کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10769694 | 1050824 | 2005 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease](/preview/png/10769694.png)
چکیده انگلیسی
SARS-CoV 3CL protease is essential for viral protein processing and is regarded as a good drug target to prevent SARS-CoV replication. In the present study, we established a high-throughput FRET technique for screening for anti-SARS-CoV 3CL protease drugs. Of a thousand existing drugs examined, hexachlorophene was identified as the most potent in inhibiting SARS-CoV 3CL protease. Further characterization showed that it was effective at micromolar concentrations (Ki = 4 μM). The binding mode was competitive, and the inhibitory effect was dependent on preincubation time. Two other drugs, triclosan and nelfinavir, were about 10 times less potent. The structure-based search and biological evaluation of various hexachlorophene analogues were described. These analogues gave optimal inhibitory activity against SARS-CoV 3CL protease with IC50 values ranging from 7.6 to 84.5 μM. Optimization of hexachlorophene analogues was shown to provide several active 3CL protease inhibitors that function as potential anti-SARS agents.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 333, Issue 1, 22 July 2005, Pages 194-199
Journal: Biochemical and Biophysical Research Communications - Volume 333, Issue 1, 22 July 2005, Pages 194-199
نویسندگان
Yu-Chih Liu, Vicky Huang, Ti-Chun Chao, Chwan-Deng Hsiao, Atsui Lin, Ming-Fu Chang, Lu-Ping Chow,