Abstract
Over the past 20 years, studies of pharmacological receptors have undergone a veritable biochemical metamorphosis. The first thorough study of the binding of a pharmacologically active compound (atropine) to its receptor (muscarinic cholinergic: Paton and Rang, 1965) was soon followed by a multitude of studies of the binding of a variety of ligands to their putative receptors. Now, it is realized that receptor structures are dynamic cellular elements that display considerable structural and functional complexities. Thus, in order to measure the interaction of a ligand with its cell surface receptor, it is essential to have a grasp of the many variables that can affect such measurements. In this chapter, we attempt to provide a suitable context in which the measurements of ligand-receptor interactions can be interpreted, and we provide several models of receptor structure and function that have emerged over the past 10 years.
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References
Aguilera, C., Hauger, R. L., and Catt, K. J., 1978, Control of aldosterone secretion during sodium restriction: Adrenal receptor regulation and increased adrenal sensitivity to angiotensin II, Proc. Natl. Acad. Sci. U.S.A. 75: 959–979.
Ariens, E. J., 1954, Affinity and intrinsic activity in the theory of competitive inhibition, Arch. Int. Pharmacodyn. 99: 32–49.
Armstrong, G. D., and Hollenberg, M. D., 1982, Crosslink-labeling and proteolytic mapping of the human placental receptor for epidermal growth factor-urogastrone, Proc. Can. Fed. Biol. Soc. 25: 15.
Arunlakshana, O., and Schild, H. O., 1959, Some quantitative uses of drug antagonists, Br. J. Pharmacol. 14: 48–58.
Baker, J. B., Barsh, G. S., Carney, D. H., and Cunningham, D. D., 1978, Dexamethasone modulates binding and action of epidermal growth factor in serum-free cell culture, Proc. Natl. Acad. Sci. U.S.A. 75: 1882–1886.
Beck, J. S., and Goren, H. J., 1983, Simulation of association curves and “Scatchard” plots of binding reactions where ligand and receptor are degraded or internalized, J. Receptor Res. 3: 561–577.
Beck, J. S., and Goren, H. J., 1985, Determination of binding parameters in the presence of coupled reactions, Cell Biophys. 7: 31–42.
Beckman, B. S., and Hollenberg, M. D., 1979, Beta-adrenergic receptors and adenylate cyclase activity in rat reticulocytes and mature erythrocytes, Biochem. Pharmacol. 28: 239–248.
Bennett, G. V., O’Keefe, E.,and Cuatrecasas, P., 1975, The mechanism of action of cholera toxin and the mobile theory of hormone-receptor-adenylate cyclase interactions, Proc. Natl. Acad. Sci. U.S.A. 72: 33–37.
Berhanu, P., and Hollenberg, M. D., 1980, Epidermal growth factor-urogastrone receptor: Selective alteration in simian virus 40 transformed mouse fibroblasts, Arch. Biochem. Biophys. 203: 134–144.
Bhaumick, B., Goren, H. J., and Bala, R. M., 1981, Further characterization of human basic-somatomedin: Comparison with insulin-like growth factors I and II, Horm. Metab. Res. 13: 515–518.
Bilezikian, J. P., Speigel, A. M., Brown, E. M., and Aurbach, G. D., 1977a, Identification and persistence of beta-adrenergic receptors during maturation of the rat reticulocyte, Mol. Pharmacol. 13: 775–785.
Bilezikian, J. P., Speigel, A. M., Gammon, D. E., and Aurbach, G. D., 1977b, The role of guanyl nucleotides in the expression of catecholamine-responsive adenylate cyclase during maturation of the rat reticulocyte, Mol. Pharmacol. 13: 786–795.
Boeynaems, J. M., and Dumont, J. E., 1975, Quantitative analysis of the binding of ligands to their receptors, J. Cyclic Nucleotide Res. 1: 123–142.
Boeynaems, J. M., and Dumont, J. E., 1977, The two-step model of ligand-receptor interaction, Mol. Cell. Endocrinol. 7: 33–47.
Boeynaems, J. M., and Dumont, J. E., 1980, Outlines of Receptor Theory, Elsevier/North- Holland Biomedical Press, Amsterdam, New York.
Bokoch, G. M., Katada, T., Northup, J. K., Hewlett, E. L., and Gilman, A. G., 1983, Identification of the predominant substrate for ADP-ribosylation by islet activating protein, J. Biol. Chem. 258: 2072–2075.
Braestrup, C., and Nielsen, M., 1980, Benzodiazepine receptors, Drug Res. 30: 852–857.
Burgen, A. S. V., 1981, Conformational changes and drug action, Fed. Proc. 40: 2723–2728.
Burgen, A. S. V., Roberts, G. C. K., and Feeney, J., 1975, Binding of flexible ligands to macromolecules, Nature 253: 753–755.
Carpenter, G., 1981, Epidermal growth factor, in: Tissue Growth Factors, Handbook of Experimental Pharmacology ( R. Baserga, ed.), Springer-Verlag, New York, pp. 89–132.
