Radioligand dissociation measurements: potential interference of rebinding and allosteric mechanisms and physiological relevance of the biological model systems

Bibliography

• Holford NHG, Sheiner LB. Kinetics of pharmacological response. Pharmacol Ther 1982;16:143-66
   PubMed Web of Science ®Google Scholar
• Eklind-Cervenka M, Benson L, Dahlstrom U, Association of candesartan vs losartan with all-cause mortality in patients with heart failure. J Am Med Assoc 2011;305:175-82
   PubMed Web of Science ®Google Scholar
• Kjeldsen SE, Stalhammar J, Hasvold P, Effects of losartan vs candesartan in reducing cardiovascular events in the primary treatment of hypertension. J Hum Hypertens 2010;24:263-73
   PubMed Web of Science ®Google Scholar
• Swinney DC. Biochemical mechanisms of drug action: what does it take for success? Nat Rev Drug Discov 2004;3:801-8
   PubMed Web of Science ®Google Scholar
• Swinney DC. Biochemical mechanisms of new molecular entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and safety. Curr Top Med Chem 2006;6:461-78
   PubMed Web of Science ®Google Scholar
• Swinney DC. Can binding kinetics translate to a clinically differentiated drug? From theory to practice. Lett Drug Des Discov 2006;3:569-74
   Web of Science ®Google Scholar
• Swinney DC. Applications of binding kinetics to drug discovery: translation of binding mechanisms to clinically differentiated therapeutic responses. Int J Pharm Med 2008;22:23-34
   Google Scholar
• Swinney DC. The role of binding kinetics in therapeutically useful drug action. Curr Opin Drug Discov Dev 2009;12:31-9
   PubMed Web of Science ®Google Scholar
• Copeland RA, Pompliano DL, Meek TD. Drug-target residence time and its implications for lead optimization. Nat Rev Drug Discov 2006;5:730-9
   PubMed Web of Science ®Google Scholar
• Tummino PJ, Copeland RA. Residence time of receptor-ligand complexes and its effect on biological function. Biochemistry 2008;47:5481-92
   PubMed Web of Science ®Google Scholar
• Copeland RA. The dynamics of drug-target interactions: drug-target residence time and its impact on efficacy and safety. Expert Opin Drug Discov 2010;5:305-10
   PubMed Web of Science ®Google Scholar
• Zhang R, Monsma F. The importance of drug-target residence time. Curr Opin Drug Discov Devel 2009;12:488-96
   PubMed Web of Science ®Google Scholar
• Zhang R, Monsma F. Binding kinetics and mechanism of action: toward the discovery and development of better and best in class drugs. Expert Opin Drug Discov 2010;5:1023-9
   PubMed Web of Science ®Google Scholar
• Vauquelin G, Van Liefde I. Slow antagonist dissociation and long-lasting in vivo receptor protection. Trends Pharmacol Sci 2006;27:356-9
   PubMed Web of Science ®Google Scholar
• Vauquelin G. Rebinding: or why drugs may act longer in vivo than expected from their in vitro target residence time. Expert Opin Drug Discov 2010;5:927-41
   PubMed Web of Science ®Google Scholar
• Vauquelin G, Charlton S. Long-lasting target binding and rebinding as mechanisms to prolong in vivo drug action. Br J Pharmacol 2010;161:488-508
   PubMed Web of Science ®Google Scholar
• Vauquelin G, Bostoen S, Vanderheyden P, Seeman P. Clozapine, atypical antipsychotics and the benefits of fast-off D2 dopamine receptor antagonism. Naunyn Schmiedebergs Arch Pharmacol 2012, published online Feb 14 2012, doi 10.1007/s00210-012-0734-2
   PubMed Web of Science ®Google Scholar
• Vauquelin G. Determination of drug-receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance. Med Chem Commun 2012; doi 10.1039/C2MD20015E
   Google Scholar
• Dowling MR, Charlton SJ. Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor. Br J Pharmacol 2006;148:1134-42
   Google Scholar
• Heise CE, Sullivan S, Crowe PD. Scintillation proximity assay as high-throughput method to identify slowly dissociating nonpeptide ligand binding to the GnRH receptor. J Biomol Screen 2007;12:235-9
   PubMed Web of Science ®Google Scholar
