Label-free optical biosensor: A tool for G protein-coupled receptors pharmacology profiling and inverse agonists identification

References

• Bleicher K, Bohm H, Muller K, Alanine A. Hit and lead generation: Beyond high-throughput screening. Nat Rev Drug Discov 2003;2:369–78.
   PubMed Web of Science ®Google Scholar
• Zheng C, Han L, Yap C, Ji Z, Cao Z, Chen Y. Therapeutic targets: Progress of their exploration and investigation of their characteristics. Pharmacol Rev 2006;58:259–79.
   PubMed Web of Science ®Google Scholar
• Denholm E, Stankus G. Differential effects of two fluorescent probes on macrophage migration as assessed by manual and automated methods. Cytometry 1995;19:366–9.
   Google Scholar
• Abbitt K, Rainger G, Nash G. Effects of fluorescent dyes on selectin and integrin-mediated stages of adhesion and migration of flowing leukocytes. J Immunol Methods 2000;239:109–19.
   Google Scholar
• Cooper M. Non-optical screening platforms: The next wave in label-free screening? Drug Discovery Today 2006;11:1068–74.
   PubMed Web of Science ®Google Scholar
• Cooper M. Optical biosensors: Where next and how soon? Drug Discovery Today 2006;11:1061–7.
   PubMed Web of Science ®Google Scholar
• Fang Y. Label-free cell-based assays with optical biosensors in drug discovery. Assay Drug Dev Technol 2006;4:583–95.
   PubMed Web of Science ®Google Scholar
• Giaever I, Keese C. A morphological biosensor for mammalian cells. Nature 1993;366:591–2.
   PubMed Web of Science ®Google Scholar
• Solly K, Wang X, Xu X, Strulovici B, Zheng W. Application of real-time cell electronic sensing (RT-CES) technology to cell-based assays. Assay Drug Dev Technol 2004;2:363–72.
   PubMed Web of Science ®Google Scholar
• Atienza J, Yu N, Kirstein S, Xi B, Wang X, Xu X, Abassi Y. Dynamic and label-free cell-based assays using the real-time cell electronic sensing system. Assay Drug Dev Technol 2006;4:597–607.
   PubMed Web of Science ®Google Scholar
• Fang Y, Li G, Ferrie A. Non-invasive optical biosensor for assaying endogenous G protein-coupled receptors in adherent cells. J Pharmacol Toxicol Methods 2007;55:314–22.
   PubMedGoogle Scholar
• McGuinness R, Proctor J, Gallant D, van Staden C, Ly J, Tang F, Lee P. Enhanced selectivity screening of GPCR ligands using a label-free cell based assay technology. Combinatorial Chemistry and High-throughput Screening 2009, in press.
   Google Scholar
• Ciambrone G, Liu V, Lin D, McGuinness R, Leung G, Pitchford S. Cellular dielectric spectroscopy: A powerful new approach to label-free cellular analysis. J Biomol Screen 2004;9:467–80.
   PubMed Web of Science ®Google Scholar
• Fang Y, Ferrie A, Fontaine N, Mauro J, Balakrishnan J. Resonant waveguide grating biosensor for living cell sensing. Biophys J 2006;91:1925–40.
   PubMed Web of Science ®Google Scholar
• Kenakin T. Principles: Receptor theory in pharmacology. Trends Pharmacol Sci 2004;25:186–92.
   PubMed Web of Science ®Google Scholar
• Vilardaga J, Steinmeyer R, Harms G, Lohse M. Molecular basis of inverse agonism in a G protein-coupled receptor. Nat Chem Biol 2005;1:25–8.
   PubMed Web of Science ®Google Scholar
• Kenakin T. Efficacy as a vector: The relative prevalence and paucity of inverse agonism. Mol Pharmacol 2004;65:2–11.
   PubMed Web of Science ®Google Scholar
• George S, Bungay P, Naylor L. Evaluation of a CRE-directed luciferase reporter gene assay as an alternative to measuring cAMP accumulation. J Biomol Screen 1997;2:235–40.