Carpenter, G., and Cohen, S., 1976, 125I-Labeled human epidermal growth factor. Binding, internalization and degradation in human fibroblasts, J. Cell. Biol. 71: 159–171.
Catt, K. J., Harwood, J. P., Aguilera, G., and Dafau, M. L., 1979, Hormonal regulation of peptide receptors and target cell responses, Nature 280: 109–116.
Charness, M. D., Bylund, D. B., Beckman, B. S., Hollenberg, M. D., and Snyder, S. H., 1976, Independent variation of -adrenergic receptor binding and catecholamine-stimulated adenylate cyclase activity in rat erythrocytes, Life Sci. 19: 243–250.
Clark, A. J., 1926a, The reaction between acetylcholine and muscle cells, J. Physiol. (Lond. ) 61: 530–546.
Clark, A. J., 1926b, The antagonism of acetylcholine by atropine, J. Physiol. (Lond. ) 61: 541–556.
Clark, A. J., 1933, The Mode of Action of Drugs on Cells, Edward Arnold, London.
Cohen, S., Carpenter, G., and King, L., Jr., 1980, Epidermal growth factor-receptor-protein kinase interactions. Copurification of receptor and epidermal growth factor-enhanced phosphorylation activity, J. Biol. Chem. 255: 4834–4842.
Conn, P. M., Rogers, D. C., Stewart, J. M., Neidel, J., and Sheffield, T., 1982, Conversion of a gonadotropin-releasing hormone antagonist to an agonist, Nature 296: 653–655.
Conti-Tronconi, B. M., and Raftery, M. A., 1982, The nicotinic cholinergic receptor: Cor relation of molecular structure with functional properties, Annu. Rev. Biochem. 51:491– 530.
Cuatrecasas, P., 1974, Membrane receptors, Annu. Rev. Biochem. 43: 169–214.
Cuatrecasas, P., and Hollenberg, M. D., 1976, Membrane receptors and hormone action, Adv. Protein Chem. 30: 251–451.
Dahlquist, F. W., 1974, The quantitative interpretation of maximum Scatchard plots, FEBS Lett. 49: 267–268.
Das, M., 1980, Mitogenic hormone-induced intracellular message: Assay and partial char acterization of an activator of DNA replication induced by epidermal growth factor, Proc. Natl. Acad. Sci. U.S.A. 77: 112–116.
DeHaen, C., 1976, The non-stoichiometric floating receptor model for hormone-sensitive adenylate cyclase, J. Theor. Biol. 58: 383–400.
DeLean, A., and Rodbard, D., 1979, Kinetics of co-operative binding, in: The Receptors: A Comprehensive Treatise, Vol. 1 ( R. D. O’Brien, ed.), Plenum Press, New York, pp. 143–192.
DeLean, A., Munson, P. J., and Rodbard, D., 1979, Multisubsite receptors for multivalent ligands, Mol. Pharmacol. 15: 60–70.
DeLean, A., Hancock, A. A., and Lefkowitz, R. J., 1982, Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacologic receptor subtypes, Mol. Pharmacol. 21: 5–16.
DeLisi, C., and Chabay, R., 1979, The influence of cell surface receptor clustering on the thermodynamics of ligand binding and the kinetics of its dissociation, Cell. Biophys. 1: 117–131.
DeLisi, C., and Wiegel, F. W., 1981, Effect of nonspecific forces and finite receptor number on rate constants of ligand-cell brand receptor interactions, Proc. Natl. Acad. Sci. USA 78: 556920135572.
DeMeyts, P., 1976, Cooperative properties of hormone receptors in cell membranes, J. Supramol. Struct. 4: 201–218.
DeMeyts, P., and Roth, J., 1975, Cooperativity in ligand binding: A new graphic analysis, Biochem. Biophys. Res. Commun. 66: 1118–1125.
DeMeyts, P., Roth, J., Neville, D. M., Jr., Gavin, J. R. Ill, and Lesniak, M. A., 1973, Insulin interactions with its receptors: Experimental evidence for negative cooperativ ity, Biochem. Biophys. Res. Commun. 55: 154–161.
DeMeyts, P., van Obberghen, E., Roth, J., Wollmer, A., and Brandenburg, D., 1978, Map ping of the residues responsible for the negative cooperativity of the receptor binding region of insulin, Nature 273: 504–509.
Deranleu, D. A., 1969, Theory of the measurement of weak molecular complexes. I. General considerations, J. Am. Chem. Soc. 91: 4044–4049.
Deutsch, P. J., Wan, C. F., Rosen, O. M., and Rubin, C. S., 1983, Latent insulin receptors and possible receptor precursors in 3T3-L1 adipocytes, Proc. Natl. Acad. Sci. U.S.A. 80: 133–136.
Devreotes, P. N., and Fambrough, D. M., 1975, Acetylcholine receptor turnover in mem branes of developing muscle fibers, J. Cell Biol. 65: 335–358.