• Malany S, Hernandez LM, Smith WF, Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors. J Recept Signal Transduct Res 2009;29:84-93
   PubMed Web of Science ®Google Scholar
• Packeu A, Wennerberg M, Ballendran A, Vauquelin G. Estimation of the dissociation rate of unlabelled ligand-receptor complexes by a “two-step” competition binding approach. Br J Pharmacol 2010;161:1311-28
   PubMed Web of Science ®Google Scholar
• De Meyts P, Roth J, Neville DM Jr, Insulin interactions with its receptors: experimental evidence for negative cooperativity. Biochem Biophys Res Commun 1973;55:154-61
   PubMed Web of Science ®Google Scholar
• De Meyts P. Insulin and its receptor: structure, function and evolution. Bioessays 2004;26:1351-62
   PubMed Web of Science ®Google Scholar
• Christopoulos A, Kenakin T. G protein-coupled receptor allosterism and complexing. Pharmacol Rev 2002;54:323-74
   PubMed Web of Science ®Google Scholar
• Christopoulos A. Allosteric binding sites on cell-surface receptors: novel targets for drug discovery. Nat Rev Drug Discov 2002;1:198-210
   PubMed Web of Science ®Google Scholar
• Valant C, Robert Lane J, Sexton PM, Christopoulos A. The best of two worlds? Bitopic orthostetic/allosteric ligands of G protein-coupled receptors. Annu Rev Pharmacol Toxicol 2012;52:153-78
   PubMed Web of Science ®Google Scholar
• Kostenis E, Mohr K. Composite action of allosteric modulators on ligand binding. Trends Pharmacol Sci 1996;17:443-4
   PubMedGoogle Scholar
• Ellis J. Allosteric binding sites on muscarinic receptors. Drug Dev Res 1997;40:193-204
   Web of Science ®Google Scholar
• Ellis J, Seidenberg M. Interactions of alcuronium, TMB-8, and other allosteric ligands with muscarinic acetylcholine receptors: studies with chimeric receptors. Mol Pharmacol 2000;58:1451-60
   PubMed Web of Science ®Google Scholar
• Molderings GJ, Menzel S, Kathmann M, Dual interaction of agmatine with the rat alpha2D-adrenoceptor: competitive antagonism and allosteric activation. Br J Pharmacol 2000;130:1706-12
   PubMed Web of Science ®Google Scholar
• Limbird LE, Lefkowitz RJ. Negative cooperativity among beta-adrenergic receptors in frog erythrocyte membrane. J Biol Chem 1976;251:5007-14
   PubMed Web of Science ®Google Scholar
• De Meyts P, Bianco R, Roth J. Site-site interactions among insulin receptors. Characterization of the negative cooperativity. J Biol Chem 1977;251:1877-88
   Web of Science ®Google Scholar
• Sutter A, Riopelle RG, Harris-Warrick RM, Shooter EM. Nerve growth factor receptors. Characterization of two distinct classes of binding sites on chick embryo sensory ganglia cells. J Biol Chem 1979;254:5972-82
   PubMed Web of Science ®Google Scholar
• Springael JY, Le Minh PN, Urizar E, Allosteric modulation of binding properties between units of chemokine receptor homo- and hetero-oligomers. Mol Pharmacol 2006;69:1652-61
   PubMed Web of Science ®Google Scholar
• Szidonya L, Cserzo M, Hunyady L. Dimerization and oligomerization of G-protein-coupled receptors: debated structures with established and emerging functions. J Endocrinol 2008;196:435-53
   PubMed Web of Science ®Google Scholar
• Berg HC, Purcell EM. Physics of chemoreception. Biophys J 1977;20:193-219
   PubMed Web of Science ®Google Scholar
• Shoup D, Szabo A. Role of diffusion in ligand binding to macromolecules and cell-bound receptors. Biophys J 1982;40:33-9
   PubMed Web of Science ®Google Scholar
• Goldstein B, Posner RG, Torney DC, Competition between solution and cell surface receptors for ligand. Dissociation of hapten bound to surface antibody in the presence of solution antibody. Biophys J 1989;56:955-66
   PubMed Web of Science ®Google Scholar
• Goldstein B, Dembo M. Approximating the effects of diffusion on reversible reactions at the cell surface: ligand-receptor kinetics. Biophys J 1995;68:1222-30
   PubMed Web of Science ®Google Scholar
• Fierens F, Vanderheyden PML, Roggeman C, Distinct binding properties of the AT1 receptor antagonist [3H]candesartan to intact cells and membrane preparations. Biochem Pharmacol 2002;63:1273-9
