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- NCIT_C200199 IAO_0000115 "A small molecule-drug conjugate (SMDC) composed of an integrin alphaVbeta3 binder conjugated, via a cleavable linker, to a camptothecin-based topoisomerase I inhibitor, with potential antineoplastic activity. Upon administration of integrin alphaVbeta3-targeted SMDC VIP236, the integrin alphaVbeta3 binder targets and binds to integrin alphaVbeta3 expressed on tumor cells and tumor vessel endothelial cells. Upon binding and linker cleavage by neutrophil elastase in the tumor microenvironment (TME), the camptothecin-based topoisomerase I inhibitor is released. The topoisomerase I inhibitor inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and generating DNA single- and double-strand breaks, and leading to cell cycle arrest and apoptosis. This inhibits the proliferation of integrin alphaVbeta3-expressing tumor cells, angiogenesis and metastasis. Integrin alphaVbeta3, a cell adhesion and signaling receptor, is overexpressed on the surface of tumor vessel endothelial cells, some tumor cells, and a number of other cell types." @default.
- NCIT_C200199 NCIT_A7 NCIT_C38953 @default.
- NCIT_C200199 NCIT_NHC0 "C200199" @default.
- NCIT_C200199 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C200199 NCIT_P108 "Integrin AlphaVbeta3-targeted Small Molecule-drug Conjugate VIP236" @default.
- NCIT_C200199 NCIT_P322 "GDC" @default.
- NCIT_C200199 NCIT_P399 "812552" @default.
- NCIT_C200199 normalizedInformationContent "100" @default.
- NCIT_C200199 referenceCount "1" @default.
- NCIT_C200199 hasExactSynonym "Integrin AlphaVbeta3-targeted SMDC VIP236" @default.
- NCIT_C200199 hasExactSynonym "Integrin AlphaVbeta3-targeted Small Molecule-drug Conjugate VIP236" @default.
- NCIT_C200199 hasExactSynonym "Integrin AlphaVbeta3-targeted Topoisomerase I Inhibitor VIP236" @default.
- NCIT_C200199 hasExactSynonym "VIP 236" @default.
- NCIT_C200199 hasExactSynonym "VIP-236" @default.
- NCIT_C200199 hasExactSynonym "VIP236" @default.
- NCIT_C200199 inSubset NCIT_C128784 @default.
- NCIT_C200199 inSubset NCIT_C157711 @default.
- NCIT_C200199 inSubset NCIT_C157712 @default.
- NCIT_C200199 inSubset NCIT_C176424 @default.
- NCIT_C200199 type Class @default.
- NCIT_C200199 isDefinedBy ncit.owl @default.
- NCIT_C200199 label "Integrin AlphaVbeta3-targeted Small Molecule-drug Conjugate VIP236" @default.
- NCIT_C200199 subClassOf NCIT_C129824 @default.
- NCIT_C200199 subClassOf NCIT_C129825 @default.
- NCIT_C200199 subClassOf NCIT_C1748 @default.
- NCIT_C200199 subClassOf NCIT_C1904 @default.
- NCIT_C200199 subClassOf NCIT_C1908 @default.
- NCIT_C200199 subClassOf NCIT_C1909 @default.
- NCIT_C200199 subClassOf NCIT_C200199 @default.
- NCIT_C200199 subClassOf NCIT_C2189 @default.
- NCIT_C200199 subClassOf NCIT_C274 @default.
- NCIT_C200199 subClassOf NCIT_C2843 @default.
- NCIT_C200199 subClassOf NCIT_C471 @default.