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- NCIT_C183151 IAO_0000115 "An orally bioavailable androgen receptor (AR)-targeted protein degrader, composed of an AR ligand attached to an E3 ligase recognition moiety and utilizing the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Upon oral administration, AR degrader ARV-766 targets and binds to the AR ligand binding domain on the AR. E3 ligase is then recruited to the AR by the E3 ligase recognition moiety of ARV-766 and the AR is tagged by ubiquitin. This causes ubiquitination and degradation of AR by the proteasome, and prevents the expression of AR target genes and halts AR-mediated signaling. This inhibits the proliferation of AR-overexpressing tumor cells. In addition, the degradation of the AR releases ARV-766, allowing it to bind to additional AR. AR plays a key role in the proliferation of castration-resistant prostate cancer cells (CRPC). ARV-766 may degrade resistance-driving point mutations of AR, including the L702H mutation associated with treatments including abiraterone." @default.
- NCIT_C183151 NCIT_A7 NCIT_C17063 @default.
- NCIT_C183151 NCIT_NHC0 "C183151" @default.
- NCIT_C183151 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C183151 NCIT_P107 "Androgen Receptor Degrader ARV-766" @default.
- NCIT_C183151 NCIT_P108 "Androgen Receptor Degrader ARV-766" @default.
- NCIT_C183151 NCIT_P208 "CL1771378" @default.
- NCIT_C183151 NCIT_P322 "CTRP" @default.
- NCIT_C183151 NCIT_P322 "GDC" @default.
- NCIT_C183151 NCIT_P399 "807024" @default.
- NCIT_C183151 normalizedInformationContent "100" @default.
- NCIT_C183151 referenceCount "1" @default.
- NCIT_C183151 hasExactSynonym "AR Degrader ARV-766" @default.
- NCIT_C183151 hasExactSynonym "AR PROTAC ARV-766" @default.
- NCIT_C183151 hasExactSynonym "AR-targeted PROTAC Protein Degrader ARV-766" @default.
- NCIT_C183151 hasExactSynonym "ARV 766" @default.
- NCIT_C183151 hasExactSynonym "ARV-766" @default.
- NCIT_C183151 hasExactSynonym "ARV766" @default.
- NCIT_C183151 hasExactSynonym "Androgen Receptor Degrader ARV-766" @default.
- NCIT_C183151 hasExactSynonym "Androgen Receptor PROTAC Degrader ARV-766" @default.
- NCIT_C183151 inSubset NCIT_C116977 @default.
- NCIT_C183151 inSubset NCIT_C116978 @default.
- NCIT_C183151 inSubset NCIT_C128784 @default.
- NCIT_C183151 inSubset NCIT_C157711 @default.
- NCIT_C183151 inSubset NCIT_C157712 @default.
- NCIT_C183151 inSubset NCIT_C176424 @default.
- NCIT_C183151 type Class @default.
- NCIT_C183151 isDefinedBy ncit.owl @default.
- NCIT_C183151 label "Androgen Receptor Degrader ARV-766" @default.
- NCIT_C183151 subClassOf NCIT_C146993 @default.
- NCIT_C183151 subClassOf NCIT_C147908 @default.
- NCIT_C183151 subClassOf NCIT_C163758 @default.
- NCIT_C183151 subClassOf NCIT_C183151 @default.
- NCIT_C183151 subClassOf NCIT_C1908 @default.
- NCIT_C183151 subClassOf NCIT_C1909 @default.
- NCIT_C183151 subClassOf NCIT_C242 @default.
- NCIT_C183151 subClassOf NCIT_C274 @default.
- NCIT_C183151 subClassOf NCIT_C547 @default.