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Inhibition of HIV-1 Pretense by Novel Dipeptide Isosteres Containing 2-Isoxazoline or $\alpha$-Hydroxy Ketomethylene

Kim, Do-Hyung  
  • 초록

    Human immunodeficiency virus type 1 (HIV-1) protease is essential for the replication of the virus and it is therefore an attractive target for antiviral drugs of HIV-1. Several dipeptide isosteres containing 2-isoxazoline or $\alpha$ -hydroxy ketomethylene have been synthesized and their inhibitory effects on the HIV-1 protease examined. The enzymatically active HIV-1 protease was purified to homogeniety from E. coli transformed with a recombinant plasmid (pMAL-pro) containing the entire gene encoding the protease. The purified protease had the substrate specificity with Km value of 9.8 $\mu$ M when an undecapeptide His-Lys-Ala-Arg-Val-Leu-(p-nitro)Phe-Glu-Ala-Nle-Ser-amide was used as a substrate, and the products from the substrate after specific cleavage by HIV-1 protease were analyzed by HPLC. The synthetic compounds containing dipeptide isosteres showed specific inhibitory effects while a dipeptide isostere containing an isoxazoline ring inhibited the HIV-1 protease competitively with Ki value of 500 $\mu$ M. Even if the inhibition effects of HIV-1 protease were not very high, these novel dipeptide isosteres can be used as key structural moieties for developing specific inhibitors of HIV-1 protease.


  • 주제어

    Human Immunodeficiency Virus type 1 (HIV-1) .   HIV-1 protease .   dipeptide isostere .   2-isoxazoline .   $\alpha$-hydroxy ketomethylene.  

 저자의 다른 논문

  • Kim, Byeang-Hyean (3)

    1. 2004 "Modified Triplexes from Oligonucleotides Bridged by Two Cholane-3,24-diol (3α, 5β) Units" Bulletin of the Korean Chemical Society 25 (11): 1619~1620    
    2. 2005 "Sol-gel Transcription of Novel Low-molecular-weight Hydrogel Assembly Based on 2'-Deoxyuridine into the Silica Structure" Bulletin of the Korean Chemical Society 26 (1): 34~35    
    3. 2006 "Chemical Modification of Nucleic Acids toward Functional Nucleic Acid Systems" Bulletin of the Korean Chemical Society 27 (5): 613~630    

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