Skip to main content

Receptor Regulation

Problems and Perspectives

  • Chapter
Mechanisms of Receptor Regulation

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

Abstract

It is now well accepted that the interaction of ligands, especially peptide hormones, with their surface receptor is the initial step in a chain of events that leads to subsequent biological responses. Therefore, the regulation of surface receptors is crucial as a control point for these responses. Current investigation of hormone action must focus, in part, on regulation of receptors, which goes beyond the simple binding studies of the past decade or more that opened the field to further exploration.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 54.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Ackerman, G. A., Yang, J., and Wolken, K.W., 1983, Differential surface labeling and internalization of glucagon by peripheral leukocytes, J. Histochem. Cytochem. 31: 433–440.

    Article  PubMed  CAS  Google Scholar 

  • Amatruda, J. M., Newmeyer, H. W., and Chang, C. L., 1982, Insulin-induced alterations in insulin binding and insulin action in primary cultures of rat hepatocytes, Diabetes 31: 145–148.

    Article  PubMed  CAS  Google Scholar 

  • Anderson, R. G. W., Goldstein, J. L., and Brown, M. S., 1976, Localization of low density lipoprotein receptors on plasma membrane of normal human fibroblasts and their absence in cells from a familial hypercholesterolemia homozygote, Proc. Natl. Acad. Sci., U.S.A. 73: 2434–2438.

    Article  PubMed  CAS  Google Scholar 

  • Anderson, R. G. W., Goldstein, J. L., and Brown, M. S., 1977, A mutation that impairs the ability of lipoprotein receptors to localise in coated pits on the cell surface of human fibroblasts, Nature 270: 695–699.

    Article  PubMed  CAS  Google Scholar 

  • Balkin, M. S., and Sonenberg, M., 1981, Hormone-induced homologous and heterologous desensitization in the rat adipocyte, Endocrinology 109: 1176–1183.

    Article  PubMed  CAS  Google Scholar 

  • Bergmann, J. S., and Carney, D. H., 1982, Receptor-bound thombin is not internalized through coated pits in mouse embryo cells, J. Cell. Biochem. 20: 247–258.

    Article  PubMed  CAS  Google Scholar 

  • Berhanu, P., and Olefsky, J. M., 1982, Photoaffinity labeling of insulin receptors in viable cultured human lymphocytes, demonstration of receptor shedding and degradation, Diabetes 31: 410–417.

    Article  PubMed  CAS  Google Scholar 

  • Bourguignon, L. Y. W., and Singer, S. J., 1977, Transmembrane interactions and the mechanism of capping of surface receptors by their specific ligands, Proc. Natl. Acad. Sci. U.S.A. 74: 5031–5035.

    Article  PubMed  CAS  Google Scholar 

  • Brown, M. S., and Goldstein, J. L., 1979, Receptor-mediated endocytosis: insights from the lipoprotein receptor system, Proc. Natl. Acad. Sci. U.S.A. 76: 3330–3337.

    Article  PubMed  CAS  Google Scholar 

  • Carney, D. H., and Bergmann, J. S., 1982,125I-Thrombin binds to clustered receptors on noncoated regions of mouse embryo cell surfaces, J. Cell Biol. 95: 697–703.

    Article  PubMed  CAS  Google Scholar 

  • Carpenter, G., King, L., Jr., and Cohen, S., 1978, Epidermal growth factor stimulates phosphorylation in membrane preparations in vitro, Nature 276: 409–410.

    Article  PubMed  CAS  Google Scholar 

  • Czech, M. P., Oppenheimer, C. L., and Massague, J., 1983, Interrelationships among receptor structures for insulin and peptide growth factors, Fed. Proc. 42: 2598–2601.

    PubMed  CAS  Google Scholar 

  • Davies, A. O., and Lefkowitz, R. J., 1981, Regulation of adrenergic receptors, in: Receptors and Recognition, series B, Vol. 13 ( R. J. Lefkowitz, ed.), Chapman and Hall, New York, pp. 83–121.

    Google Scholar 

  • DeMeyts, P., 1976, Cooperative properties of hormone receptors in cell membranes, J. Supramol. Struct. 4: 241–258.

    Article  CAS  Google Scholar 

  • Domnina, L. V., Pletyushkina, O. Y., Vasiliev, J. M., and Gelfand, I. M., 1977, Effects of antitubulins on the redistribution of crosslinked receptors on the surface of fibroblasts and epithelial cells, Proc. Natl. Acad. Sci., U.S.A. 74: 2865–2868.

