Dual Gene Delivery Reagents From Antiproliferative Alkylphospholipids for Combined Antitumor Therapy.
alkylphospholipid
chemotherapy
erufosine
gene therapy
hemolytic toxicity
miltefosine
perifosine
prodrug
Journal
Frontiers in chemistry
ISSN: 2296-2646
Titre abrégé: Front Chem
Pays: Switzerland
ID NLM: 101627988
Informations de publication
Date de publication:
2020
2020
Historique:
received:
08
07
2020
accepted:
31
08
2020
entrez:
2
11
2020
pubmed:
3
11
2020
medline:
3
11
2020
Statut:
epublish
Résumé
Alkylphospholipids (APLs) have elicited great interest as antitumor agents due to their unique mode of action on cell membranes. However, their clinical applications have been limited so far by high hemolytic activity. Recently, cationic prodrugs of erufosine, a most promising APL, have been shown to mediate efficient intracellular gene delivery, while preserving the antiproliferative properties of the parent APL. Here, cationic prodrugs of the two APLs that are currently used in the clinic, miltefosine, and perifosine, are investigated and compared to the erufosine prodrugs. Their synthesis, stability, gene delivery and self-assembly properties, and hemolytic activity are discussed in detail. Finally, the potential of the pro-miltefosine and pro-perifosine compounds
Identifiants
pubmed: 33134279
doi: 10.3389/fchem.2020.581260
pmc: PMC7566913
doi:
Types de publication
Journal Article
Langues
eng
Pagination
581260Informations de copyright
Copyright © 2020 Gaillard, Remy, Pons and Lebeau.
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