   Google Scholar
• Kenakin T. Drug efficacy at G protein-coupled receptors. Annu Rev Pharmacol Toxicol 2002;42:349–79.
   PubMedGoogle Scholar
• Kenakin T, Onaran O. The ligand paradox between affinity and efficacy: Can you be there and not make a difference? Trends Pharmacol Sci 2002;23:275–80.
   PubMed Web of Science ®Google Scholar
• Ghanouni P, Gryczynski Z, Steenhuis J, Lee T, Farrens D, Lakowicz J, Kobilka B. Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor. J Biol Chem 2001;276:24433–6.
   PubMed Web of Science ®Google Scholar
• Fang Y, Ferrie AM, Li G. Cellular functions of cholesterol probed with optical biosensors. Biochim Biophys Acta (BBA) Mol Cell Res 2006;1763:254–61.
   Google Scholar
• Lee P, Gao A, van Staden C, Ly J, Salon J, Xu A, Fang Y, Verkleeren R. Evaluation of dynamic mass redistribution technology for pharmacological studies of recombinant and endogenously expressed G protein-coupled receptors. Assay Drug Dev Technol 2008;6:83–94.
   PubMed Web of Science ®Google Scholar
• Hall D, Strange P. Evidence that antipsychotic drugs are inverse agonists at D2 dopamine receptor. Br J Pharmacol 1997;121:731–6.
   Google Scholar
• Kenakin T. Functional selectivity through protean and biased agonism: Who steers the ship? Mol Pharmacol 2007;72:1393–401.
   PubMed Web of Science ®Google Scholar
• Costa T, Herz A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci USA 1989;86:7321–5.
   PubMed Web of Science ®Google Scholar
• Chidiac P, Hebert T, Valiquette M, Dennis M, Bouvier M. Inverse agonist activity of beta-adrenergic antagonists. Mol Pharmacol 1994;45:490–9.
   PubMed Web of Science ®Google Scholar
• Barker E, Westphal R, Schmidt D, Sanders-Bush E. Constitutively active 5-hydroxytryptamine2C receptors reveal novel inverse agonist activity of receptor ligands. J Biol Chem 1994;269:11687–90.
   PubMed Web of Science ®Google Scholar
• Leeb-Lundberg L, Mathis S, Herzig M. Antagonists of bradykinin that stabilize a G-protein-uncoupled state of the B2 receptor act as inverse agonists in rat myometrial cells. J Biol Chem 1994;269:25970–3.
   PubMed Web of Science ®Google Scholar
• Hanf R, Li Y, Szabo G, Fischmeister R. Agonist-independent effects of muscarinic antagonists on Ca2+ and K+ currents in frog and rat cardiac cells. J Physiol 1993;461: 743–65.
   Google Scholar
• Milligan G. Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Mol Pharmacol 2003;64:1271–6.
   PubMed Web of Science ®Google Scholar
• Parnot C, Miserey-Lenkei S, Bardin S, Corvol P, Clauser E. Lessons from constitutively active mutants of G protein-coupled receptors. Trends Endocrinol Metab TEM 2002;13:336–43.
   PubMedGoogle Scholar
• Levin M, Marullo S, Muntaner O, Andersson B, Magnusson Y. The myocardium-protective Gly-49 variant of the beta1-adrenergic receptor exhibits constitutive activity and increased desensitization and down-regulation. J Biol Chem 2002;277:30429–435.
   Google Scholar
• Okada M, Northup J, Ozaki N, Russell J, Linnoila M, Goldman D. Modification of human 5-HT(2C) receptor function by Cys23Ser, an abundant, naturally occurring amino-acid substitution. Mol Psychiatry 2004;9:55–64.
