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

Peeters, M.C. (2011)

Doctoral Thesis

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.

• S. cerevisiae
• Receptor activation and inactivation
• Mutagenesis
• G protein-coupled receptor
• Extracellular loops
• Constitutive activity
• Adenosine receptors

• All authors: Peeters, M.C.
• Supervisor: IJzerman, A.P.
• Qualification: Doctor (dr.)
• Awarding Institution: Faculty of Science, Leiden University
• Date: 2011-11-17
• Sponsorship: The research described in this thesis was part of the TI-Pharma initiative "The GPCR forum for established targets" (D1-105)