    Article  PubMed  CAS  Google Scholar 

  • Galbraith, R. A., Tucker, S., Wise, C., and Buse, M. G., 1980, Insulin binding to erythroblastic leukemic cells is decreased by insulin and increased by amino acids, Biochem. Biophys, Res. Commun. 96: 1434–1440.

    Article  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 concentrations: A direct demonstration in cell culture, Proc. Natl. Acad. Sci. U.S.A. 71: 84–88.

    Article  PubMed  CAS  Google Scholar 

  • Goldfine, I. D., and Smith, G. J., 1976, Binding of insulin to isolated nuclei, Proc. Natl. Acad. Sci. U.S.A. 73: 1427–1431.

    Article  PubMed  CAS  Google Scholar 

  • Gorden, P., Carpentier, J.-L, Cohen, S., and Orci, L., 1978, Epidermal growth factor: Morphological demonstration of binding, internalization, and lysosomal association in human fibroblasts, Proc. Natl. Acad. Sci. U.S.A. 75: 5025–5029.

    Article  PubMed  CAS  Google Scholar 

  • Grunfeld, C., Van Obberghen, E., Karlsson, F. A., and Kahn, C. R., 1980, Antibody-induced desensitization of the insulin receptor, J. Clin. Invest. 66: 1124–1134.

    Article  PubMed  CAS  Google Scholar 

  • Haigler, H. T., McKanna, J. A., and Cohen, S., 1979, Direct visualization of the binding and internalization of a ferritin conjugate of epidermal growth factor in human carcinoma cells A-431, J. Cell Biol. 81: 382–395.

    Article  PubMed  CAS  Google Scholar 

  • Harmon, J. T., Hedo, J. A., and Kahn, C. R., 1983, Characterization of a membrane regulator of insulin receptor affinity, J. Biol. Chem. 258: 6875–6881.

    PubMed  CAS  Google Scholar 

  • Hirata, F., and Axelrod, J., 1980, Phospholipid methylation and biological signal transmission, Science 209: 1082–1090.

    Article  PubMed  CAS  Google Scholar 

  • Jacobs, S., and Cuatrecasas, P., 1980, Disulfide reduction converts the insulin receptor of human placenta to a low affinity form, J. Clin. Invest. 66: 1424–1427.

    Article  PubMed  CAS  Google Scholar 

  • Jarett, L., and Smith, R. M., 1977, The natural occurrence of insulin receptors in groups on adipocyte plasma membranes as demonstrated with monomeric ferritin-insulin, J. Supramol. Struct. 6: 45–59.

    Article  PubMed  CAS  Google Scholar 

  • Jarett, L., and Smith, R. M., 1983, Partial disruption of naturally ocurring groups of insulin receptors on adipocyte plasma membranes by dithiothreitol and N-ethylmaleimide: The role of disulfide bonds, Proc. Natl’s Acad. Sci., U.S.A. 80: 1023–1027.

    Article  CAS  Google Scholar 

  • Jarett, L., Kiechle, F. L., Parker, J. C., and Macaulay, S. L., 1983, The chemical mediators of insulin action: Possible targets for postreceptor defects, A. J. Med. 74: 31–37.

    Article  CAS  Google Scholar 

  • Karlsson, F. A., Van Obberghen, E., Grunfeld, C., and Kahn, C. R., 1979, Desensitization of the insulin receptor at an early postreceptor step by prolonged exposure to antireceptor antibody, Proc. Natl. Acad. Sci. U.S.A. 76: 809–813.

    Article  PubMed  CAS  Google Scholar 

  • Kelly, K. L., and Jarett, L., 1984, Insulin stimulation of phospholipid methylation in isolated rat adipocyte plasma membranes, Proc. Natl. Acad. Sci. U.S.A. 81: 1089–1092.

    Article  PubMed  CAS  Google Scholar 

  • Klausner, R. D., Bhalla, D. K., Dragsten, P., Hoover, R. L., and Karnovsky, M. J., 1980, Model for capping derived from inhibition of surface receptor capping by free fatty acids, Proc. Natl. Acad. Sci. U.S.A. 77: 437–441.

