کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1938224 1050736 2007 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of potent inhibitors of the coxsackievirus 3C protease
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
پیش نمایش صفحه اول مقاله
Development of potent inhibitors of the coxsackievirus 3C protease
چکیده انگلیسی

Coxsackievirus B3 (CVB3) 3C protease (3CP) plays essential roles in the viral replication cycle, and therefore, provides an attractive therapeutic target for treatment of human diseases caused by CVB3 infection. CVB3 3CP and human rhinovirus (HRV) 3CP have a high degree of amino acid sequence similarity. Comparative modeling of these two 3CPs revealed one prominent distinction; an Asn residue delineating the S2′ pocket in HRV 3CP is replaced by a Tyr residue in CVB3 3CP. AG7088, a potent inhibitor of HRV 3CP, was modified by substitution of the ethyl group at the P2′ position with various hydrophobic aromatic rings that are predicted to interact preferentially with the Tyr residue in the S2′ pocket of CVB3 3CP. The resulting derivatives showed dramatically increased inhibitory activities against CVB3 3CP. In addition, one of the derivatives effectively inhibited the CVB3 proliferation in vitro.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 358, Issue 1, 22 June 2007, Pages 7–11
نویسندگان
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