Preferred Label : EphA2-targeting Bicycle Toxin Conjugate BT5528;
NCIt synonyms : Bicycle Toxin Conjugate-targeting EphA2 BT5528; Bicyclic Peptide Conjugate BT5528; EphA2-targeting BTC BT5528; EphA2-targeting-MMAE Bicycle Toxin BT5528; Bicycle BT5528; BTC BT5528;
NCIt related terms : BT-5528;
NCIt definition : 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.;
UNII : CIT3DOS0DW;
CAS number : 2648849-70-9;
Molecule name : BT 5528; BT-5528;
NCI Metathesaurus CUI : CL1405523;
Origin ID : C171425;
UMLS CUI : C5417866;
Semantic type(s)
- concept_is_in_subset
- has_target
