کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1357744 | 981275 | 2015 | 15 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthetic, structural mimetics of the β-hairpin flap of HIV-1 protease inhibit enzyme function
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthetic, structural mimetics of the β-hairpin flap of HIV-1 protease inhibit enzyme function Synthetic, structural mimetics of the β-hairpin flap of HIV-1 protease inhibit enzyme function](/preview/png/1357744.png)
چکیده انگلیسی
Small-molecule mimetics of the β-hairpin flap of HIV-1 protease (HIV-1 PR) were designed based on a 1,4-benzodiazepine scaffold as a strategy to interfere with the flap–flap protein–protein interaction, which functions as a gated mechanism to control access to the active site. Michaelis–Menten kinetics suggested our small-molecules are competitive inhibitors, which indicates the mode of inhibition is through binding the active site or sterically blocking access to the active site and preventing flap closure, as designed. More generally, a new bioactive scaffold for HIV-1PR inhibition has been discovered, with the most potent compound inhibiting the protease with a modest Ki of 11 μM.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 23, Issue 21, 1 November 2015, Pages 7095–7109
Journal: Bioorganic & Medicinal Chemistry - Volume 23, Issue 21, 1 November 2015, Pages 7095–7109
نویسندگان
Jay Chauhan, Shen-En Chen, Katherine J. Fenstermacher, Aurash Naser-Tavakolian, Tali Reingewertz, Rosene Salmo, Christian Lee, Emori Williams, Mithun Raje, Eric Sundberg, Jeffrey J. DeStefano, Ernesto Freire, Steven Fletcher,