    Article  PubMed  CAS  Google Scholar 

  • Krupp, M. N., and Livingston, J. N., 1978, Insulin binding to solubilized material from fat cell membranes: Evidence for two binding species, Proc. Natl. Acad. Sci. U.S.A. 75: 2593–2597.

    Article  PubMed  CAS  Google Scholar 

  • Lesniak, M. A., and Roth, J., 1976, Regulation of receptor concentration by homologous hormone: Effect of human growth hormone on its receptor in IM-9 lymphocytes, J. Biol. Chem. 251: 3720–3729.

    PubMed  CAS  Google Scholar 

  • Lloyd, C. E., and Ascoli, M., 1983, On the mechanisms involved in the regulation of the cell-surface receptors for human choriogonadotropin and mouse epidermal growth factor in cultured Leydig tumor cells, J. Cell Biol. 96: 521–526.

    Article  PubMed  CAS  Google Scholar 

  • Lyen, K. R., Smith, R. M., and Jarett, L., 1983, Differences in the ability of anti-insulin antibody to aggregate monomeric ferritin-insulin occupied receptor sites on liver and adipocyte plasma membranes, Diabetes 32: 648–653.

    PubMed  CAS  Google Scholar 

  • Marshall, S., and Olefsky, J. M., 1980, Effects of insulin incubation on insulin binding, glucose transport, and insulin degradation by isolated rat adipocytes, J. Clin. Invest. 66: 763–772.

    Article  PubMed  CAS  Google Scholar 

  • Maturo, J. M. Ill, and Hollenberg, M. D., 1978, Insulin receptor: Interaction with nonreceptor glycoprotein from liver cell membranes, Proc. Natl. Acad. Sci. U.S.A. 75:3070– 3074.

    Article  PubMed  CAS  Google Scholar 

  • Maxfield, F. R., Schlessinger, J., Shechter, Y., Pastan, I., and Willingham, M. C., 1978, Collection of insulin, EGF, and alpha-2-macroglobulin in the same patches on the surface of cultured fibroblasts and common internalization, Cell 14: 805–810.

    Article  PubMed  CAS  Google Scholar 

  • McKanna, J. A., Haigler, H. T., and Cohen, S., 1979, Hormone receptor topology and dynamics: Morphological analysis using ferritin-labeled epidermal growth factor, Proc. Natl. Acad. Sci. U.S.A. 76: 5689–5693.

    Article  PubMed  CAS  Google Scholar 

  • Montesano, R., Roth, J., Robert, A., and Orci, L., 1982, Non-coated membrane invaginations are involved in binding and internalization of cholera and tetanus toxins, Nature 296: 651–653.

    Article  PubMed  CAS  Google Scholar 

  • Moore, W. V., Wohnlich, L. P., and Fix, J. A., 1983, Role of disulfide bonds in human growth hormone binding and dissociation in isolated rat hepatocytes and liver plasma membranes, Endocrinology 112: 2152–2158.

    Article  PubMed  CAS  Google Scholar 

  • Nelson, D. M., Smith, R. M., and Jarett, L., 1978, Nonuniform distribution and grouping of insulin receptors on the surface of human placental syncytial trophoblast, Diabetes 27: 530–538.

    Article  PubMed  CAS  Google Scholar 

  • Nieto, A., and Catt, K. J., 1983, Hormonal activation of phospholipid methyltransferase in the Leydig cell, Endocrinology 113: 758–762.

    Article  PubMed  CAS  Google Scholar 

  • Ozawa, Y., Chopra, I. J., Solomon, D. H., and Smith, F., 1979, The role of sulfhydryl groups in thyrotropin binding and adenylate cyclase activities of thyroid plasma membranes, Endocrinology 105: 1221–1225.

    Article  PubMed  CAS  Google Scholar 

  • Perelson, A. S., 1980, Receptor clustering on a cell surface. II. Theory of receptor cross- linking by ligands bearing two chemically distinct functional groups, Math Biosci. 49: 87–110.

    Article  CAS  Google Scholar 

  • Perelson, A. S., and DeLisi, C., 1980, Receptor clustering on a cell surface. I. Theory of receptor cross-linking by ligands bearing two chemically identical functional groups, Math Biosci. 48: 71–110.

    Article  Google Scholar 

  • Pessin, J. E., Gitomer, W., Oka, Y., Oppenheimer, C. L., and Czech, M. P., 1983, β3- Adrenergic regulation of insulin and epidermal growth factor receptors in rat adipocytes, J. Biol. Chem. 258: 7386–7394.

