The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel Example

Seven transmembrane G protein—coupled receptors are among the most common in biology and they transduce cellular signals from a plethora of hormones. As well as their own well-characterized signaling pathways, they can also transactivate tyrosine kinase growth factor receptors to greatly expand thei...

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Main Authors: Peter J. Little, Micah L. Burch, Sefaa Al-aryahi, Wenhua Zheng
Format: Article
Language:English
Published: Wiley 2011-01-01
Series:The Scientific World Journal
Online Access:http://dx.doi.org/10.1100/tsw.2011.75
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author Peter J. Little
Micah L. Burch
Sefaa Al-aryahi
Wenhua Zheng
author_facet Peter J. Little
Micah L. Burch
Sefaa Al-aryahi
Wenhua Zheng
author_sort Peter J. Little
collection DOAJ
description Seven transmembrane G protein—coupled receptors are among the most common in biology and they transduce cellular signals from a plethora of hormones. As well as their own well-characterized signaling pathways, they can also transactivate tyrosine kinase growth factor receptors to greatly expand their own cellular repertoire of responses. Recent data in vascular smooth muscle cells have expanded the breadth of transactivation to include serine/threonine kinase receptors, specifically the receptor for transforming growth factor beta (TGF-β). Stimulation with endothelin and thrombin leads to the rapid formation of C-terminal phosphorylated Smad2, which is the immediate product of activation of the TGF-β receptor. Additionally, it appears that no definition of transactivation based on mechanism is available, so we have provided a definition involving temporal aspects and the absence of de novo protein synthesis. The phenomenon of transactivation is an important biochemical mechanism and potential drug target in multiple diseases.
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spelling doaj-art-9a4e074e3f0547318a607f931f7d7e902025-08-20T03:36:54ZengWileyThe Scientific World Journal1537-744X2011-01-011170971410.1100/tsw.2011.75The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel ExamplePeter J. Little0Micah L. Burch1Sefaa Al-aryahi2Wenhua Zheng3Discipline of Pharmacy, School of Medical Sciences, RMIT University, Melbourne, Victoria, AustraliaDiabetes and Cell Biology Laboratory, BakerIDI Heart and Diabetes Institute, Melbourne, Victoria, AustraliaDiabetes Complications Group, Health Innovations Research Institute, RMIT University, Melbourne, Victoria, AustraliaNeuropharmacology, School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, Guangdong, ChinaSeven transmembrane G protein—coupled receptors are among the most common in biology and they transduce cellular signals from a plethora of hormones. As well as their own well-characterized signaling pathways, they can also transactivate tyrosine kinase growth factor receptors to greatly expand their own cellular repertoire of responses. Recent data in vascular smooth muscle cells have expanded the breadth of transactivation to include serine/threonine kinase receptors, specifically the receptor for transforming growth factor beta (TGF-β). Stimulation with endothelin and thrombin leads to the rapid formation of C-terminal phosphorylated Smad2, which is the immediate product of activation of the TGF-β receptor. Additionally, it appears that no definition of transactivation based on mechanism is available, so we have provided a definition involving temporal aspects and the absence of de novo protein synthesis. The phenomenon of transactivation is an important biochemical mechanism and potential drug target in multiple diseases.http://dx.doi.org/10.1100/tsw.2011.75
spellingShingle Peter J. Little
Micah L. Burch
Sefaa Al-aryahi
Wenhua Zheng
The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel Example
The Scientific World Journal
title The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel Example
title_full The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel Example
title_fullStr The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel Example
title_full_unstemmed The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel Example
title_short The Paradigm of G Protein Receptor Transactivation: A Mechanistic Definition and Novel Example
title_sort paradigm of g protein receptor transactivation a mechanistic definition and novel example
url http://dx.doi.org/10.1100/tsw.2011.75
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