کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1364605 | 981540 | 2008 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Reprint of “Crystal structure of chemically synthesized HIV-1 protease and a ketomethylene isostere inhibitor based on the p2/NC cleavage site” [Bioorg. Med. Chem. Lett. 18 (2008) 4554-4557]
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Reprint of “Crystal structure of chemically synthesized HIV-1 protease and a ketomethylene isostere inhibitor based on the p2/NC cleavage site” [Bioorg. Med. Chem. Lett. 18 (2008) 4554-4557] Reprint of “Crystal structure of chemically synthesized HIV-1 protease and a ketomethylene isostere inhibitor based on the p2/NC cleavage site” [Bioorg. Med. Chem. Lett. 18 (2008) 4554-4557]](/preview/png/1364605.png)
چکیده انگلیسی
Here we report the X-ray structures of chemically synthesized HIV-1 protease and the inactive [D25N]HIV-1 protease complexed with the ketomethylene isostere inhibitor Ac–Thr–Ile–Nleψ[CO–CH2]Nle–Gln–Arg.amide at 1.4 and 1.8 Å resolution, respectively. In complex with the active enzyme, the keto-group was found to be converted into the hydrated gem-diol, while the structure of the complex with the inactive D25N enzyme revealed an intact keto-group. These data support the general acid–general base mechanism for HIV-1 protease catalysis.
Crystal structure of HIV-1 protease with its ketomethylene isostere inhibitor is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 22, 15 November 2008, Pages 6012–6015
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 22, 15 November 2008, Pages 6012–6015
نویسندگان
Vladimir Yu. Torbeev, Kalyaneswar Mandal, Valentina A. Terechko, Stephen B.H. Kent,