Devreotes, P. N., and Fambrough, D. M., 1976, Synthesis of the acetylcholine receptor by cultured chick myotubes and denervated mouse extensor digitorum longus muscles, Proc. Natl. Acad. Sci. USA 73: 161–164.
Devreotes, P. N, Gardner, J. M., and Fambrough, D. M., 1977, Kinetics of biosynthesis of acetylcholine receptor and subsequent incorporation into plasma membrane of cultured chick skeletal muscle, Cell 10: 365–373.
Dickson, R. B., Willingham, M. C., and Pastan, I., 1981, a2-macroglobulin adsorbed to colloidal gold: A new probe in the study of receptor-mediated endocytosis, J. Cell Biol. 89: 29–34.
Ebina, Y., Ellis, L., Jarnagin, K., Edery, M., Graf, L., Clauser, E., Ou, J.-h., Maslarz, F., Kan, Y. W., Goldfine, I. D., Roth, R. A, and Rutter, W. J., 1985, The human insulin receptor cDNA: the structural basis for hormone-activated transmembrane signalling, Cell 40: 747–758.
Edidin, M., Laganasky, Y., and Lardner, T. J., 1976, Measurement of membrane protein lateral diffusion in single cells, Science 191: 466–468.
Ehrlich, P., 1908, Nobel lecture on partial functions of the cell, in: The Collected Papers of P. Ehrlich, Vol. Ill ( F. Himmelweit, M. Marquardt, H. Dale, eds.), Pergamon Press, Oxford, p. 183.
Feldman, H. A., 1972, Mathematical theory of complex ligand-binding systems at equilib rium: Some methods for parameter fitting, Anal. Biochem. 48: 317–338.
Friedman, S. J., and Skehan, P., 1979, Morphological differentiation of human choriocar cinoma cells induced by methotrexate, Cancer Res. 39: 1960–1967.
Frye, L. D., and Edidin, M., 1970, The rapid intermixing of cell surface antigens after formation of mouse-human heterokaryons, J. Cell Sci. 7: 319–335.
Gavin, J. R., III, Roth, J., Neville, D. M., Jr., DeMeyts, P., and Buell, D. N., 1974, Insulin– dependent regulation of insulin receptor concentration. A direct demonstration in cell culture, Proc. Natl. Acad. Sci. U.S.A. 71: 84–88.
Gavish, M., Chang, R. S. L., and Snyder, S. H., 1979, Solubilization of histamine H-l, GAB A and benzodiazepine receptors, Life Sci. 25: 783–790.
Gilman, A. G., 1984, Guanine nucleotide-binding regulatory proteins and dual control of adenylate cyclase, J. Clin. Invest. 73: 1–4.
Goldstein, B., and Wiegel, F. W., 1983, The effect of receptor clustering on diffusion-limited forward rate constants, Biophys. J. 43: 121–125.
Goldstein, J. L., and Brown, M. S., 1975, Hyperlipidemia in coronary artery disease: A biochemical genetic appraoch, J. Lab. Clin. Med. 85: 15–28.
Goren, H. J., Bauce, L. G., and Vale, W., 1977, Forces and structural limitations of binding of thyrotrophin-releasing factor to the thyrotrophin-releasing receptor: The pyroglu- tamic acid moiety, Mol. Pharmacol. 16: 2265–2279.
Gregory, H., Taylor, C. L., and Hopkins, C. R., 1982, Leuteinizing hormone release from dissociated pituitary cells by dimerization of occupied LHRH receptors, Nature 300: 269–271.
Guidotti, A., Baraldi, M., and Costa, E., 1979, 1,4-Benzodiazepines and gamma-amino- butyric acid: Pharmacological and biochemical correlates, Pharmacology 19: 267–277.
Hartzell, H. C., and Fambrough, D. M., 1973, Acetylcholine receptor production and in corporation into membranes of developing muscle fibers, Dev. Biol. 30: 153–165.
Hauger, R. L., Aguilera, G., and Catt, K. J., 1978, Angiotensin II regulates its receptor sites in the adrenal glomerulosa zone, Nature 271: 176–177.
Helderman, J. H., and Strom, T. B., 1978a, Emergence of insulin receptors upon alloimmune T cells in the rat, J. Clin. Invest. 59: 334–338.
Helderman, H. J., and Strom, T. B., 1978b, Specific insulin binding site on T and B lym phocytes as a marker of cell activation, Nature 274: 62–63.
Herrup, K., and Shooter, E. M., 1975, Properties of the (3-nerve growth factor receptor in development, J. Cell. Biol. 67: 118–125.
Hillman, G. M., and Schlessinger, J., 1982, Lateral diffusion of epidermal growth factor complexed to its surface receptors does not account for the thermal sensitivity of patch formation and endocytosis, Biochemistry 21: 1667–1672.
Hock, R. A., Nexø, E., and Hollenberg, M. D., 1979, Isolation of the human placenta receptor for epidermal growth factor-urogastrone, Nature 277: 403–405.
Hollenberg, M. D., 1979, Membrane receptors and hormone action, Pharmacol. Rev. 30: 393–410.
