Abstract
Corticotropin releasing factor (CRF) receptors belong to the secretin family of G proteincoupled receptors (GPCRs) and are responsible for initiating endocrine stress responses and mediating anxiety related behaviors upon activation via stressors. The main binding site for the CRF ligands is the first extracellular domain (ECD) of the receptors. Several structures of ligand-free and ligand-bound ECDs were recently determined either by nuclear magnetic resonance (NMR) spectroscopy or X-ray crystallography. They reveal how the ligands bind through both hydrophobic and hydrophilic interactions to the ECDs, which is highly dynamic in the absence of ligands. It is the purpose of this review to discuss these structures with a particular focus on ligand-receptor interaction.
Keywords: GPCR, CRF receptors, first extracellular domain, structure, ligand binding, ECD.
Graphical Abstract
Current Molecular Pharmacology
Title:Structures of the First Extracellular Domain of CRF Receptors
Volume: 10
Author(s): Viviane Zelenay, Marilyn Perrin and Roland Riek*
Affiliation:
- Department of Physical Chemistry, ETH Zurich, Vladimir-Prelog-Weg 2, 8093 Zurich,Switzerland
Keywords: GPCR, CRF receptors, first extracellular domain, structure, ligand binding, ECD.
Abstract: Corticotropin releasing factor (CRF) receptors belong to the secretin family of G proteincoupled receptors (GPCRs) and are responsible for initiating endocrine stress responses and mediating anxiety related behaviors upon activation via stressors. The main binding site for the CRF ligands is the first extracellular domain (ECD) of the receptors. Several structures of ligand-free and ligand-bound ECDs were recently determined either by nuclear magnetic resonance (NMR) spectroscopy or X-ray crystallography. They reveal how the ligands bind through both hydrophobic and hydrophilic interactions to the ECDs, which is highly dynamic in the absence of ligands. It is the purpose of this review to discuss these structures with a particular focus on ligand-receptor interaction.
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Cite this article as:
Zelenay Viviane, Perrin Marilyn and Riek Roland*, Structures of the First Extracellular Domain of CRF Receptors, Current Molecular Pharmacology 2017; 10 (4) . https://dx.doi.org/10.2174/1874467210666170110120301
DOI https://dx.doi.org/10.2174/1874467210666170110120301 |
Print ISSN 1874-4672 |
Publisher Name Bentham Science Publisher |
Online ISSN 1874-4702 |
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