MMAE Delivery Using the
Animals
Antibodies, Monoclonal
/ pharmacology
Antineoplastic Agents
/ pharmacokinetics
Apoptosis
Cell Proliferation
Drug Delivery Systems
Female
Fibrosarcoma
/ drug therapy
Humans
Immunotoxins
/ pharmacokinetics
Male
Mice
Mice, Inbred BALB C
Mice, Nude
Oligopeptides
/ administration & dosage
Peptides, Cyclic
/ pharmacokinetics
Receptor, EphA2
/ genetics
Tissue Distribution
Tumor Cells, Cultured
Xenograft Model Antitumor Assays
Journal
Molecular cancer therapeutics
ISSN: 1538-8514
Titre abrégé: Mol Cancer Ther
Pays: United States
ID NLM: 101132535
Informations de publication
Date de publication:
07 2020
07 2020
Historique:
received:
28
11
2019
revised:
24
02
2020
accepted:
29
04
2020
pubmed:
14
5
2020
medline:
3
6
2021
entrez:
14
5
2020
Statut:
ppublish
Résumé
The EphA2 receptor is found at high levels in tumors and low levels in normal tissue and high EphA2 expression in biopsies is a predictor of poor outcome in patients. Drug discovery groups have therefore sought to develop EphA2-based therapies using small molecule, peptide, and nanoparticle-based approaches (1-3). However, until now only EphA2-targeting antibody-drug conjugates (ADC) have entered clinical development. For example, MEDI-547 is an EphA2-targeting ADC that displayed encouraging antitumor activity in preclinical models and progressed to phase I clinical testing in man. Here we describe the development of BT5528, a bicyclic peptide ("
Identifiants
pubmed: 32398269
pii: 1535-7163.MCT-19-1092
doi: 10.1158/1535-7163.MCT-19-1092
doi:
Substances chimiques
Antibodies, Monoclonal
0
Antineoplastic Agents
0
Immunotoxins
0
Oligopeptides
0
Peptides, Cyclic
0
Receptor, EphA2
EC 2.7.10.1
monomethyl auristatin E
V7I58RC5EJ
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1385-1394Informations de copyright
©2020 American Association for Cancer Research.