Hollenberg, M. D, 1981, Membrane receptors and hormone action. I. New trends related to receptor structure and receptor regulation, Trends Pharmacol. Sci. 2: 320–323.
Hollenberg, M. D., 1982a, Membrane receptors and hormone action. II. New perspectives for receptor-modulated cell function, Trends Pharmacol. Sci. 3: 25–28.
Hollenberg, M. D., 1982b, Receptor-mediated phosphorylation reactions, Trends Pharmacol. Sci. 3: 271–273.
Hollenberg, M. D., 1984, Receptor models and the action of neurotransmitters and hor mones: Some new perspectives, in: Neurotransmitter Receptors, 2nd ed. ( H. I. Ya- mamura, S. J. Enna, and M. J. Kuhar, eds.), Raven Press, New York, pp. 1–39.
Hollenberg, M. D., and Armstrong, G., 1985, Epidermal growth factor-urogastrone and its receptor, in: Polypeptide Hormone Receptors ( B. Posner, ed.), Marcel Dekker, New York, pp. 201–206.
Hollenberg, M. D., and Cuatrecasas, P., 1974, Hormone receptors and membrane glyco proteins during in vitro transformation of lymphocytes, in: Control of Proliferation of Animal cells ( B. Clarkson and R. Baserga, eds.), Cold Spring Harbor Laboratory, Cold Spring Harbor, New York, pp. 423–434.
Hollenberg, M. D., and Cuatrecasas, P., 1979, Distinction of receptor from non-receptor interaction in binding studies: Historical and practical perspectives, in: The Receptors, A Comprehensive Treatise, Vol. I ( R. D. O’Brien, ed.), Plenum Press, New York, pp. 193–214.
Hollenberg, M. D, and Nexø, E., 1981, Receptor binding assays, in: Receptors and Recognition, Series B, Vol. II: Membrane Receptors: Methods for Purification and Characterization ( S. Jacobs and P. Cuatrecasas, eds.), Chapman and Hall, London, pp. 1–31.
Hollenberg, M. D., Barrett, J. C., Ts’o, P. O. P., and Berhanu, P., 1979, Selective reduction in receptors for epidermal growth factor-urogastrone in chemically transformed tu- morigenic Syrian hamster embryo fibroblasts, Cancer Res 39: 4166–4169.
Hollenberg, M. D., Nexø, E., Berhanu, P., and Hock, R. A., 1981, Phorbol ester and the selective modulation of receptors for epidermal growth factor-urogastrone, in: Receptor- Mediated Binding and Internalization of Toxins and Hormones ( J. L. Middlebrook and L. D. Kohn, eds.), Academic Press, New York, pp. 181–195.
Holley, R. W., Armour, R., Baldwin, J. H., Brown, K. D., and Yeh, Y.-C., 1977, Density- dependent regulation of growth of BSC-1 cell culture: Control of growth by serum factors, Proc. Natl. Acad. Sci. U.S.A. 74: 5046–5050.
Hopkins, C. R., Semoff, S., and Gregory, H., 1981, Regulation of gonadotropin secretion to the anterior pituitary, Phil. Trans R. Soc. Lond. [Biol. ] 296: 73–81.
Huang, D., and Cuatrecasas, P., 1975, Insulin-induced reduction of membrane receptor concentrations in isolated fat cells and lymphocytes: Independence from receptor oc cupation and possible relation to proteolytic activity of insulin, J. Biol. Chem. 250:8251– 8259.
Jacobs, S., and Cuatrecasas, P., 1976, The mobile receptor hypothesis and “cooperativity” of hormone binding application to insulin, Biochim. Biophys. Acta 433: 482–495.
Jacobs, S., and Cuatrecasas, P., 1977, The mobile receptor hypothesis for cell membrane receptor action, Trends Biochem. Sci. 2: 280–282.
Jacobs, S., and Cuatrecasas, P., 1983, The insulin receptor, Anna. Rev. Pharmacol. Toxicol. 23: 461–479.
Jacobs, S., Chang, K.-J., and Cuatrecasas, P., 1978, Antibodies to purified insulin receptor have insulin-like activity, Science 200: 1283–1284.
Jacobs, S., Kull, F. C., and Cuatrecasas, 1983, Monensin blocks the maturation of receptors for insulin and somatomedin C: Identification of receptor precursors, Proc. Natl. Acad. Sci. U.S.A. 80: 1228–1231.
Jarett, L., and Seals, J. R., 1979, Pyruvate dehydrogenase activation in adipocyte mito chondria by an insulin-generated mediator from muscle, Science 206: 1407–1408.
Jose, M. V., and Larralde, C., 1982, Alternative interpretation of unusual Scatchard plots: Contribution of interactions and heterogeneity, Math. Biosci. 58: 159–170.
Kahn, C. R., Baird, K. L., Flier, J. S., Grunfeld, C., Harmon, J. T., Harrison, L. C., Karlsson, F. A., Kasuga, M., King, G. L., Lang, U. C., Podskalny, J. M., and van Obberghen, E., 1981, Insulin receptor, receptor antibodies and the mechanism of insulin action, Recent Prog. Horm Res. 37: 477–538.
