Rapid CommunicationMinireview—Exploring the biology of GPCRs: from in vitro to in vivo
Ligand Residence Time at G-protein–Coupled Receptors—Why We Should Take Our Time To Study It
C. Hoffmann, M. Castro, A. Rinken, R. Leurs, S. J. Hill and H. F. Vischer
Molecular Pharmacology September 2015, 88 (3) 552-560; DOI: https://doi.org/10.1124/mol.115.099671
C. Hoffmann
Bio-Imaging-Center/Rudolf-Virchow-Zentrum and Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (C.H.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Spain (M.C.); Institute of Chemistry, University of Tartu, Tartu, Estonia (A.R.); Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University, Amsterdam, Amsterdam, The Netherlands (R.L., H.F.V.); and Cell Signalling Research Group, School of Life Sciences, Medical School, Queen’s Medical Centre, University of Nottingham, Nottingham, United Kingdom (S.J.H.)
M. Castro
Bio-Imaging-Center/Rudolf-Virchow-Zentrum and Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (C.H.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Spain (M.C.); Institute of Chemistry, University of Tartu, Tartu, Estonia (A.R.); Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University, Amsterdam, Amsterdam, The Netherlands (R.L., H.F.V.); and Cell Signalling Research Group, School of Life Sciences, Medical School, Queen’s Medical Centre, University of Nottingham, Nottingham, United Kingdom (S.J.H.)
A. Rinken
Bio-Imaging-Center/Rudolf-Virchow-Zentrum and Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (C.H.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Spain (M.C.); Institute of Chemistry, University of Tartu, Tartu, Estonia (A.R.); Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University, Amsterdam, Amsterdam, The Netherlands (R.L., H.F.V.); and Cell Signalling Research Group, School of Life Sciences, Medical School, Queen’s Medical Centre, University of Nottingham, Nottingham, United Kingdom (S.J.H.)
R. Leurs
Bio-Imaging-Center/Rudolf-Virchow-Zentrum and Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (C.H.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Spain (M.C.); Institute of Chemistry, University of Tartu, Tartu, Estonia (A.R.); Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University, Amsterdam, Amsterdam, The Netherlands (R.L., H.F.V.); and Cell Signalling Research Group, School of Life Sciences, Medical School, Queen’s Medical Centre, University of Nottingham, Nottingham, United Kingdom (S.J.H.)
S. J. Hill
Bio-Imaging-Center/Rudolf-Virchow-Zentrum and Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (C.H.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Spain (M.C.); Institute of Chemistry, University of Tartu, Tartu, Estonia (A.R.); Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University, Amsterdam, Amsterdam, The Netherlands (R.L., H.F.V.); and Cell Signalling Research Group, School of Life Sciences, Medical School, Queen’s Medical Centre, University of Nottingham, Nottingham, United Kingdom (S.J.H.)
H. F. Vischer
Bio-Imaging-Center/Rudolf-Virchow-Zentrum and Institute of Pharmacology and Toxicology, University of Würzburg, Würzburg, Germany (C.H.); Molecular Pharmacology Laboratory, Biofarma Research Group (GI-1685), University of Santiago de Compostela, Center for Research in Molecular Medicine and Chronic Diseases, Spain (M.C.); Institute of Chemistry, University of Tartu, Tartu, Estonia (A.R.); Amsterdam Institute for Molecules, Medicines and Systems, Division of Medicinal Chemistry, Faculty of Sciences, VU University, Amsterdam, Amsterdam, The Netherlands (R.L., H.F.V.); and Cell Signalling Research Group, School of Life Sciences, Medical School, Queen’s Medical Centre, University of Nottingham, Nottingham, United Kingdom (S.J.H.)
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In this issue
Rapid CommunicationMinireview—Exploring the biology of GPCRs: from in vitro to in vivo
Residence Time at GPCRs
C. Hoffmann, M. Castro, A. Rinken, R. Leurs, S. J. Hill and H. F. Vischer
Molecular Pharmacology September 1, 2015, 88 (3) 552-560; DOI: https://doi.org/10.1124/mol.115.099671
Jump to section
- Article
- Visual Overview
- Abstract
- Introduction
- The Concept of Ligand Residence Time at GPCRs
- State of the Art: Currently Used Assays
- Surface Plasmon Resonance Analysis
- Novel Approaches and Promising Developments
- Binding of Fluorescent Ligands by Fluorescence Intensity
- Binding Determined by Fluorescence Anisotropy
- Binding Determined by Fluorescence Correlation Spectroscopy
- Binding Determined by Resonance Energy Transfer Techniques
- Examples for Biologic Discrimination by Different Ligand Residence Times
- Author Contributions
- Footnotes
- Abbreviations
- References
- Figures & Data
- Info & Metrics
- eLetters
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