   PubMedGoogle Scholar
• Millan M, Gobert A, Audinot V, Dekeyne A, Newman-Tancredi A. Inverse agonists and serotonergic transmission: From recombinant, human serotonin (5-HT)1B receptors to G-protein coupling and function in corticolimbic structures in vivo. Neuropsychopharmacology 1999;21:61S–67S.
   Google Scholar
• Schipani E, Kruse K, Juppner H. A constitutively active mutant PTH-PTHrP receptor in Jansen-type metaphyseal chondrodysplasia. Science 1995;268:98–100.
   PubMed Web of Science ®Google Scholar
• Spiegel A. Defects in G protein-coupled signal transduction in human disease. Ann Rev Physiol 1996;58:143–70.
   PubMed Web of Science ®Google Scholar
• De Ligt R, Kourounakis A, Ijzerman A. Inverse agonism at G protein-coupled receptors: (Patho)physiological relevance and implications for drug discovery. Br J Pharmacol 2000;130:1–12.
   Google Scholar
• Convineau A, Laburthe M. The human vasoactive intestinal peptide receptor: Molecular identification by covalent cross-linking in colonic epithelium. J Clin Endocrinol Metab 1985;61:50–5.
   Google Scholar
• Virgolini I, Yang Q, Li S, Angelberger P, Neuhold N, Niederle B, Scheithauer W, Valent P. Cross-competition between vasoactive intestinal peptide and somatostatin for binding to tumor cell membrane receptors. Cancer Res 1994;54:690–700.
   PubMed Web of Science ®Google Scholar
• O’Dorisio M, Fleshman D, Qualman S, O’Dorisio T. Vasoactive intestinal peptide: Autocrine growth factor in neuroblastoma. Regul Pept 1992;37:213–26.
   Google Scholar
• Moody T, Zia F, Draoui M, Brenneman D, Fridkin M, Davidson A, Gozes I. A vasoactive intestinal peptide antagonist inhibits non-small cell lung cancer growth. Proc Natl Acad Sci USA 1993;90:4345–9.
   PubMed Web of Science ®Google Scholar
• Cuttitta F, Carney D, Mulshine J, Moody T, Fedorko J, Fischler A, Minna J. Bombesin-like peptides can function as autocrine growth factors in human small-cell lung cancer. Nature 1985;316:823–6.
   PubMed Web of Science ®Google Scholar
• Mahmoud S, Staley J, Taylor J, Bogden A, Moreau J, Coy D, Avis I, Cuttitta F, Mulshine J, Moody T. [Psi 13,14] bombesin analogues inhibit growth of small cell lung cancer in vitro and in vivo. Cancer Res 1991;51:1798–802.
   PubMed Web of Science ®Google Scholar
• Kroog G, Jensen R, Battey J. Mammalian bombesin receptors. Med Res Rev 1995;15:389–417.
   PubMed Web of Science ®Google Scholar
• Gozes I, McCune S, Jacobson L, Warren D, Moody T, Fridkin M, Brenneman D. An antagonist to vasoactive intestinal peptide affects cellular functions in the central nervous system. J Pharmacol Exp Ther 1991;257:959–66.
   PubMed Web of Science ®Google Scholar
• Kenakin T. Inverse, protean, and ligand-selective agonism: Matters of receptor conformation. FASEB J 2001;15:598–611.
   PubMed Web of Science ®Google Scholar
• Nwokolo C, Smith J, Sawyerr A, Pounder R. Rebound intragastric hyperacidity after abrupt withdrawal of histamine H2 receptor blockade. Gut 1991;32:1455–60.
   PubMed Web of Science ®Google Scholar
• Wilder-Smith C, Ernst T, Gennoni M, Zeyen B, Halter F, Merki H. Tolerance to oral H2-receptor antagonists. Dig Dis Sci 1990;35:976–83.
   PubMed Web of Science ®Google Scholar
• Deakin M, Williams J. Histamine H2-receptor antagonists in peptic ulcer disease. Efficacy in healing peptic ulcers. Drugs 1992;44:709–19.