Kaplan, J., 1981, Polypeptide-binding membrane receptors: Analysis and classification, Sci ence 212: 14–20.
Karlin, A., 1980, Molecular properties of nicotinic acetylcholine receptors, in: The Cell Surface and Neuronal Function ( G. Poste, G. L. Nicolson, and C. W. Cotman, eds.), Elsevier/North-Holland Biomedical Press, Amsterdam, pp. 191–260.
Kasuga, M., Hedo, J. A., Yamada, K. M., and Kahn, C. R., 1982a, The structure of insulin receptor and its subunits. Evidence for multiple nonreduced forms and a 210,000 pos sible proreceptor, J. Biol. Chem. 257: 10392–10399.
Kasuga, M., Zick, Y., Blithe, D. L., Crettaz, M., and Kahn, C. R., 1982b, Insulin stimulates tyrosine phosphorylation of the insulin receptor in a cell-free system, Nature 298: 667–669.
King, G. L., Kahn, C. R., Rechler, M. M., and Nissley, S. P., 1980, Direct demonstration of separate receptors for growth and metabolic activities of insulin and multiplication- stimulating activity (an insulin-like growth factor) using antibodies to the insulin receptor, J. Clin. Invest. 66: 130–140.
King, G. L., Rechler, M. M., and Kahn, C. R., 1982, Interactions between the receptors for insulin and the insulin-like growth factors on adipocytes, J. Biol. Chem. 257:10001– 10006.
Klotz, I. M., 1982, Number of receptor sites from Scatchard graphs: Facts and fantasies, Science 217: 1247–1249.
Klotz, I. M., and Hunston, D. L., 1971, Properties of graphical representations of multiple classes of binding sites, Biochemistry 10: 3065–3069.
Kolterman, O. G., Insel, J., Saekow, M., and Olefsky, J. M., 1980, Mechanisms of insulin resistance in human obesity. Evidence for receptor and postreceptor defects, J. Clin. Invest. 65: 1271–1284.
Kolterman, O. G., Gray, R. S., Griffin, J., Burstein, P., Insel, J., Scarlett, J. A., and Olefsky, J. M., 1981, Receptor and postreceptor defects contribute to the insulin resistance in non-insulin-dependent diabetes mellitus, J. Clin. Invest. 68: 957–969.
Koppel, D. F., Axelrod, D., Schlessinger, J., Elson, E. L., and Webb, W. W., 1976, Dy namics of fluorescence marker concentration as a probe of mobility, Biophys. J. 16: 1315–1329.
Koren, R., and Hammes, G. G., 1976, A kinetic study of protein-protein interactions, Biochemistry 15: 1165–1175.
Krug, U., Krug, F., and Cuatrecasas, P., 1972, Emergence of insulin receptors on human lymphocytes during in vitro transformation, Proc. Natl. Acad. Sci. U.S.A. 69: 2604–2608.
Krupp, M. N., Connolly, D. T., and Lane, M. D., 1982, Synthesis, turnover, and down- regulation of epidermal growth factor receptors in human A431 epidermoid carcinoma cells and skin fibroblasts, J. Biol. Chem. 257: 11489–11496.
Labrie, F., Belanger, A., Cusan, L., Seguin, C., Pelletier, G., Kelly, P. A., Reeves, J. J., Lefebvre, F. A., Lemay, A., Gourdeau, Y., and Raynaud, J.-P., 1980, Antifertility effects of LHRH agonists in the male, J. Androlog. 1: 209–228.
Lamb, J. E., Ray, F., Ward, J. H., Kushner, J. P., and Kaplan, J., 1983, Internalization and subcellular localization of transferrin and transferrin receptors in HeLa cells, J. Biol. Chem. 258: 8751–8758.
Langley, J. N., 1906, On nerve endings and on special excitable substances, Proc. R. Soc. Lond. [Biol. ] 78: 170–194.
Larner, J., Galasko, G., Cheng, K., DePaoli-Roach, A. A., Huang, L., Daggy, P., and Kellogg, J., 1979, Generation by insulin of a chemical mediator that controls phos- phorylation-dephosphorylation, Science 206: 1408–1410.
Lefebvre, F. A., Reeves, J. J., Seguin, C., Massicot, J., and Labrie, F., 1980, Specific binding of a potent LHRH agonist in rat testis, Mol. Cell. Endocrinol. 20: 127–134.
Lefkowitz, R., 1978, Identification and regulation of alpha and beta-adrenergic receptors, Fed. Proc. 37: 123–129.
Lin, M. C., and Beckner, S. K., 1983, Induction of hormone receptors and responsiveness during cellular differentiation, in: Current Topics in Membranes and Transport, Vol. 18 ( A. Kleinzeller, ed.), Academic Press, New York, pp. 287–315.
Linsley, P. S., and Fox, C. F., 1980, Controlled proteolysis of EGF receptors: Evidence for transmembrane distribution of the EGF binding and phosphate acceptor sites, J. Supramol. Struct. 14: 461–471.