   PubMed Web of Science ®Google Scholar
• Silhavy TJ, Szmelcman S, Boos W, Schwartz M. On the significance of the retention of ligand by protein. Proc Natl Acad Sci USA 1975;72:2120-4
   PubMed Web of Science ®Google Scholar
• Spivak CE, Oz M, Beglan CL, Shrager RI. Diffusion delays and unstirred layer effects at monolayer cultures of Chinese hamster ovary cells: radioligand binding, confocal microscopy, and mathematical simulations. Cell Biochem Biophys 2006;45:43-58
   PubMed Web of Science ®Google Scholar
• Pike LJ. Lipid rafts: bringing order to chaos. J Lipid Res 2003;44:655-67
   PubMed Web of Science ®Google Scholar
• Andrews SS. Serial rebinding of ligands to clustered receptors as exemplified by bacterial chemotaxis. Phys Biol 2005;2:111-22
   PubMed Web of Science ®Google Scholar
• Gopalakrishnan M, Forsten-Williams K, Nugent MA, Tauber UC. Effects of receptor clustering on ligand dissociation kinetics: theory and simulations. Biophys J 2005;89:3686-700
   PubMed Web of Science ®Google Scholar
• Coombs D, Goldstein B. Effects of geometry of the immunological synapse on the delivery of effector molecules. Biophys J 2004;87:2215-20
   PubMed Web of Science ®Google Scholar
• Perry DC, Mullis KB, Øie S, Sadee W. Opiate antagonist receptor binding in vivo: evidence for a new receptor binding model. Brain Res 1980;199:49-61
   PubMed Web of Science ®Google Scholar
• Sadee W, Perry DC, Rosenbaum JS, Herz A. [3H]-diprenorphine receptor binding in vivo and in vitro. Eur J Pharmacol 1982;81:431-40
   PubMed Web of Science ®Google Scholar
• Szczuka A, Packeu A, Wennerberg M, Vauquelin G. Molecular mechanism of the persistent bronchodilatory effect of the partial beta2-adrenoceptor agonist salmeterol. Br J Pharmacol 2009;158:183-94
   PubMed Web of Science ®Google Scholar
• Frost JJ, Wagner HR Jr. Kinetics of binding to opiate receptors in vivo predicted from in vitro parameters. Brain Res 1984;305:1-11
   PubMed Web of Science ®Google Scholar
• Nieba L, Krebber A, Pluckthun A. Competition BIAcore for measuring true affinities: large differences from values determined from binding kinetics. Anal Biochem 1996;234:155-65
   PubMed Web of Science ®Google Scholar
• Schuck P, Minton AP. Analysis of mass transport-limited binding kinetics in evanescent wave biosensors. Anal Biochem 1996;240:262-72
   PubMed Web of Science ®Google Scholar
• Myszka DG, He X, Dembo M, Extending the range of rate constants available from BIACORE: interpreting mass transport-influenced binding data. Biophys J 1998;75:583-94
   PubMed Web of Science ®Google Scholar
• Abbott AJ, Nelsestuen GL. The collisional limit: an important consideration for membrane-associated enzymes and receptors. FASEB J 1988;2:2858-66
   PubMed Web of Science ®Google Scholar
• Le MT, Pugsley M, Vauquelin G, Van Liefde I. Angiotensin II AT1 antagonism and insurmountability: comparison of olmesartan and telmisartan. Br J Pharmacol 2007;151:952-62
   PubMed Web of Science ®Google Scholar
• Holliger P, Hudson PJ. Engineered antibody fragments and the rise of single domains. Nat Biotechnol 2005;23:1126-36
   PubMed Web of Science ®Google Scholar
• Steinfeld T, Hughes AD, Klein U, THRX-198321 is a bifunctional muscarinic receptor antagonist and beta2-adrenoceptor agonist (MABA) that binds in a bimodal and multivalent manner. Mol Pharmacol 2011;79:389-99
   PubMed Web of Science ®Google Scholar
• Kaufman EN, Jain RK. Effect of bivalent interaction upon apparent antibody affinity: experimental confirmation of a theory using fluorescence photobleaching and implications for antibody binding assays. Cancer Res 1992;52:4157-67
   PubMed Web of Science ®Google Scholar
• Pluckthun A, Pack P. New protein engineering approaches to multivalent and bispecific antibody fragments. Immunotechnology 1997;3:83-105
   PubMedGoogle Scholar
