A Peptidic Thymidylate-Synthase Inhibitor Loaded on Pegylated Liposomes Enhances the Antitumour Effect of Chemotherapy Drugs in Human Ovarian Cancer Cells.
Antimetabolites, Antineoplastic
/ pharmacology
Apoptosis
Cell Proliferation
Drug Resistance, Neoplasm
/ drug effects
Drug Therapy, Combination
Enzyme Inhibitors
/ pharmacology
Female
Fluorouracil
/ pharmacology
Humans
Liposomes
/ chemistry
Ovarian Neoplasms
/ drug therapy
Peptide Fragments
/ pharmacology
Polyethylene Glycols
/ chemistry
Quinazolines
/ pharmacology
Thiophenes
/ pharmacology
Thymidylate Synthase
/ antagonists & inhibitors
Tumor Cells, Cultured
5-fluorouracil
drug-resistance
human thymidylate synthase peptidic-inhibitors
ovarian cancer
pH-sensitive PEGylated liposomes
raltitrexed
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
23 Jun 2020
23 Jun 2020
Historique:
received:
30
05
2020
revised:
20
06
2020
accepted:
20
06
2020
entrez:
27
6
2020
pubmed:
27
6
2020
medline:
23
3
2021
Statut:
epublish
Résumé
There is currently no effective long-term treatment for ovarian cancer (OC) resistant to poly-chemotherapy regimens based on platinum drugs. Preclinical and clinical studies have demonstrated a strong association between development of Pt-drug resistance and increased thymidylate synthase (hTS) expression, and the consequent cross-resistance to the hTS inhibitors 5-fluorouracil (5-FU) and raltitrexed (RTX). In the present work, we propose a new tool to combat drug resistance. We propose to treat OC cell lines, both Pt-sensitive and -resistant, with dual combinations of one of the four chemotherapeutic agents that are widely used in the clinic, and the new peptide, hTS inhibitor, [D-Gln
Identifiants
pubmed: 32585842
pii: ijms21124452
doi: 10.3390/ijms21124452
pmc: PMC7352236
pii:
doi:
Substances chimiques
Antimetabolites, Antineoplastic
0
Enzyme Inhibitors
0
Liposomes
0
Peptide Fragments
0
Quinazolines
0
Thiophenes
0
Polyethylene Glycols
3WJQ0SDW1A
Thymidylate Synthase
EC 2.1.1.45
raltitrexed
FCB9EGG971
Fluorouracil
U3P01618RT
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Associazione Italiana per la Ricerca sul Cancro
ID : IG 10474
Organisme : Associazione Italiana per la Ricerca sul Cancro
ID : IG 16977
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