Synthesis and anti-cancer evaluation of folic acid-peptide- paclitaxel conjugates for addressing drug resistance.
Antineoplastic Agents
/ chemical synthesis
Cell Death
/ drug effects
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Dose-Response Relationship, Drug
Drug Resistance, Neoplasm
/ drug effects
Drug Screening Assays, Antitumor
Folic Acid
/ chemistry
Humans
Molecular Structure
Paclitaxel
/ chemistry
Peptides
/ chemistry
Structure-Activity Relationship
Tumor Cells, Cultured
Apoptosis
Conjugates of paclitaxel
Drug resistance
Folate receptor targeted
Lytic peptides
Membranolytic
Paclitaxel
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Jun 2019
01 Jun 2019
Historique:
received:
10
12
2018
revised:
13
03
2019
accepted:
13
03
2019
pubmed:
27
3
2019
medline:
29
5
2019
entrez:
27
3
2019
Statut:
ppublish
Résumé
The drug resistance and the poor water solubility are major limitations of paclitaxel (PTX) of based chemotherapy. To conquer the two problems, targeting folate (FA) receptor PTX-lytic peptides conjugates were synthesized and evaluated. Compared with PTX, FA-P3-PTX and FA-P7-PTX displayed significantly enhanced cell toxicity in many cancer cells, particularly drug resistant cancer cells MCF-7/PTX. FA-P7-PTX possessed stronger effect on cell toxicity (IC
Identifiants
pubmed: 30913525
pii: S0223-5234(19)30249-1
doi: 10.1016/j.ejmech.2019.03.031
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Peptides
0
Folic Acid
935E97BOY8
Paclitaxel
P88XT4IS4D
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
104-115Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.