• De Meyts P, Gauguin L, Svendsen AM, Structural basis of allosteric ligand-receptor interactions in the insulin-relaxin peptide family: implications for other receptor tyrosine kinases and G-protein-coupled receptors. Ann NY Acad Sci 2009;1160:45-53
   PubMed Web of Science ®Google Scholar
• De Meyts P. The insulin receptor: a prototype for dimeric, allosteric membrane receptors? Trends Biochem Sci 2008;33:376-84
   PubMed Web of Science ®Google Scholar
• Christopoulos A, Lunzafame A, Ziegler A, Mitchelson F. Kinetic studies of co-operativity at atrial muscarinic M2 receptors with an ‘‘infinite dilution’’ procedure. Biochem Pharmacol 1997;53:795-800
   PubMed Web of Science ®Google Scholar
• Packeu A, De Backer J-P, Van Liefde I, Antagonist- dopamine D2L- receptor interactions in intact cells. Biochem Pharmacol 2008;75:2192-203
   PubMedGoogle Scholar
• Wennerberg M, Cheng L, Hjorth S, Binding properties of antagonists to cannabinoid receptors in intact cells. Fundam Clin Pharmacol 2010;25:200-10
   Web of Science ®Google Scholar
• De Meyts P. The structural basis of insulin and insulin-like growth factor-I (IGF-I) receptor binding and negative cooperativity, and its relevance to mitogenic versus metabolic signaling. Diabetologia 1994;37:S135-48
   PubMed Web of Science ®Google Scholar
• Macdonald JL, Pike LJ. Heterogeneity in EGF-binding affinities arises from negative cooper- ativity in an aggregating system. Proc Natl Acad Sci USA 2008;105:112-17
   PubMed Web of Science ®Google Scholar
• De Meyts P, Urso B, Christoffersen CT, Shymko RM. Mechanism of insulin and IGF-I receptor activation and signal transduction specificity. Receptor dimer crosslinking, bell-shaped curves, and sustained versus transient signaling. Ann NY Acad Sci 1995;766:388-401
   PubMed Web of Science ®Google Scholar
• Kiselyov VV, Versteyhe S, Gauguin L, De Meyts P. Harmonic oscillator model of the insulin and IGF1 receptors' allosteric binding and activation. Mol Syst Biol 2009;5:243
   PubMedGoogle Scholar
• Knudsen L, De Meyts P, Kiselyov VV. Insight into the molecular basis for the kinetic differences between the two insulin receptor isoforms. Biochem J 2011;440:397-403
   PubMed Web of Science ®Google Scholar
• McKern NM, Lawrence MC, Streltsov VA, Structure of the insulin receptor ectodomain reveals a folded-over conformation. Nature 2006;443:218-21
   PubMed Web of Science ®Google Scholar
• Copeland RA. Conformational adaptation in drug-target interactions and residence time. Future Med Chem 2011;3:1491-501
   PubMed Web of Science ®Google Scholar
• Bulenger S, Marullo S, Bouvier M. Emerging role of homo- and heterodimerization in G- protein-coupled receptor biosynthesis and maturation. Trends Pharmacol Sci 2005;26:131-7
   PubMed Web of Science ®Google Scholar
• Pizard A, Machetti J, Allegrini J, Negative cooperativity in the human bradykinin B2 receptor. J Biol Chem 1998;273:1309-15
   PubMed Web of Science ®Google Scholar
• Springael JY, Urizar E, Costagliola S, Allosteric properties of G protein-coupled receptor oligomers. Pharmacol Ther 2007;115:410-18
   PubMed Web of Science ®Google Scholar
• Urizar E, Montanelli L, Loy T, Glycoprotein hormone receptors: link between receptor homodimerization and negative cooperativity. EMBO J 2005;24:1954-64
   PubMed Web of Science ®Google Scholar
• Svendsen AM, Vrecl M, Ellis TM, Cooperative binding of insulin-like peptide 3 to a dimeric relaxin family peptide receptor 2. Endocrinology 2008;149:113-20
   Google Scholar
• Kenakin T. Ligand-selective receptor conformations revisited: the promise and the problem. Trends Pharmacol Sci 2003;24:346-54
   PubMed Web of Science ®Google Scholar
• Urban JD, Vargas GA, von Zastrow M, Mailman RB. Functional selectivity and classical concepts of quantitative pharmacology. J Pharmacol Exp Ther 2007;320:1-13
   PubMed Web of Science ®Google Scholar
• Nygaard R, Frimurer TM, Holst B, Ligand binding and micro-switches in 7TM receptor structures. Trends Pharmacol Sci 2009;30:249-59
   PubMed Web of Science ®Google Scholar
• Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 2009;8:41-54
