The role of blood cell membrane lipids on the mode of action of HIV-1 fusion inhibitor sifuvirtide.
Biochem Biophys Res Commun
; 403(3-4): 270-4, 2010 Dec 17.
Article
em En
| MEDLINE
| ID: mdl-21075080
ABSTRACT
Sifuvirtide is a gp41 based peptide that inhibits HIV-1 fusion with the host cells and is currently under clinical trials. Previous studies showed that sifuvirtide partitions preferably to saturated phosphatidylcholine lipid membranes, instead of fluid-phase lipid vesicles. We extended the study to the interaction of the peptide with circulating blood cells, by using the dipole potential sensitive probe di-8-ANEPPS. Sifuvirtide decreased the dipole potential of erythrocyte and lymphocyte membranes in a concentration dependent manner, demonstrating its interaction. Also, the lipid selectivity of the peptide towards more rigid phosphatidylcholines was confirmed based on the dipole potential variations. Overall, the interaction of the peptide with the cell membranes is a contribution of different lipid preferences that presumably directs the peptide towards raft-like domains where the receptors are located, facilitating the reach of the peptide to its molecular target, the gp41 in its pre-fusion conformation.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
HIV-1
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Inibidores da Fusão de HIV
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Membrana Eritrocítica
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Internalização do Vírus
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Lipídeos de Membrana
Limite:
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article