   Google Scholar
• Smit M, Leurs R, Alewijnse A, Blauw J, Van Nieuw Amerongen G, Van De Vrede Y, Roovers E, Timmerman H. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci USA 1996;93:6802–7.
   PubMed Web of Science ®Google Scholar
• Milligan G, Bond R. Inverse agonism and the regulation of receptor number. Trends Pharmacol Sci 1997;18:468–74.
   PubMed Web of Science ®Google Scholar
• MacEwan D, Milligan G. Inverse agonist-induced up-regulation of the human beta2-adrenoceptor in transfected neuroblastoma X glioma hybrid cells. Mol Pharmacol 1996;50:1479–86.
   PubMed Web of Science ®Google Scholar
• Lee T, Cotecchia S, Milligan G. Up-regulation of the levels of expression and function of a constitutively active mutant of the hamster alpha1B-adrenoceptor by ligands that act as inverse agonists. Biochem J 1997;325 (Pt 3):733–9.
   Google Scholar
• Seifert R, Wenzel-Seifert K. Constitutive activity of G-protein-coupled receptors: Cause of disease and common property of wild-type receptors. Naunyn Schmiedebergs Arch Pharmacol 2002;366:381–416.
   PubMed Web of Science ®Google Scholar
• Herrick-Davis K, Grinde E, Teitler M. Inverse agonist activity of atypical antipsychotic drugs at human 5-hydroxytryptamine2C receptors. J Pharmacol Exp Ther 2000;295:226–232.
   PubMed Web of Science ®Google Scholar
• The Cardiac Insufficiency Bisoprolol Study II (CIBIS-II): A randomised trial. Lancet 1999;353:9–13.
   Google Scholar
• Hjalmarson A, Goldstein S, Fagerberg B, Wedel H, Waagstein F, Kjekshus J, Wikstrand J, El Allaf D, Vitovec J, Aldershvile J, Halinen M, Dietz R, Neuhaus K, Janosi A, Thorgeirsson G, Dunselman P, Gullestad L, Kuch J, Herlitz J, Rickenbacher P, Ball S, Gottlieb S, Deedwania P. Effects of controlled-release metoprolol on total mortality, hospitalizations, and well-being in patients with heart failure. The Metoprolol CR/XL Randomized Intervention Trial in congestive heart failure (MERIT-HF). MERIT-HF Study Group. JAMA 2000;283:1295–1302.
   PubMed Web of Science ®Google Scholar
• Packer M, Bristow M, Cohn J, Colucci W, Fowler M, Gilbert E, Shusterman N. The effect of carvedilol on morbidity and mortality in patients with chronic heart failure. U.S. Carvedilol Heart Failure Study Group. N Engl J Med 1996;334:1349–55.
   PubMed Web of Science ®Google Scholar
• Lechat P, Packer M, Chalon S, Cucherat M, Arab T, Boissel J. Clinical effects of beta-adrenergic blockade in chronic heart failure: A meta-analysis of double-blind, placebo-controlled, randomized trials. Circulation 1998;98:1184–91.
   PubMed Web of Science ®Google Scholar
• Maack C, Cremers B, Flesch M, Hoper A, Sudkamp M, Bohm M. Different intrinsic activities of bucindolol, carvedilol and metoprolol in human failing myocardium. Br J Pharmacol 2000;130:1131–9.
   PubMed Web of Science ®Google Scholar
• Callaerts-Vegh Z, Evans K, Dudekula N, Cuba D, Knoll B, Callaerts P, Giles H, Shardonofsky F, Bond R. Effects of acute and chronic administration of beta-adrenoceptor ligands on airway function in a murine model of asthma. Proc Natl Acad Sci USA 2004;101:4948–4953.
   PubMed Web of Science ®Google Scholar
• Devlin M, Smith N, Ryan O, Guida E, Sexton P, Christopoulos A. Regulation of serotonin 5-HT2C receptors by chronic ligand exposure. Eur J Pharmacol 2004;498:59–69.
   Google Scholar