کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2530032 1558135 2010 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Allostery and population shift in drug discovery
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
Allostery and population shift in drug discovery
چکیده انگلیسی

Proteins can exist in a large number of conformations around their native states that can be characterized by an energy landscape. The landscape illustrates individual valleys, which are the conformational substates. From the functional standpoint, there are two key points: first, all functionally relevant substates pre-exist; and second, the landscape is dynamic and the relative populations of the substates will change following allosteric events. Allosteric events perturb the structure, and the energetic strain propagates and shifts the population. This can lead to changes in the shapes and properties of target binding sites. Here we present an overview of dynamic conformational ensembles focusing on allosteric events in signaling. We propose that combining equilibrium fluctuation concepts with genomic screens could help drug discovery.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Current Opinion in Pharmacology - Volume 10, Issue 6, December 2010, Pages 715–722
نویسندگان
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