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Biochem Biophys Res Commun. 2010 Dec 17;403(3-4):270-4. doi: 10.1016/j.bbrc.2010.11.013. Epub 2010 Nov 12.

The role of blood cell membrane lipids on the mode of action of HIV-1 fusion inhibitor sifuvirtide.

Author information

1
Instituto de Medicina Molecular, Faculdade de Medicina da Universidade de Lisbon, Av. Prof. Egas Moniz, 1649-028 Lisboa, Portugal.

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.

PMID:
21075080
DOI:
10.1016/j.bbrc.2010.11.013
[Indexed for MEDLINE]

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