Activation of G protein-coupled receptors : the role of extracellular loops in adenosine receptors

Leiden Repository

Activation of G protein-coupled receptors : the role of extracellular loops in adenosine receptors

Title: Activation of G protein-coupled receptors : the role of extracellular loops in adenosine receptors
Author: Peeters, Miriam Cornelia
Publisher: Division of Medicinal Chemistry, Leiden/Amsterdam Center for Drug Research (LACDR), Leiden University
Issue Date: 2011-11-17
Keywords: Adenosine receptors
Constitutive activity
Extracellular loops
G protein-coupled receptor
Mutagenesis
Receptor activation and inactivation
S. cerevisiae
Abstract: The research described in this thesis has provided new insights in the activation mechanism of class A GPCRs and in particular of adenosine receptors. By a variety of mutagenesis approaches and the use of a robust yeast reporter gene system, we identified several regions and amino acid positions that contribute to both agonist responses and constitutive activity of the human adenosine A1 receptor and the human adenosine A2B receptor. These results reveal new and surprising roles of the extracellular loops in the activation mechanism, greatly contributing to our notion of receptor activation.
Description: Promotor: A.P. IJzerman
With summary in Dutch
Faculty: Faculteit der Wiskunde en Natuurwetenschappen
Citation: Peeters, M.C., 2011, Doctoral thesis, Leiden University
Sponsor: The research described in this thesis was part of the TI-Pharma initiative "The GPCR forum for established targets" (D1-105)
Handle: http://hdl.handle.net/1887/18092
 

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