   PubMed Web of Science ®Google Scholar
• Albizu L, Balestre MN, Breton C, Probing the existence of G protein-coupled receptor dimers by positive and negative ligand-dependent cooperative binding. Mol Pharmacol 2006;70:1783-91
   PubMed Web of Science ®Google Scholar
• El Asmar L, Springael JY, Ballet S, Evidence for negative binding cooperativity within CCR5-CCR2b heterodimers. Mol Pharmacol 2005;67:460-9
   PubMed Web of Science ®Google Scholar
• Kopelman R. Fractal reaction kinetics. Science 1988;241:1620-6
   PubMed Web of Science ®Google Scholar
• Christensen LLH. Theoretical analysis of protein concentration determination using biosensor technology under conditions of partial mass transport limitation. Anal Biochem 1997;249:153-64
   PubMed Web of Science ®Google Scholar
• Fujimori K, Covell DC, Fletcher JE, Weinstein JN. Modeling analysis of the global and microscopic distribution of immunoglobulin G, F(ab′)2, and Fab in tumors. Cancer Res 1989;49:5656-63
   PubMed Web of Science ®Google Scholar
• Kenakin TP. Cellular assays as portals to seven-transmembrane receptor-based drug discovery. Nat Rev Drug Discov 2009;8:617-26
   PubMed Web of Science ®Google Scholar
• Hara M, Tozawa F, Itazaki K, Endothelin ET(B) receptors show different binding profiles in intact cells and cell membrane preparations. Eur J Pharmacol 1998;345:339-42
   PubMed Web of Science ®Google Scholar
• Smith C, Rahman T, Toohey N, Risperidone irreversibly binds to and inactivates the h5-HT7 serotonin receptor. Mol Pharmacol 2006;70:1264-70
   PubMed Web of Science ®Google Scholar
• Vauquelin G, Packeu A. Ligands, their receptors and plasma membranes. Mol Cell Endocrinol 2009;311:1-10
   PubMed Web of Science ®Google Scholar
• Vauquelin G. Determination of drug-receptor residence times by radioligand binding and functional assays: experimental strategies and physiological relevance. Med Chem Commun 2012, published online March 27 2012, doi:10.1039/C2MD20015E
   Google Scholar
• Hrabctova S, Nicholson C. Contribution of dead-space microdomains to tortuosity of brain extracellular space. Neurochem Int 2004;45:467-77
   PubMed Web of Science ®Google Scholar
• Dokoumetzidis A, Karalis V, Iliadis A, Macheras P. The heterogeneous course of drug transit through the body. Trends Pharmacol Sci 2004;25:140-6
   PubMed Web of Science ®Google Scholar
• Adam G, Delbruck M. Reduction of dimensionality in biological diffusion processes. In: Rich A, Davidson R, editors, Structural Chemistry and Molecular Biology. W.H. Freeman & Co., San Francisco; 1968. p. 198-215
   Google Scholar
• Langlois X, Megens A, Lavreysen H, Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. Poster, presented at the 23nd Congress of European College of Neuropsychopharmacology; Amsterdam, 9/2010. Eur Neuropsychopharmacol 2010;20:S502
   Web of Science ®Google Scholar
• Karbe H, Wienhard K, Haniacher K, Positron emission tomography with [18F]methylspipcronc demonstrates D2 dopamine receptor binding differences of clozapine and haloperidol. J Neural Transm 1991;86:163-73
   PubMed Web of Science ®Google Scholar
• Nordstrom A-L, Farde L, Halldin C. Time course of D2-dopamine receptor occupancy examined by PET after single oral doses of haloperidol. Psychopharmacology 1992;106:433-8
   PubMed Web of Science ®Google Scholar
• Leysen JE, Gommeren WJ. The dissociation of unlabelled dopamine antagonists and agonists from the dopamine D2-receptor. Implication of an original filter method. J Recept Res 1984;4:817-45
   PubMed Web of Science ®Google Scholar
• Vauquelin G, Morsing P, Fierens FLP, A two-state receptor model for the interaction between angiotensin II AT1 receptors and their non-peptide antagonists. Biochem Pharmacol 2001;61:277-84
   PubMed Web of Science ®Google Scholar
• Lazareno S, Birdsall NJM. Detection, quantitation and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors. Mol Pharmacol 1995;48:362-78
   PubMed Web of Science ®Google Scholar