Livingston, J. N., Purvis, B. J., and Lockwood, D. H., 1978, Insulin-dependent regulation of the insulin-sensitivity of adipocytes, Nature 273: 394–396.
Mahoney, M. S., and Rosenberg, L. E., 1975, Inborn errors of cobalamine metabolism, in: Cobalamine Biochemistry and Pathophysiology ( B. M. Babior, ed.), John Wiley & Sons, New York, pp. 369–402.
Maxfield, F. R., Schlessinger, J., Schechter, Y., Pastan, I., and Willingham, M. C., 1978, Insulin, epidermal growth factor and a2-macroglobulin rapidly collect in the same patches on the surface of cultured fibroblasts and are internalized together, Cell 14:805- 810.
Mayes, E. L. V., and Waterfield, M. D., 1984, Biosynthesis of the epidermal growth factor receptor in A431 cells, EMBO J. 3: 531–537.
Minton, A. P., 1981, The bivalent ligand hypothesis: A quantitative model for hormone action, Mol. Pharmacol. 19: 1–14.
Muller, W. E., 1981, The benzodiazepine receptor, Pharmacology 22: 153–161.
Munson, P. J., Rodbard, D., and Klotz, I. M., 1983, Number of receptor sites from Scatchard and Klotz graphs: A constructive critique, Science 220: 979–981.
Nexø, E., 1978, Transcobalamin I and other receptor-binders: Purification, structural, spec tral, and physiologic studies, Scand. J. Haematol. 20: 221–236.
Nexø, E., Hollenberg, M. D., and Oleson, H., 1979, Solubilization and characterization of the transcobalamin-II acceptor from human placenta and rabbit liver, in: Vitamin Bi2 ( B. Zagalak and W. Friedrich, eds.), Walter de Gruyter & Co., New York, pp. 843–850.
Nexø, E., Hollenberg, M. D., Figueroa, A., and Pratt, A. M., 1980, Detection of epidermal growth factor-urogastrone and its receptor during fetal mouse development, Proc. Natl. Acad. Sci. U.S.A. 77: 2782–2785.
Nimrod, A., Tsafriri, A., and Linder, H. R., 1977, In vitro induction of binding sites for hCG in rat granulosa cells by FSH, Nature 267: 632 - 633.
O’Connor-McCourt, M., and Hollenberg, M. D., 1983, Receptors, acceptors, and the action of polypeptide hormones: Illustrative studies with epidermal growth factor (urogas-trone), Can. J. Biochem. Cell. Biol. 61: 670 - 682.
Oppenheimer, C. L., Pessin, J. E., Massague, J., Gitomer, W., and Czech, M. P., 1983, Insulin action rapidly modulates the apparent affinity of the insulin-like growth factor II receptor, J. Biol. Chem. 258: 4824 - 4833.
Parsons, D. L., and Vollner, J. J., 1978a, Theoretical models for cooperative binding. 1. One-site creator of binding sites. Math. Biosci. 41: 189 - 215.
Parsons, D. L., and Vollner, J. J., 1978b, Theoretical models for cooperative binding. II. Two-site creator of sites and destruction of pre-existing sites, Math. Biosci. 41:217¬230.
Parsons, D. L., and Vollner, J. J., 1978c, Theoretical models for cooperative binding. III. Positive and negative site-site cooperativity, Math. Biosci. 41: 231 - 240.
Pastan, I. H., and Willingham, M. C., 1981, Journey to the center of the cell: Role of the receptosome, Science 214: 504 - 509.
Paton, W. D. M., 1961, A theory of drug action based on the rate of drug-receptor combination, Proc. R. Soc. Lond. [Biol.] 154: 21 - 69.
Paton, W. D. M., and Rang, H. P., 1965, The uptake of atropine and related drugs by intestinal smooth muscle of the guinea pig in relation to acetylcholine receptors, Proc. R. Soc. Lond [Biol] 163: 1 - 44.
Perelson, A. S., and DeLisi, C., 1980, Receptor clustering on a cell surface. 1. Theory of receptor cross-linking by ligands bearing two chemically identical functional groups, Math. Biosci. 48: 71 - 110.
Peters, F., and Pingoud, V. A., 1982, A critical interpretation of experiments on binding of peptide hormones to specific receptors by computer modelling, Biochem. Biophys. Acta 714: 442 - 444.
Pollet, R. J., Standaert, M. L., and Haase, B. A., 1977, Insulin binding to the human lym-phocyte receptor: Evaluation of the negative cooperativity model, J. Biol. Chem. 252: 5828 - 5834.
Posner, B. I., Kelley, P. A., and Friesen, H. G., 1974, Induction of lactogenic receptor in rat liver: Influence of estrogen and the pituitary, Proc. Natl. Acad. Sci. U.S.A. 71:2407¬2410.
Posner, B. I., Kelley, P. A., and Friesen, H. J., 1975, Prolactin receptor in rat liver: Possible induction by prolactin, Science 188: 57 - 59.
