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Design, synthesis and structure-activity study of shorter hexa peptide analogues as HIV-1 protease inhibitors.

Bioorganic & medicinal chemistry 2007 Oct 22; In press

Link to PubMed abstract

Narendra Babu S SN, Rangappa K KS

Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570006, Karnataka, India.

Inhibition of HIV-1 protease enzyme can render the Human Immunodeficiency Virus (HIV-1) non-infectious in vitro. Previous studies have shown that several shorter peptides were discovered as HIV-1 protease inhibitors. In this context, a series of shorter synthetic hexapeptides, Leu-Leu-Glu-Tyr-Val-Xaa (Xaa=Phe, Met, Tyr and Trp), were designed. The synthesized hexa peptides were screened for their HIV-1 protease inhibition. These peptides showed moderately good HIV-1 protease inhibition when compared to acetyl pepstatin.

Keywords: HIV