کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2049941 1074147 2007 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Manifold active-state conformations in GPCRs: Agonist-activated constitutively active mutant AT1 receptor preferentially couples to Gq compared to the wild-type AT1 receptor
موضوعات مرتبط
علوم زیستی و بیوفناوری علوم کشاورزی و بیولوژیک دانش گیاه شناسی
پیش نمایش صفحه اول مقاله
Manifold active-state conformations in GPCRs: Agonist-activated constitutively active mutant AT1 receptor preferentially couples to Gq compared to the wild-type AT1 receptor
چکیده انگلیسی

The angiotensin II type I (AT1) receptor mediates regulation of blood pressure and water-electrolyte balance by Ang II. Substitution of Gly for Asn111 of the AT1 receptor constitutively activates the receptor leading to Gq-coupled IP3 production independent of Ang II binding. The Ang II-activated conformation of the AT1N111G receptor was proposed to be similar to that of the wild-type AT1 receptor, although, various aspects of the Ang II-induced conformation of this constitutively active mutant receptor have not been systematically studied. Here, we provide evidence that the conformation of the active state of the wild-type and the constitutively active AT1 receptors are different. Upon Ang II binding an activated conformation of the wild-type AT1 receptor activates G protein and recruits β-arrestin. In contrast, the agonist-bound AT1N111G mutant receptor preferentially couples to Gq and is inadequate in β-arrestin recruitment.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: FEBS Letters - Volume 581, Issue 13, 29 May 2007, Pages 2517–2522
نویسندگان
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