Nuzefatide pevedotin
Term · Oncology and biomedicine · MLC-T-ONC-015560
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, nuzefatide pevedotin 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.
| Identifier | MLC-T-ONC-015560 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | bicycle BT5528; bicycle toxin conjugate-targeting EphA2 BT5528; bicyclic peptide conjugate BT5528; BTC BT5528; EphA2-targeting Bicycle Toxin Conjugate BT5528; EphA2-targeting BTC BT5528; EphA2-targeting-MMAE bicycle toxin BT5528 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-015560",
"term": "Nuzefatide pevedotin",
"field": "Oncology and biomedicine",
"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, nuzefatide pevedotin 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.",
"synonyms": [
"bicycle BT5528",
"bicycle toxin conjugate-targeting EphA2 BT5528",
"bicyclic peptide conjugate BT5528",
"BTC BT5528",
"EphA2-targeting Bicycle Toxin Conjugate BT5528",
"EphA2-targeting BTC BT5528",
"EphA2-targeting-MMAE bicycle toxin BT5528"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/nuzefatide-pevedotin/"
}
Record 12,032 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.