کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10870885 1074025 2013 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
First generation inhibitors of the adenovirus proteinase
ترجمه فارسی عنوان
مهار کننده نسل اول پروتئیناز آدنویروس
موضوعات مرتبط
علوم زیستی و بیوفناوری علوم کشاورزی و بیولوژیک دانش گیاه شناسی
چکیده انگلیسی
As there are more than 50 adenovirus serotypes, the likelihood of developing an effective vaccine is low. Here we describe inhibitors of the adenovirus proteinase (AVP) with the ultimate objective of developing anti-adenovirus agents. Inhibitors were identified via structure-based drug design using as druggable sites the active site and a conserved cofactor pocket in the crystal structures of AVP. A lead compound was identified that had an IC50 of 18 μM. One of eight structural derivatives of the lead compound had an IC50 of 140 nM against AVP and an IC50 of 490 nM against the AVP with its cofactor bound.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: FEBS Letters - Volume 587, Issue 15, 2 August 2013, Pages 2332-2339
نویسندگان
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