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The ß-Cell Sulfonylurea Receptor

  • Chapter
New Concepts in the Pathogenesis of NIDDM

Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 334))

Abstract

It is now 50 years since the accidental observations which indicated that a sulfonamide, p-amino-benzene-sulfamido-isopropyl-thiodiazole (2254 RP), could induce hypoglycaemia (Janbon et al., 1942). This response was shown to be due to stimulation of insulin secretion and led to the use of this class of sulfonamides (called sulfonylureas) to treat diabetes (Loubatières, 1955; Bertram et al., 1955; Franke et al., 1955). Loubatières (1944) also found that a related sulfonamide, 3-methy1-7-chloro-1,2,4-benzothiadiazine-1,1-dioxide (diazoxide) elicited hyperglycaemia, via inhibition of insulin secretion.

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References

  • Ashcroft, F.M., 1988, Adenosine triphosphate-sensitive K+-channels, Ann. Rev. Neurosci. 11:97–118.

    Article  PubMed  CAS  Google Scholar 

  • Ashcroft, F.M, Ashcroft, S.J.H. and Harrison, D.E., 1988, Properties of single potassium channels modulated by glucose in rat pancreatic ß-cells, J. Physiol. 400: 501–527.

    PubMed  CAS  Google Scholar 

  • Ashcroft, F. M. and Kakei, M., 1989, ATP-sensitive K+ channels in rat pancreatic beta-cells: Modulation by ATP and Mg2+ ions, J. Physiol. 416: 349–367.

    PubMed  CAS  Google Scholar 

  • Ashcroft, S. J. H. and Ashcroft, F. M., 1990, Properties and functions of ATP-sensitive K-channels, Cellular Signalling 2: 197–214.

    Article  PubMed  CAS  Google Scholar 

  • Ashcroft, S. J. H. and Ashcroft, F.M, 1989, The role of the ATP-sensitive K-channel in stimulus-response coupling in the pancreatic ß-cell, in “Hormones and Cell Regulation No. 14,” Eds J. Nunez, J.E. Dumont. Colloque INSERM/J. Libbey Eurotext Ltd. 198: 99–103.

    Google Scholar 

  • Ashcroft, F.M. and Rorsman, P, 1989, Electrophysiology of the pancreatic ß-cell, Prog. Biophys. Molec. Biol. 54: 87–143.

    Article  CAS  Google Scholar 

  • Bertram, F., Bendfeldt, E. and Otto, H., 1955, Über ein wirksames perorales Antidiabeticum (BZ 55), Deutsch Med. Woschenschrift: 1455.

    Google Scholar 

  • Bokvist, K., Ämmälä, C., Ashcroft, F.M., Bergrren, P.-O., Larsson, O. and Rorsman, P., 1991, Separate processes mediate nucleotide-induced inhibition and stimulation of the ATP-regulated K+ channels in mouse pancreatic ß-cells, Froc. Roy. Soc. B: 243: 139–144.

    Article  CAS  Google Scholar 

  • De Weille, J. R., Müller, M., and Lazdunski, M., 1992, Activation and inhibition of ATP-sensitive K+ channels by fluorescein derivatives, J. Biol. Chem. 267: 4557–4563.

    Google Scholar 

  • Dunne, M.J., 1990, Effects of pinacidil, RP 49356 and nicorandil on ATP-sensitive potassium channels in insulin-secreting cells, Br J Pharmacol. 99:487–492.

    Article  PubMed  CAS  Google Scholar 

  • Dunne, M.J., Aspinall, R.J., and Petersen, O.H., 1990, The effects of cromakalim on ATP-sensitive potassium channels in insulin-secreting cells, Br. J. Pharmacol. 99:169–175.

    Article  PubMed  CAS  Google Scholar 

  • Dunne, M.J., Dott, M.C. and Petersen O.H., 1987, Interactions of diazoxide, tolbutamide and ATP4-on nucleotide-dependent K+ channels in an insulin-secreting cell line, J. Membr. Biol. 99: 215–224.

    Article  PubMed  CAS  Google Scholar 

  • Findlay, I., 1992, Effects of pH upon the inhibition by sulphonylurea drugs of ATP-sensitive K+ channels in cardiac muscle J. Pharmacol. Exp. Ther. 262:71–79.

    PubMed  CAS  Google Scholar 

  • Franke, H. and Fuchs, J., 1955, Ein neues antidiabetisches Prinzip, Deutsch Med. Woschenschrift 80:1449.

