کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8466003 | 1549479 | 2014 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Functional and structural perspectives on allosteric modulation of GPCRs
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موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
بیولوژی سلول
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چکیده انگلیسی
Traditionally, optimizing lead molecule interactions with the orthosteric site has been viewed as the best means for attaining selectivity at G protein-coupled receptors (GPCRs), but GPCRs possess spatially distinct allosteric sites that can also modulate receptor activity. Allosteric sites offer a greater potential for receptor subtype selectivity, the ability to fine-tune physiological responses, and the ability to engender signal pathway bias. The detection and quantification of allosteric drug candidates remain an ongoing challenge, but the development of novel analytical approaches for quantifying allostery is enriching structure-activity and structure-function studies of the phenomenon. Very recent breakthroughs in both structural and computational biology of GPCRs are also beginning to unravel the mechanistic basis of allosteric modulation at the molecular level.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Current Opinion in Cell Biology - Volume 27, April 2014, Pages 94-101
Journal: Current Opinion in Cell Biology - Volume 27, April 2014, Pages 94-101
نویسندگان
Christopher J Langmead, Arthur Christopoulos,