Design, synthesis and bioactivity investigation of peptide-camptothecin conjugates as anticancer agents with a potential to overcome drug resistance.
Anticancer
Camptothecin (CPT)
Drug resistance
Peptide-drug conjugates
Selectivity
Journal
International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127
Informations de publication
Date de publication:
15 Oct 2023
15 Oct 2023
Historique:
received:
20
07
2023
revised:
22
08
2023
accepted:
08
09
2023
pubmed:
12
9
2023
medline:
12
9
2023
entrez:
11
9
2023
Statut:
ppublish
Résumé
Camptothecin (CPT) is a natural plant alkaloid from Camptotheca that exhibits a potent anticancer activity. However, its continued utilization is hindered by drawbacks such as low water solubility and restricted tumor selectivity. Cationic anticancer peptides (CAPs) are generally soluble in water, and exhibit favorable selectivity against malignant cells. In previous study, we have reported a CAP termed KM8-Aib present conspicuous selective anticancer effect. Thus, it is postulated conjugating KM8-Aib with CPT might be a plausible approach to improve the defects of CPT. A series of peptide-CPT conjugates were synthesized and subjected to biological evaluation. Among these compounds, Kb-CC07 displayed the highest selective activity against a set of cancer cell lines including drug-resistant cells, showing the IC
Identifiants
pubmed: 37696345
pii: S0378-5173(23)00823-2
doi: 10.1016/j.ijpharm.2023.123402
pii:
doi:
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
123402Informations de copyright
Copyright © 2023. Published by Elsevier B.V.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.