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Journal of Receptors and Signal Transduction Volume 29, 2009 - Issue 3-4
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Research Article

An optical dynamic mass redistribution assay reveals biased signaling of dualsteric GPCR activators

Anna KebigPharmacology and Toxicology Section, Institute of Pharmacy, Rheinische Friedrich-Wilhelms-University, Bonn, Germany
,
Evi KostenisInstitute of Pharmaceutical Biology, Rheinische Friedrich-Wilhelms-University, Bonn, Germany
,
Klaus MohrPharmacology and Toxicology Section, Institute of Pharmacy, Rheinische Friedrich-Wilhelms-University, Bonn, GermanyCorrespondence[email protected]
&
Marion Mohr-AndräPharmacology and Toxicology Section, Institute of Pharmacy, Rheinische Friedrich-Wilhelms-University, Bonn, Germany
Pages 140-145 | Received 15 Jan 2009, Accepted 11 Mar 2009, Published online: 08 Jul 2009

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Ye Fang. (2012) Ligand–receptor interaction platforms and their applications for drug discovery. Expert Opinion on Drug Discovery 7:10, pages 969-988.
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Ye Fang. (2011) The development of label-free cellular assays for drug discovery. Expert Opinion on Drug Discovery 6:12, pages 1285-1298.
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Ye Fang. (2010) Probing cancer signaling with resonant waveguide grating biosensors. Expert Opinion on Drug Discovery 5:12, pages 1237-1248.
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Jinyin Zha, Jixiao He, Chengwei Wu, Mingyang Zhang, Xinyi Liu & Jian Zhang. (2023) Designing drugs and chemical probes with the dualsteric approach. Chemical Society Reviews.
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Andr? S. Pupo, Diego A. Duarte, Vanessa Lima, Larissa B. Teixeira, Lucas T. Parreiras-e-Silva & Claudio M. Costa-Neto. (2016) Recent updates on GPCR biased agonism. Pharmacological Research 112, pages 49-57.
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Arthur Christopoulos. (2014) Advances in G Protein-Coupled Receptor Allostery: From Function to Structure. Molecular Pharmacology 86:5, pages 463-478.
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Jeremy Shonberg, Laura Lopez, Peter J. Scammells, Arthur Christopoulos, Ben Capuano & J. Robert Lane. (2014) Biased Agonism at G Protein-Coupled Receptors: The Promise and the Challenges-A Medicinal Chemistry Perspective. Medicinal Research Reviews 34:6, pages 1286-1330.
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Andrew C. Kruse, Brian K. Kobilka, Dinesh Gautam, Patrick M. Sexton, Arthur Christopoulos & Jürgen Wess. (2014) Muscarinic acetylcholine receptors: novel opportunities for drug development. Nature Reviews Drug Discovery 13:7, pages 549-560.
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Régis Méjard, Hans J. Griesser & Benjamin Thierry. (2014) Optical biosensing for label-free cellular studies. TrAC Trends in Analytical Chemistry 53, pages 178-186.
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AS Ahmedat, M Warnken, WK Seemann, K Mohr, E Kostenis, UR Juergens & K Racké. (2013) Pro-fibrotic processes in human lung fibroblasts are driven by an autocrine/paracrine endothelinergic system. British Journal of Pharmacology 168:2, pages 471-487.
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Celine ValantJ. Robert LanePatrick M. SextonArthur Christopoulos. (2012) The Best of Both Worlds? Bitopic Orthosteric/Allosteric Ligands of G Protein–Coupled Receptors. Annual Review of Pharmacology and Toxicology 52:1, pages 153-178.
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Megan Morse, Elizabeth Tran, Haiyan Sun, Robert Levenson & Ye Fang. (2011) Ligand-Directed Functional Selectivity at the Mu Opioid Receptor Revealed by Label-Free Integrative Pharmacology On-Target. PLoS ONE 6:10, pages e25643.
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M. Kammermann, A. Denelavas, A. Imbach, U. Grether, H. Dehmlow, C.M. Apfel & C. Hertel. (2011) Impedance measurement: A new method to detect ligand-biased receptor signaling. Biochemical and Biophysical Research Communications 412:3, pages 419-424.
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F. Lamyel, M. Warnken-Uhlich, W. K. Seemann, K. Mohr, E. Kostenis, A. S. Ahmedat, M. Smit, R. Gosens, H. Meurs, A. Miller-Larsson & Kurt Racké. (2011) The β2-subtype of adrenoceptors mediates inhibition of pro-fibrotic events in human lung fibroblasts. Naunyn-Schmiedeberg's Archives of Pharmacology 384:2, pages 133-145.
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Natalya Zaytseva, William Miller, Vasily Goral, Jerry Hepburn & Ye Fang. (2011) Microfluidic resonant waveguide grating biosensor system for whole cell sensing. Applied Physics Letters 98:16.
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T. Steinfeld, A. D. Hughes, U. Klein, J. A. M. Smith & M. Mammen. (2010) THRX-198321 Is a Bifunctional Muscarinic Receptor Antagonist and  2-Adrenoceptor Agonist (MABA) That Binds in a Bimodal and Multivalent Manner. Molecular Pharmacology 79:3, pages 389-399.
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Richard Eglen & Terry Reisine. (2011) GPCRs Revisited: New Insights Lead to Novel Drugs. Pharmaceuticals 4:2, pages 244-272.
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Ye Fang. (2011) Label-Free Biosensors for Cell Biology. International Journal of Electrochemistry 2011, pages 1-16.
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Nicola J. Smith, Kirstie A. Bennett & Graeme Milligan. (2011) When simple agonism is not enough: Emerging modalities of GPCR ligands. Molecular and Cellular Endocrinology 331:2, pages 241-247.
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Elisa Alvarez-Curto, Richard J. Ward & Graeme Milligan. 2011. Methods for the Discovery and Characterization of G Protein-Coupled Receptors. Methods for the Discovery and Characterization of G Protein-Coupled Receptors 231 253 .
Ann M. Ferrie, Qi Wu & Ye Fang. (2010) Resonant waveguide grating imager for live cell sensing. Applied Physics Letters 97:22.
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Marco De Amici, Clelia Dallanoce, Ulrike Holzgrabe, Christian Tränkle & Klaus Mohr. (2010) Allosteric ligands for G protein-coupled receptors: A novel strategy with attractive therapeutic opportunities. Medicinal Research Reviews 30:3, pages 463-549.
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Klaus Mohr, Christian Tränkle, Evi Kostenis, Elisabetta Barocelli, Marco De Amici & Ulrike Holzgrabe. (2010) Rational design of dualsteric GPCR ligands: quests and promise. British Journal of Pharmacology 159:5, pages 997-1008.
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Magalie Rocheville & Stephen L. Garland. (2010) An industrial perspective on positive allosteric modulation as a means to discover safe and selective drugs. Drug Discovery Today: Technologies 7:1, pages e87-e94.
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Liyun Wang, Bronwen Martin, Randall Brenneman, Louis M. Luttrell & Stuart Maudsley. (2009) Allosteric Modulators of G Protein-Coupled Receptors: Future Therapeutics for Complex Physiological Disorders. Journal of Pharmacology and Experimental Therapeutics 331:2, pages 340-348.
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