Biophysical Dissection of Isolated GPCRs: The Adenosine A2A Receptor under the Bistouries
Abstract
:1. Foreword: Biophysical Approaches to Answer Which Questions?
2. Background and Introduction
3. Mass Production of A2A Receptors
3.1. Expression Systems
3.2. Molecular Constructs
4. Extraction and Purification
5. Isolation in Lipid Nanoparticles
6. Quality Controls on Isolated Receptors
7. Functionality of the Isolated A2A
7.1. Ligand Binding
7.1.1. Radioactive Ligand Binding
7.1.2. Surface Plasmon Resonance
7.1.3. Calorimetry
7.1.4. Receptor Fluorescent Labeling
7.1.5. Ligand-Based NMR
7.1.6. Native Mass Spectrometry
7.2. Activity
7.2.1. G-Protein Coupling and Arrestin Recruitment
7.2.2. Functionality of Isolated Receptors: Activity of Receptor Dimers and Oligomers
8. Structure of A2A
8.1. Structural Mass Spectrometry Approaches
8.2. X-ray Crystallography of GPCRs: Uncovering Conserved Activation Mechanisms Using A2A as a Model
8.3. Cryo-Electron Microscopy
8.4. NMR Approaches
8.5. Future Trends for GPCR Structure Studies
8.5.1. Cryo-Electron Tomography
8.5.2. Structural Flexibility of GPCR Investigated Using Single Molecule Fluorescence and Atomic Force Microscopy
9. Pharmacology of the Isolated Protein A2A
9.1. Background
9.2. Background on Ligand Chemistry
9.2.1. A2A Receptor Agonists
9.2.2. A2A Receptor Antagonists
9.3. Allosteric Modulators
9.4. Fluorescent Ligands
9.5. Structure-Based Ligand Discovery for A2A
9.6. Fragment-Based Ligand Discovery for A2A
9.7. Mass Spectrometry-Based Ligand Screening
10. Concluding Remarks and Perspectives
Funding
Conflicts of Interest
Abbreviations
References
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Banères, J.-L.; Botzanowski, T.; Boutin, J.A.; Calamini, B.; Castel, J.; Catoire, L.J.; Cianférani, S.; Demesmay, C.; Ferguson, G.; Ferry, G.; et al. Biophysical Dissection of Isolated GPCRs: The Adenosine A2A Receptor under the Bistouries. Receptors 2023, 2, 47-92. https://doi.org/10.3390/receptors2010004
Banères J-L, Botzanowski T, Boutin JA, Calamini B, Castel J, Catoire LJ, Cianférani S, Demesmay C, Ferguson G, Ferry G, et al. Biophysical Dissection of Isolated GPCRs: The Adenosine A2A Receptor under the Bistouries. Receptors. 2023; 2(1):47-92. https://doi.org/10.3390/receptors2010004
Chicago/Turabian StyleBanères, Jean-Louis, Thomas Botzanowski, Jean A. Boutin, Barbara Calamini, Jérôme Castel, Laurent J. Catoire, Sarah Cianférani, Claire Demesmay, Gavin Ferguson, Gilles Ferry, and et al. 2023. "Biophysical Dissection of Isolated GPCRs: The Adenosine A2A Receptor under the Bistouries" Receptors 2, no. 1: 47-92. https://doi.org/10.3390/receptors2010004