Inhibiting HIV-1 entry: discovery of D-peptide inhibitors that target the gp41 coiled-coil pocket

Article Abstract:

Discovery of D-peptide inhibitors that target the gp41 coiled-coil pocket is discussed relative to interfering with HIV-1 entry to the cell. A peptide, IQN17, was designed to properly present the pocket, prominent on the surface of a central trimeric coiled coil with pg41 previously identified as a potential target for drugs to inhibit the entry. Cyclic D-peptide inhibitors of HIV-1 infection that share a sequence motif were identified. It was shown that conserved residues of the inhibitors make intimate contact with the pocket.

United States, Statistical Data Included, Physiological aspects, Cytochemistry, Cell membranes, Membrane fusion, Antiviral agents

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HIV entry and its inhibition

Article Abstract:

The envelope protein complex of the HIV virus type 1 is responsible in controlling the process of viral entry. It also determines viral tropism and promotes membrane fusion which allows the viral invasion activity. Such envelope protein complex of the HIV-1 functions as a precursor gp160, which is cleaved into two subunits by a cellular convertase. In the HIV entry, complex processes such as multiple protein interactions occur.

Analysis

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Core structure of gp41 from the HIV envelope glycoprotein

Article Abstract:

A study of the core structure of gp41 from the HIV envelope glycoprotein was conducted. The crystal structure is a six-helical bundle which consists of the peptides N36 and C34. The structure is similar to the low-pH-induced conformation of influenza hemagglutinin. Furthermore, the structure suggests avenues for the design/discovery of small-molecule inhibitors of HIV infection.

Glycoproteins, Molecular structure

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