    Google Scholar 

  • Pike, L. J., Bowen-Pope, D. F., Ross, R., and Krebs, E. G., 1983, Characterization of platelet-derived growth factor-stimulated phosphorylation in cell membranes, J. Biol. Chem. 258: 9383–9390.

    PubMed  CAS  Google Scholar 

  • Rosen, O. M., Herrera, R., Olowe, Y., Petruzzelli, L. M., and Cobb, M. H., 1983, Phosphorylation activates the insulin receptor tyrosine protein kinase, Proc. Natl. Acad. Sci. U.S.A. 80: 3237–3240.

    Article  PubMed  CAS  Google Scholar 

  • Schlessinger, J., Elson, E. L., Webb, W. W., Yahara, I., Rutishauser, U., and Edelman, G. M., 1977, Receptor diffusion on cell surfaces modulated by locally bound concanavalin A, Proc. Natl. Acad. Sci. U.S.A. 74: 1110–1114.

    Article  PubMed  CAS  Google Scholar 

  • Schweitzer, J. B., Smith, R. M., and Jarett, L., 1980, Differences in organizational structure of insulin receptor on rat adipocyte and liver plasma membranes: Role of disulfide bonds, Proc. Natl. Acad. Sci. U.S.A. 77: 4692–4696.

    Article  PubMed  CAS  Google Scholar 

  • Shiu, R. P. C., and Friesen H. G., 1981, Regulation of prolactin receptors in target cells, in: Receptors and Recognition, series B. Vol. 13 ( R. J. Lefkowitz, ed.), Chapman and Hall, New York, pp. 67–81.

    Google Scholar 

  • Smith, R. M., and Jarett, L., 1982, A simplified method of producing biologically active monomeric ferritin-insulin for use as a high resolution ultrastructural marker for occupied insulin receptors, J. Histochem. Cytochem. 30: 651–656.

    Google Scholar 

  • Smith, R. M., and Jarett, L., 1983, Quantitative ultrastructural analysis of receptor-mediated insulin uptake into adipocytes, J. Cell. Physiol. 115: 199–207.

    Article  PubMed  CAS  Google Scholar 

  • Smith, R. M., and Jarett, L., 1983, Quantitative ultrastructural analysis of receptor-mediated insulin uptake into adipocytes, J. Cell. Physiol. 115: 199–207.

    Article  PubMed  CAS  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 

  • Suen, E. T., Stefanini, E., and Clement-Cormier, Y. C., 1980, Evidence for essential thiol groups and disulfide bonds in agonist and antagonist binding to the dopamine receptor, Biochem. Biophys, Res. Commun. 96: 953–960.

    Article  CAS  Google Scholar 

  • Vauquelin, G., Bottari, S., Kanarek, L., and Strosberg, A. D., 1979, Evidence for essential disulfide bonds in Pi-adrenergic receptors of turkey erythrocyte membranes, J. Biol. Chem. 254: 4462–4469.

    PubMed  CAS  Google Scholar 

  • Vigneri, R., Goldfine, I. D., Wong, K. Y., Smith, G. J., and Pezzino, V., 1978, The nuclear envelope: The major site of insulin binding in rat liver nuclei, J. Biol. Chem. 253: 2098–2103.

    PubMed  CAS  Google Scholar 

  • Walker, J. W., Lukas, R. J., and McNamee, M. G., 1981, Effects of thio-group modifications on the ion permeability control and ligand binding properties of torpedo californica acetylcholine receptor, Biochemistry 20: 2191–2199.

    Article  PubMed  CAS  Google Scholar 

  • Willingham, M. C., Maxfield, F. R., and Pastan, I. H., 1979, Alpha-2-macroglobulin binding to the plasma membrane of cultured fibroblasts, J. Cell Biol. 82: 614–625.

    Article  PubMed  CAS  Google Scholar 

  • Zick, Y., Wittaker, J., and Roth, J., 1983, Insulin stimulated phosphorylation of its own receptor, J. Biol. Chem. 258: 3431–3434.

    PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1985 Plenum Press, New York

About this chapter

Cite this chapter

Jarett, L., Smith, R.M. (1985). Receptor Regulation. 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_1

Download citation

  • DOI: https://doi.org/10.1007/978-1-4613-2131-6_1

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4612-9259-3

  • Online ISBN: 978-1-4613-2131-6

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics