Crystal structures of HIV-2 protease in complex with inhibitors containing the hydroxyethylamine dipeptide isostere
نویسندگان
چکیده
منابع مشابه
Crystal structures of HIV-2 protease in complex with inhibitors containing the hydroxyethylamine dipeptide isostere.
BACKGROUND The HIV protease is essential for the life cycle of the virus and is an important target for the development of therapeutic treatments against AIDS. The structures of HIV protease in complex with different inhibitors have helped in understanding the interactions between inhibitors and the protease and in the design and optimization of HIV protease inhibitors. RESULTS We report here...
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The crystal structure of HIV-2 protease in complex with a reduced amide inhibitor [BI-LA-398; Phe-Val-Phe-psi (CH2NH)-Leu-Glu-Ile-amide] has been determined at 2.2-A resolution and refined to a crystallographic R factor of 17.6%. The rms deviation from ideality in bond lengths is 0.018 A and in bond angles is 2.8 degrees. The largest structural differences between HIV-1 and HIV-2 proteases are ...
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Inhibition of HIV-1 protease (HIV-PR), the aspartic protease that cleaves specific amide bonds in precursor gag-pol proteins to form the mature proteins needed for production of infectious human immunodeficiency virus (HIV) particles,' is regarded as a promising approach for treating acquired immunodeficiency syndrome (AIDS) and related diseases. Tight-binding inhibitors of HIV-PR have been dis...
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ژورنال
عنوان ژورنال: Structure
سال: 1995
ISSN: 0969-2126
DOI: 10.1016/s0969-2126(01)00133-2