Reed, B. C., and Lane, M. D., 1980, Insulin receptor synthesis and turnover in differentiating 3T3-LI preadipocytes, Proc. Natl. Acad. Sci. U.S.A. 77: 285 - 289.
Reed, B. C., Ronnett, G. V., Clements, P. R., and Lane, M. D., 1981, Regulation of insulin receptor metabolism. Differentiation-induced alteration of receptor synthesis and deg-radation, J. Biol. Chem. 256: 3917 - 3925.
Rescigno, A., Beck, J. S., and Goren, H. J., 1982, Determination of dependence of binding parameters on receptor occupancy, Bull. Math. Biol. 44: 477 - 489.
Roberts, A. B., Frolik, C. A., Anzano, M. A., and Sporn, M. B., 1983, Transforming growth factors from neoplastic and non-neoplastic tissues. Fed. Proc. 42: 2621 - 2626.
Rodbard, D., 1979, Negative cooperativity: A positive finding? Am. J. Physiol. 237: E203 - E205.
Rodbard, D., and Feldman, H. A., 1975, Theory of protein-ligand interaction, Methods Enzymol 36: 3 - 16.
Rodbell, M., 1980, The role of hormone receptors and GTP-regulatory proteins in membrane transduction, Nature 284: 17–22.
Rosen, O. M., Herrera, R., Olowe, Y., Petruzzelli, L. M., and Cobb, M. H., 1983, Phos phorylation activates the insulin receptor tyrosine protein kinase, Proc. Natl. Acad. Sci. U.S.A. 80: 3237–3240.
Roth, R. A., and Cassell, D. J., 1983, Evidence that the insulin receptor is a protein kinase, Science 219: 299–301.
Roth, R. A., Cassell, D. J., Wong, K. Y., Maddux, B. A., and Goldfine, I. D., 1982, Mon oclonal antibodies to the human insulin receptor block insulin binding and inhibit insulin action, Proc. Natl. Acad. Sci. U.S.A. 79: 7312–7316.
Saltiel, A. R., Siegel, M. I., Jacobs, S., and Cuatrecasas, P., 1982, Putative mediators of insulin action: Regulation of pyruvate dehydrogenase and adenylate cyclase activities, Proc. Natl. Acad. Sci. U.S.A. 79: 3513–3517.
Scatchard, G., 1949, The attraction of proteins for small molecules and ions, Ann. N.Y. Acad. Sci. 51: 660–672.
Schafer, D. E., 1983, Measurement of receptor-ligand binding: Theory and practice, in: Tracer Kinetics and Physiological Modeling ( R. M. Lambrecht and A. Rescigno, eds.), Springer-Verlag, Berlin, p. 445–507.
Schlessinger, J., Schechter, Y., Willingham, M. C., and Pastan, I., 1978, Direct visualization of binding, aggregation and internalization of insulin and epidermal growth factor on living fibroblastic cells, Proc. Natl. Acad. Sci. U.S.A. 75: 2659–2663.
Schreiber, A. B., Liberman, T. A., Lax, I., Yarden, Y., and Schlessinger, J., 1983, Biological role of epidermal growth factor-receptor clustering, J. Biol. Chem. 258: 846–853.
Seals, J. R., and Czech, M. P., 1980, Evidence that insulin activates an intrinsic plasma membrane protease in generating a secondary chemical mediator, J. Biol. Chem. 255: 6529–6531.
Seligman, P. A., and Allan, R. H., 1978, Characterization of the receptor for transcobalamin II isolated from human placenta, J. Biol. Chem. 253: 1766–1772.
Schechter, Y., Hernaez, L., Schlessinger, J., and Cuatrecasas, P., 1979, Local aggregation of hormone-receptor complexes is required for activation by epidermal growth factor, Nature 278: 835–838.
Sheppard, J., 1977, Catecholamine hormone receptor differences identified on 3T3 and sim ian virus transformed 3T3 cells, Proc. Natl. Acad. Sci. U.S.A. 73: 1091–1094.
Smith, R. L., and Jarett, L., 1984, Tissue specific variations in insulin receptor dynamics: A high resolution ultrastrucutral and biochemical approach, in: Insulin, Its Receptor and Diabetes ( M. D. Hollenberg, ed.), Marcel Dekker, New York, pp. 105–139.
Soloff, M., 1975, Uterine receptor for oxytocin: Effects of estrogen, Biochem. Biophys. Res. Commun. 65: 205–212.
Stephenson, R. P., and Barlow, R. B., 1970, Concepts of drug action, quantitative phar macology and biological assay, in: A Companion to Medical Studies, Vol. 2 (R. Passmore and J. S. Robson, eds.), Blackwell, London, pp. 3. 1–3. 19.
Stevens, C. F., 1982, The acetylcholine receptor cloned east and west; and..., Nature 299: 776; 300: 110.
Stevens, R. L., Austen, K. F., and Nissley, S. P., 1983, Insulin-induced increase in insulin binding to cultured chondrosarcoma chondrocytes, J. Biol. Chem. 258: 2940–2944.
Tallman, J. F., Smith, C. C., and Henneberry, R. C., 1977, Induction of functional (3- adrenergic receptors in HeLa cells, Proc. Natl. Acad. Sci. U.S.A. 73: 873–877.
Taylor, P., Brown, R. D., and Johnson, D. A., 1983, The linkage betweeen ligand occupation and response of the nicotinic acetylcholine receptor, Curr. Top. Membr. Transp. 18: 407–444.
Thakur, A. K., Jaffe, M. L., and Rodbard, D., 1980, Graphical analysis of ligand-binding systems: Evaluation by Monte Carlo studies, Anal. Biochem. 107: 279–295.
Thomopoulos, P., Kosmakos, F. C., Pastan, I., and Lovelace, E., 1977, Cyclic AMP in creases the concentration of insulin receptors in cultured fibroblasts and lymphocytes, Biochem. Biophys. Res. Commun. 73: 246–252.
Thompson, C. J., and Klotz, L. M., 1971, Macromolecule-small molecule interactions: Ana lytical and graphical re-examination, Arch. Biochem. Biophys. 147: 178–185.
Todaro, G. J., Delarco, J. E., and Cohen, S., 1976, Transformation by murine and feline sarcoma viruses specifically blocks binding of epidermal growth factor to cells, Nature 264: 26–31.
Tolkovsky, A. M., and Levitzki, A., 1978, Mode of coupling between the (3-adrenergic receptor and adenylate cyclase in turkey erythrocytes, Biochemistry 17: 3795–3810.
Triggle, D. J., 1982, Receptor recruitment and cryptic signals, Trends Pharmacol. Sci. 3:273– 274.
Triggle, D. J., and Triggle, C. R., 1976, Chemical Pharmacology of the Synapse, Chapter 2, Academic Press, New York.
Ullrich, A., Coussens, L., Hayflick, J. S., Dull, T. J., Gray, A., Tam, A. W., Lee, J., Yarden, Y., Libermann, T. A., Schlessinger, J., Downward, J., Mayes, E. L. V., Whit tle, N., Waterfield, M. D., and Seeburg, P. H., 1984, Human epidermal growth factor receptor cDNA sequence and aberrant expression of the amplified gene in A431 epi dermoid carcinoma cells, Nature 309: 418–425.
Ulrich, A., Bell, J. R., Chen, E. Y., Herrara, R., Petruzzelli, L. M., Dull, T. J., Gray, A., Coussens, L., Liao, Y.-C., Tsubokawa, M., Mason, A., Seeburg, P. H., Grunfeld, C., Rosen, O. M., and Ramachandran, J., 1985, Human insulin receptor and its relationship to the tyrosine kinase family of oncogenes, Nature 313: 756–761.
Valentine, K. A., and Hollenberg, M. D., 1984, Membrane receptors and hormone action, in: Cell Biology of the Secretory Process ( M. Cantin, Ed.), S. Karger, New York, pp. 1–5.
Van Obberghen, E., and Kowalski, A., 1982, Phosphorylation of the hepatic insulin receptor. Stimulating effect of insulin on intact cells and in a cell-free system, FEBS Lett. 143: 179–182.
Varga, J. M., Dipasquale, A., Pawelek, J., McGuire, J. S., and Lerner, A. B., 1974, Reg ulation of melanocyte stimulating hormone action at the receptor level: Discontinuous binding of hormone to synchronized mouse melanoma cells during the cell cycle, Proc. Natl. Acad. Sci. U.S.A. 71: 1590–1593.
Weber, G., 1975, Energetics of ligand binding to proteins, Adv. Protein Chem. 29: 1.
Willingham, M. C., and Pastan, I., 1978, The visualization of fluorescent proteins in living cells by video intensification microscopy (VIM), Cell 13: 501–507.
Wrann, M., Fox, C. F., and Ross, R., 1980, Modulation of epidermal growth factor receptors on 3T3 cells by platelet-derived growth factor, Science 210: 1363–1365.
Yamada, S., Yamamura, H. I., and Roeske, W. R., 1980, The regulation of cardiac ar adrenergic receptors by guanine nucleotides and by muscarinic cholinergic agonists, Eur. J. Pharmacol. 63: 239–241.
Yankner, B. A., and Shooter, E. M., 1982, The biology of mechanism of action of nerve growth factor, Annu. Rev. Biochem. 51: 845–868.
Yarden, Y., Schreiber, A. B., and Schlessinger, J., 1982, A non-mitogenic analogue of epidermal growth factor induces early responses mediated by epidermal growth factor, J. Cell. Biol. 92: 687–693.
Yip, C. C., and Moule, M. L., 1983, Structure of the insulin receptor of rat adipocytes: The three interconvertable redox forms, Diabetes 32: 760–767.
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Hollenberg, M.D., Goren, H.J. (1985). Ligand-Receptor Interactions at the Cell Surface. In: Poste, G., Crooke, S.T. (eds) Mechanisms of Receptor Regulation. New Horizons in Therapeutics. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-2131-6_18
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