【摘 要】
：
The continuing emergence of resistant strains of the human immunodeficiency virus type 1 (HIV-1) makes the search for new anti-HIV-1 agents very urgent One of the most attractive target for selective
【机 构】
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Istituto Pasteur-Fondazione Cenci Bolognetti,Dipartimento di Studi Farmaceutici,P.le Aldo Moro 5, 00
【出 处】
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2006中国天津世界艾滋病日科技会议
论文部分内容阅读
The continuing emergence of resistant strains of the human immunodeficiency virus type 1 (HIV-1) makes the search for new anti-HIV-1 agents very urgent One of the most attractive target for selective therapeutic intervention is integrase (IN) enzyme,which catalyzes the insertion into the host genome of viral DNA derived by reverse transcription of RNA.Integration occurs via a multi-step sequence of reactions,including i) cleavage of a dinucleotide pair from the 3-end of the viral DNA (termed "3-processing",3’-P),ii) insertion of the resulting shortened strands into the host-cell chromosome (termed "strand transfer",ST),iii) removal of the two unpaired nucleotides at the 5-end of the viral DNA and gap-filling process.In the past several years,numerous compounds with different structural features have been reported as IN inhibitors,1 of which the most important class is typified by an aryl β-diketo acid motif (DKAs).
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