    Article  CAS  Google Scholar 

  • Geisen, K., Hitzel, V., Ökomonopoulos, R., Pünter, J., Weyer, R., and Summ, H. D., 1985, Inhibition of [3H]-glibenclamide binding to sulfonylurea receptors by oral antidiabetic agents. Arzeim. Forsch 35:707–712.

    CAS  Google Scholar 

  • Hellman, B., Sehlin, J., and Täljedal, I.-B., 1971, The pancreatic ß-cell recognition of insulin secretagogues. II. Site of action of tolbutamide. Biochem. Biophys. Res. Commun. 45: 1384–1388.

    Article  PubMed  CAS  Google Scholar 

  • Janbon, M., Chapal, J., Vedel, A., and Schaap, J., 1942, Accidents hypoglycémiques graves par un sulfamidothiazol (VK 57 ou 2254 RP), Montpellier méd. 21-22: 441.

    Google Scholar 

  • Kakei, M. Kelly, R.P., Ashcroft, S.J.H., and Ashcroft, F.M., 1986, The ATP-sensitivity of K+ channels in rat pancreatic B-cells is modulated by ADP, FEBS Lett 208: 63–66.

    Article  PubMed  CAS  Google Scholar 

  • Kaubisch, N. Hammer, R., Wollheim, C.B., Renold, A.E., and Offord, R.E., 1982, Specific receptors for sulfonylureas in brain and in a B-cell tumor of the rat. Biochem. Pharmacol. 31: 1171–1174.

    Article  PubMed  CAS  Google Scholar 

  • Kozlowski, R.Z., Hales, C.N., and Ashford, M.L.J., 1989, Dual effects of diazoxide on ATP-K+ currents recorded from an insulin-secreting cell line, Br. J. Pharmacol. 97: 1039–1050.

    Article  PubMed  CAS  Google Scholar 

  • Loubatières, A., 1944 Relations entre la structure moléculaire et l’activité hypoglycémiante des aminobenzène-sulfamido-alkylthiodiazols, Comptes Rendus Soc. Biol. (Paris) 138: 830.

    Google Scholar 

  • Loubatières, A., 1955, Effets chez l’homme diabétique du p-amino-benzène-sulfamidoisopropyl-thiodiazol, Montpellier méd. 48: 618.

    PubMed  Google Scholar 

  • Niki, I. and Ashcroft, S. J. H., 1991, Possible involvement of protein phosphorylation in the regulation of the sulphonylurea receptor of a pancreatic beta-cell line, HIT T15, Biochim. Biophys. Acta Mol. Cell Res. 1133: 95–101.

    Article  CAS  Google Scholar 

  • Niki, I., Ashcroft, F. M. and Ashcroft, S. J. H., (1989), The dependence on intracellular ATP concentration of ATP-sensitive K-channels and of Na-K-ATPase in intact HTT-T15 ß-cells, FEBS Lett. 257: 361–364.

    Article  PubMed  CAS  Google Scholar 

  • Niki, I. Kelly R.P., Ashcroft, S.J.H., and Ashcroft, F.M., 1989, ATP-sensitive K-channels in HIT T15 ß-cells studies by patch-clamp methods, 86Rb efflux and glibenclamide binding, Pflügers Arch. 415: 47–55.

    Article  PubMed  CAS  Google Scholar 

  • Niki, I., Nicks, J.L., and Ashcroft, S.J.H., 1990, The beta-cell glibenclamide receptor is an ADP-binding protein, Biochem J 268: 713–718.

    PubMed  CAS  Google Scholar 

  • Niki, I., Welsh, M., Berggren, P.-O., Hubbard, P., and Ashcroft, S. J. H., 1991, Characterization of the solubilized glibenclamide receptor in a hamster pancreatic beta-cell line, HIT T15, Biochem. J. 277: 619–624.

    PubMed  CAS  Google Scholar 

  • Noma, A., 1983, ATP-regulated K+ channels in cardiac muscle, Nature 305: 147–148.

    Article  PubMed  CAS  Google Scholar 

  • Ohno-Shosaku, T., Zünckler, B., and Trube, G., 1987, Dual effects of ATP on K+ currents of mouse pancreatic ß-cells, Pflügers Arch 408:133–138.

