کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2564113 1127604 2011 17 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Dimers and beyond: The functional puzzles of class C GPCRs
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی داروشناسی
پیش نمایش صفحه اول مقاله
Dimers and beyond: The functional puzzles of class C GPCRs
چکیده انگلیسی

Our understanding of G protein-coupled receptor (GPCR) activation has evolved during the last ten years, both at a molecular level thanks to the resolution of several crystal structures, and at a cellular level with the characterization of complexes surrounding the receptor. Class C GPCRs, including receptors for glutamate, γ-aminobutyric acid (GABA), taste compounds, amino acids and Ca2+, have several structural features that make them unique in the GPCR family. First, they possess a large and structurally-defined extracellular domain, which is distal from the transmembrane core and bears the agonist binding site. Second, they form obligatory dimers providing a unique mode of activation compared to GPCRs of other classes. In this article, we aim to provide an overview of the molecular mechanisms of class C GPCR activation as dimeric entities. Furthermore, we discuss the possibility of modulating receptor function through the use of ligands or by association, direct or indirect, with other receptors (GPCRs or not) with the aim to better understand receptor function. Finally, we present the therapeutic scope for the class C GPCRs that highlights the need to fully characterize the functioning of these receptors in their native environment to develop better therapeutic molecules.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pharmacology & Therapeutics - Volume 130, Issue 1, April 2011, Pages 9–25
نویسندگان
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