Synthesis and biological studies of c(RGDyK) conjugates of cucurbitacins.
RGD peptide
angiogenesis
anticancer therapy
cucurbitacins
integrin avβ3
targeted drug delivery
Journal
Future medicinal chemistry
ISSN: 1756-8927
Titre abrégé: Future Med Chem
Pays: England
ID NLM: 101511162
Informations de publication
Date de publication:
05 2021
05 2021
Historique:
pubmed:
17
4
2021
medline:
21
10
2021
entrez:
16
4
2021
Statut:
ppublish
Résumé
Cucurbitacins (CUCUs) are triterpenoids known to display potent cytotoxic effects; however, their clinical application is limited due to poor pharmacokinetics and systemic toxicity. This work focuses on the development of c(RGDyK)-CUCU conjugates for the selective delivery of CUCUs to integrin-overexpressing cancer cells. The activity of the conjugates against various cancer cells was studied. They exhibited a mild cytostatic effect to six cancer cell lines and a cytotoxic effect against integrin-overexpressing MCF-7 and A549 cells. Their chemical and metabolic stability was extensively studied using LC-MS analysis. The conjugates maintained high affinity for α
Identifiants
pubmed: 33858195
doi: 10.4155/fmc-2020-0309
doi:
Substances chimiques
Antineoplastic Agents
0
Oligopeptides
0
Cucurbitacins
60137-06-6
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM