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Ligand-Receptor Interactions at the Cell Surface

  • Chapter
Mechanisms of Receptor Regulation

Part of the book series: New Horizons in Therapeutics ((NHTH))

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.

    Google Scholar 

  • Ariens, E. J., 1954, Affinity and intrinsic activity in the theory of competitive inhibition, Arch. Int. Pharmacodyn. 99: 32–49.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Arunlakshana, O., and Schild, H. O., 1959, Some quantitative uses of drug antagonists, Br. J. Pharmacol. 14: 48–58.

    CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • Beck, J. S., and Goren, H. J., 1985, Determination of binding parameters in the presence of coupled reactions, Cell Biophys. 7: 31–42.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • Boeynaems, J. M., and Dumont, J. E., 1977, The two-step model of ligand-receptor interaction, Mol. Cell. Endocrinol. 7: 33–47.

    PubMed  CAS  Google Scholar 

  • Boeynaems, J. M., and Dumont, J. E., 1980, Outlines of Receptor Theory, Elsevier/North- Holland Biomedical Press, Amsterdam, New York.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Braestrup, C., and Nielsen, M., 1980, Benzodiazepine receptors, Drug Res. 30: 852–857.

    CAS  Google Scholar 

  • Burgen, A. S. V., 1981, Conformational changes and drug action, Fed. Proc. 40: 2723–2728.

    PubMed  CAS  Google Scholar 

  • Burgen, A. S. V., Roberts, G. C. K., and Feeney, J., 1975, Binding of flexible ligands to macromolecules, Nature 253: 753–755.

    PubMed  CAS  Google Scholar 

  • Carpenter, G., 1981, Epidermal growth factor, in: Tissue Growth Factors, Handbook of Experimental Pharmacology ( R. Baserga, ed.), Springer-Verlag, New York, pp. 89–132.

    Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Clark, A. J., 1926a, The reaction between acetylcholine and muscle cells, J. Physiol. (Lond. ) 61: 530–546.

    CAS  Google Scholar 

  • Clark, A. J., 1926b, The antagonism of acetylcholine by atropine, J. Physiol. (Lond. ) 61: 541–556.

    Google Scholar 

  • Clark, A. J., 1933, The Mode of Action of Drugs on Cells, Edward Arnold, London.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Cuatrecasas, P., 1974, Membrane receptors, Annu. Rev. Biochem. 43: 169–214.

    PubMed  CAS  Google Scholar 

  • Cuatrecasas, P., and Hollenberg, M. D., 1976, Membrane receptors and hormone action, Adv. Protein Chem. 30: 251–451.

    PubMed  CAS  Google Scholar 

  • Dahlquist, F. W., 1974, The quantitative interpretation of maximum Scatchard plots, FEBS Lett. 49: 267–268.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • DeHaen, C., 1976, The non-stoichiometric floating receptor model for hormone-sensitive adenylate cyclase, J. Theor. Biol. 58: 383–400.

    CAS  Google Scholar 

  • 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.

    Google Scholar 

  • DeLean, A., Munson, P. J., and Rodbard, D., 1979, Multisubsite receptors for multivalent ligands, Mol. Pharmacol. 15: 60–70.

    CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • DeMeyts, P., 1976, Cooperative properties of hormone receptors in cell membranes, J. Supramol. Struct. 4: 201–218.

    Google Scholar 

  • DeMeyts, P., and Roth, J., 1975, Cooperativity in ligand binding: A new graphic analysis, Biochem. Biophys. Res. Commun. 66: 1118–1125.

    CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • Deranleu, D. A., 1969, Theory of the measurement of weak molecular complexes. I. General considerations, J. Am. Chem. Soc. 91: 4044–4049.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Devreotes, P. N., and Fambrough, D. M., 1975, Acetylcholine receptor turnover in mem branes of developing muscle fibers, J. Cell Biol. 65: 335–358.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Edidin, M., Laganasky, Y., and Lardner, T. J., 1976, Measurement of membrane protein lateral diffusion in single cells, Science 191: 466–468.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Feldman, H. A., 1972, Mathematical theory of complex ligand-binding systems at equilib rium: Some methods for parameter fitting, Anal. Biochem. 48: 317–338.

    PubMed  CAS  Google Scholar 

  • Friedman, S. J., and Skehan, P., 1979, Morphological differentiation of human choriocar cinoma cells induced by methotrexate, Cancer Res. 39: 1960–1967.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Gilman, A. G., 1984, Guanine nucleotide-binding regulatory proteins and dual control of adenylate cyclase, J. Clin. Invest. 73: 1–4.

    PubMed  CAS  Google Scholar 

  • Goldstein, B., and Wiegel, F. W., 1983, The effect of receptor clustering on diffusion-limited forward rate constants, Biophys. J. 43: 121–125.

    PubMed  CAS  Google Scholar 

  • Goldstein, J. L., and Brown, M. S., 1975, Hyperlipidemia in coronary artery disease: A biochemical genetic appraoch, J. Lab. Clin. Med. 85: 15–28.

    PubMed  CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Guidotti, A., Baraldi, M., and Costa, E., 1979, 1,4-Benzodiazepines and gamma-amino- butyric acid: Pharmacological and biochemical correlates, Pharmacology 19: 267–277.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Herrup, K., and Shooter, E. M., 1975, Properties of the (3-nerve growth factor receptor in development, J. Cell. Biol. 67: 118–125.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Hollenberg, M. D., 1979, Membrane receptors and hormone action, Pharmacol. Rev. 30: 393–410.

    Google Scholar 

  • 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.

    CAS  Google Scholar 

  • Hollenberg, M. D., 1982a, Membrane receptors and hormone action. II. New perspectives for receptor-modulated cell function, Trends Pharmacol. Sci. 3: 25–28.

    CAS  Google Scholar 

  • Hollenberg, M. D., 1982b, Receptor-mediated phosphorylation reactions, Trends Pharmacol. Sci. 3: 271–273.

    CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Jacobs, S., and Cuatrecasas, P., 1976, The mobile receptor hypothesis and “cooperativity” of hormone binding application to insulin, Biochim. Biophys. Acta 433: 482–495.

    PubMed  CAS  Google Scholar 

  • Jacobs, S., and Cuatrecasas, P., 1977, The mobile receptor hypothesis for cell membrane receptor action, Trends Biochem. Sci. 2: 280–282.

    CAS  Google Scholar 

  • Jacobs, S., and Cuatrecasas, P., 1983, The insulin receptor, Anna. Rev. Pharmacol. Toxicol. 23: 461–479.

    CAS  Google Scholar 

  • Jacobs, S., Chang, K.-J., and Cuatrecasas, P., 1978, Antibodies to purified insulin receptor have insulin-like activity, Science 200: 1283–1284.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Jose, M. V., and Larralde, C., 1982, Alternative interpretation of unusual Scatchard plots: Contribution of interactions and heterogeneity, Math. Biosci. 58: 159–170.

    CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Kaplan, J., 1981, Polypeptide-binding membrane receptors: Analysis and classification, Sci ence 212: 14–20.

    CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Klotz, I. M., 1982, Number of receptor sites from Scatchard graphs: Facts and fantasies, Science 217: 1247–1249.

    PubMed  CAS  Google Scholar 

  • Klotz, I. M., and Hunston, D. L., 1971, Properties of graphical representations of multiple classes of binding sites, Biochemistry 10: 3065–3069.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Koren, R., and Hammes, G. G., 1976, A kinetic study of protein-protein interactions, Biochemistry 15: 1165–1175.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Langley, J. N., 1906, On nerve endings and on special excitable substances, Proc. R. Soc. Lond. [Biol. ] 78: 170–194.

    CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Lefkowitz, R., 1978, Identification and regulation of alpha and beta-adrenergic receptors, Fed. Proc. 37: 123–129.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Livingston, J. N., Purvis, B. J., and Lockwood, D. H., 1978, Insulin-dependent regulation of the insulin-sensitivity of adipocytes, Nature 273: 394–396.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    Google Scholar 

  • Mayes, E. L. V., and Waterfield, M. D., 1984, Biosynthesis of the epidermal growth factor receptor in A431 cells, EMBO J. 3: 531–537.

    PubMed  CAS  Google Scholar 

  • Minton, A. P., 1981, The bivalent ligand hypothesis: A quantitative model for hormone action, Mol. Pharmacol. 19: 1–14.

    PubMed  CAS  Google Scholar 

  • Muller, W. E., 1981, The benzodiazepine receptor, Pharmacology 22: 153–161.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Nexø, E., 1978, Transcobalamin I and other receptor-binders: Purification, structural, spec tral, and physiologic studies, Scand. J. Haematol. 20: 221–236.

    Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    CAS  Google Scholar 

  • Pastan, I. H., and Willingham, M. C., 1981, Journey to the center of the cell: Role of the receptosome, Science 214: 504 - 509.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Posner, B. I., Kelley, P. A., and Friesen, H. J., 1975, Prolactin receptor in rat liver: Possible induction by prolactin, Science 188: 57 - 59.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Rodbard, D., 1979, Negative cooperativity: A positive finding? Am. J. Physiol. 237: E203 - E205.

    PubMed  CAS  Google Scholar 

  • Rodbard, D., and Feldman, H. A., 1975, Theory of protein-ligand interaction, Methods Enzymol 36: 3 - 16.

    PubMed  CAS  Google Scholar 

  • Rodbell, M., 1980, The role of hormone receptors and GTP-regulatory proteins in membrane transduction, Nature 284: 17–22.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Roth, R. A., and Cassell, D. J., 1983, Evidence that the insulin receptor is a protein kinase, Science 219: 299–301.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Scatchard, G., 1949, The attraction of proteins for small molecules and ions, Ann. N.Y. Acad. Sci. 51: 660–672.

    CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    Google Scholar 

  • Soloff, M., 1975, Uterine receptor for oxytocin: Effects of estrogen, Biochem. Biophys. Res. Commun. 65: 205–212.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Stevens, C. F., 1982, The acetylcholine receptor cloned east and west; and..., Nature 299: 776; 300: 110.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • Thompson, C. J., and Klotz, L. M., 1971, Macromolecule-small molecule interactions: Ana lytical and graphical re-examination, Arch. Biochem. Biophys. 147: 178–185.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Triggle, D. J., 1982, Receptor recruitment and cryptic signals, Trends Pharmacol. Sci. 3:273– 274.

    Google Scholar 

  • Triggle, D. J., and Triggle, C. R., 1976, Chemical Pharmacology of the Synapse, Chapter 2, Academic Press, New York.

    Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    Google Scholar 

  • 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.

    PubMed  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Weber, G., 1975, Energetics of ligand binding to proteins, Adv. Protein Chem. 29: 1.

    PubMed  CAS  Google Scholar 

  • Willingham, M. C., and Pastan, I., 1978, The visualization of fluorescent proteins in living cells by video intensification microscopy (VIM), Cell 13: 501–507.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • Yankner, B. A., and Shooter, E. M., 1982, The biology of mechanism of action of nerve growth factor, Annu. Rev. Biochem. 51: 845–868.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

  • 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.

    PubMed  CAS  Google Scholar 

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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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