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  • Title: Inhibition of human immunodeficiency virus type-1 reverse transcriptase by a novel peptide derived from the viral integrase.
    Author: Oz Gleenberg I, Herschhorn A, Goldgur Y, Hizi A.
    Journal: Arch Biochem Biophys; 2007 Feb 15; 458(2):202-12. PubMed ID: 17257575.
    Abstract:
    Previous studies show that the reverse transcriptase (RT) of human immunodeficiency virus type-1 (HIV-1) and RT-derived peptides interact with and inhibit the viral integrase (IN). In the present study, we have performed the complementary study by screening a complete library of HIV-1 IN-derived peptides for their effects on the RT. We have identified a 20-residues long peptide, derived from the IN (residues 46-65) that binds the RT and inhibits its DNA-polymerase activities (without affecting the ribonuclease-H activity). The full 20-residues sequence is required for maximal inhibition. This inhibition is non-competitive and probably results from obstructing the formation of RT-DNA complexes by the peptide. The data and the molecular docking model presented suggest that this inhibition is probably caused by a steric hindrance or conformational changes of the RT. These results can facilitate the development of novel and specific peptide-based HIV-1 RT inhibitors that might help in the fight against AIDS.
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