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- NCIT_C171425 IAO_0000115 "A bicyclic peptide targeting Ephrin receptor A2 (EphA2) and conjugated, through an inert sarcosine spacer chain and a valine-citrulline cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE), an auristatin derivative and a potent inhibitor of microtubule polymerization, with potential antineoplastic activity. Upon administration of the EphA2-targeting bicycle toxin conjugate BT5528, this agent targets and binds to EphA2-expressing tumor cells. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAE binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) involved in mammalian development, is overexpressed by a variety of different cancer cell types. EphA2 expression is associated with poor prognosis." @default.
- NCIT_C171425 NCIT_A32 NCIT_C1909 @default.
- NCIT_C171425 NCIT_A7 NCIT_C26156 @default.
- NCIT_C171425 NCIT_NHC0 "C171425" @default.
- NCIT_C171425 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C171425 NCIT_P107 "EphA2-targeting Bicycle Toxin Conjugate BT5528" @default.
- NCIT_C171425 NCIT_P108 "EphA2-targeting Bicycle Toxin Conjugate BT5528" @default.
- NCIT_C171425 NCIT_P208 "CL1405523" @default.
- NCIT_C171425 NCIT_P322 "CTRP" @default.
- NCIT_C171425 NCIT_P322 "GDC" @default.
- NCIT_C171425 NCIT_P329 "801972" @default.
- NCIT_C171425 NCIT_P330 "801972" @default.
- NCIT_C171425 NCIT_P375 "EphA2-targeting Bicycle Toxin Conjugate BT5528" @default.
- NCIT_C171425 NCIT_P399 "801972" @default.
- NCIT_C171425 normalizedInformationContent "100" @default.
- NCIT_C171425 referenceCount "1" @default.
- NCIT_C171425 hasExactSynonym "BT 5528" @default.
- NCIT_C171425 hasExactSynonym "BT-5528" @default.
- NCIT_C171425 hasExactSynonym "BT5528" @default.
- NCIT_C171425 hasExactSynonym "BTC BT5528" @default.
- NCIT_C171425 hasExactSynonym "Bicycle BT5528" @default.
- NCIT_C171425 hasExactSynonym "Bicycle Toxin Conjugate-targeting EphA2 BT5528" @default.
- NCIT_C171425 hasExactSynonym "Bicyclic Peptide Conjugate BT5528" @default.
- NCIT_C171425 hasExactSynonym "EphA2-targeting BTC BT5528" @default.
- NCIT_C171425 hasExactSynonym "EphA2-targeting Bicycle Toxin Conjugate BT5528" @default.
- NCIT_C171425 hasExactSynonym "EphA2-targeting-MMAE Bicycle Toxin BT5528" @default.
- NCIT_C171425 inSubset NCIT_C116977 @default.
- NCIT_C171425 inSubset NCIT_C116978 @default.
- NCIT_C171425 inSubset NCIT_C128784 @default.
- NCIT_C171425 inSubset NCIT_C157711 @default.
- NCIT_C171425 inSubset NCIT_C157712 @default.
- NCIT_C171425 inSubset NCIT_C176424 @default.
- NCIT_C171425 inSubset NCIT_C177537 @default.
- NCIT_C171425 type Class @default.
- NCIT_C171425 isDefinedBy ncit.owl @default.
- NCIT_C171425 label "EphA2-targeting Bicycle Toxin Conjugate BT5528" @default.
- NCIT_C171425 subClassOf NCIT_C129821 @default.
- NCIT_C171425 subClassOf NCIT_C129823 @default.
- NCIT_C171425 subClassOf NCIT_C1512 @default.
- NCIT_C171425 subClassOf NCIT_C171425 @default.
- NCIT_C171425 subClassOf NCIT_C1908 @default.
- NCIT_C171425 subClassOf NCIT_C1909 @default.
- NCIT_C171425 subClassOf NCIT_C274 @default.
- NCIT_C171425 subClassOf NCIT_C307 @default.
- NCIT_C171425 subClassOf NCIT_C308 @default.