCIT_C274 @default.