New Concepts in the Pathogenesis of NIDDM pp 47-61 | Cite as
The ß-Cell Sulfonylurea Receptor
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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.
Keywords
Insulin Secretion Scatchard Plot Rose Bengal Sulfonylurea Receptor Fluorescein DerivativePreview
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References
- Ashcroft, F.M., 1988, Adenosine triphosphate-sensitive K+-channels, Ann. Rev. Neurosci. 11:97–118.PubMedCrossRefGoogle 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.PubMedGoogle 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.PubMedGoogle Scholar
- Ashcroft, S. J. H. and Ashcroft, F. M., 1990, Properties and functions of ATP-sensitive K-channels, Cellular Signalling 2: 197–214.PubMedCrossRefGoogle 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.CrossRefGoogle 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.CrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedGoogle Scholar
- Franke, H. and Fuchs, J., 1955, Ein neues antidiabetisches Prinzip, Deutsch Med. Woschenschrift 80:1449.CrossRefGoogle 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.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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedGoogle 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.CrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedGoogle 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.PubMedGoogle Scholar
- Noma, A., 1983, ATP-regulated K+ channels in cardiac muscle, Nature 305: 147–148.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.CrossRefGoogle 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.CrossRefGoogle 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.PubMedCrossRefGoogle 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.PubMedCrossRefGoogle 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.CrossRefGoogle 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.PubMedCrossRefGoogle Scholar