    Article  PubMed  CAS  Google Scholar 

  • Schwanstecher, M., Brandt, C., Behrends, S., Schaupp, U., and Panten, U., 1992, Effect of MgATP on pinacidil-induced displacement of glibenclamide from the sulphonylurea receptor in a pancreatic beta-cell line and rat cerebral cortex Br J. Pharmacol. 106: 295–301.

    Article  PubMed  CAS  Google Scholar 

  • Schwanstecher, M., Löser, S., Rietze, I., and Panten, U., 1991, Phosphate and thiophosphate group donating adenine and guanine nucleotides inhibit glibenclamide binding to membranes from pancreatic islets, Naunyn-Schmiedeberg’s Arch. Pharmacol. 343: 83–89.

    Article  CAS  Google Scholar 

  • Sehlin, J., 1973, Evidence for specific binding of tolbutamide to the plasma membrane of the pancreatic ß-cells, Acta Diabetol. Lat. 10:1052–1060.

    Article  CAS  Google Scholar 

  • Sturgess, N. C., Ashford, M.L.I., Cook, D.L., and Hales, C.N., 1985, The sulphonylurea receptor may be an ATP-sensitive potassium channel, Lancet 2: 474–475.

    Article  PubMed  CAS  Google Scholar 

  • Sturgess, N.C., Kozlowski, R.Z., Carrington, C.A., Hales, C.N., and Ashford, M.L.J., 1988, Effects of sulphonylureas and diazoxide on insulin secretion and nucleotide-sensitive channels in an insulin-secreting cell line, Br J. Pharmacol. 9583–9594; 1988.

    Google Scholar 

  • Trube, G., Rorsman, P., and Ohno-Shosaku, T., 1986, Opposite effects of tolbutamide and diazoxide on the ATP-dependent K+ channel in mouse pancreatic beta-cells, Pflügers Arch. 407: 493–499.

    Article  PubMed  CAS  Google Scholar 

  • Virsolvy-Vergine, A., Leray, H., Kuroki, S., Lupo, B., Dufour, N., and Bataille, D., 1992, Endosulfine, an endogenous peptidic ligand for the sulfonylurea receptor: purification and partial characterization from ovine brain, Proc. Natl. Acad. Sci. 89: 6623–6629.

    Article  Google Scholar 

  • Zünckler, B.J., Lenzen, S., Manner, K., Panten, U., and Trube, G., 1988, Concentration-dependent effects of tolbutamide, meglitinide, glipizide, glibenclamide and diazoxide on ATP-regulated K+ currents in pancreatic B-cells, Naunyn-Schmiedeberg’s Arch. Pharmacol. 337: 225–230.

    Google Scholar 

  • Zünkler, B.J., Lins, S., Ohno-shosaku, T., Trube, G., and Panten, U., 1988, Cytosolic ADP enhances the sensitivity to tolbutamide of ATP-dependent K+ channels from pancreatic ß-cells, FEBS Lett. 239: 241–244.

    Article  PubMed  Google Scholar 

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Author information

Authors and Affiliations

  1. Nuffield Department of Clinical Biochemistry, John Radcliffe Hospital, Headington, Oxford, OX3 9DU, UK

    Stephen J. H. Ashcroft, Ichiro Niki, Sue Kenna & Ling Weng

  2. University Laboratory of Physiology, Parks Road, Oxford, OX1 3PT, UK

    Jackie Skeer, Barbara Coles & Frances M. Ashcroft

Authors
  1. Stephen J. H. Ashcroft
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  2. Ichiro Niki
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  3. Sue Kenna
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  4. Ling Weng
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  5. Jackie Skeer
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  6. Barbara Coles
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  7. Frances M. Ashcroft
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Editor information

Editors and Affiliations

  1. Karolinska Hospital, Stockholm, Sweden

    Claes Göran Östenson  & Suad Efendić  & 

  2. University of Toronto, Toronto, Ontario, Canada

    Mladen Vranic

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© 1993 Springer Science+Business Media New York

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Ashcroft, S.J.H. et al. (1993). The ß-Cell Sulfonylurea Receptor. In: Östenson, C.G., Efendić, S., Vranic, M. (eds) New Concepts in the Pathogenesis of NIDDM. Advances in Experimental Medicine and Biology, vol 334. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-2910-1_4

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  • DOI: https://doi.org/10.1007/978-1-4615-2910-1_4

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4613-6262-3

  • Online ISBN: 978-1-4615-2910-1

  • eBook Packages: Springer Book Archive

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