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Diabetologia

Erschienen in:

01.07.2003 | Review

Sulphonylurea action revisited: the post-cloning era

verfasst von: Dr. F. M. Gribble, F. Reimann

Erschienen in: Diabetologia | Ausgabe 7/2003

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Abstract

Hypoglycaemic agents such as sulphonylureas and the newer group of "glinides" stimulate insulin secretion by closing ATP-sensitive potassium (K_ATP) channels in pancreatic beta cells, but have varying cross-reactivity with related channels in extrapancreatic tissues such as heart, vascular smooth and skeletal muscle. Experiments on the structure-function relationships of recombinant K_ATP channels and the phenotypes of mice deficient in different K_ATP channel subunits have provided important insights into the mechanisms underlying sulphonylurea selectivity, and the potential consequences of K_ATP channel blockade outside the pancreatic beta cell. The different pharmacological properties of K_ATP channels from beta cells compared with those from cardiac, smooth and skeletal muscle, are accounted for by the expression of alternative types of sulphonylurea receptor, with non-identical drug binding sites. The sulphonylureas and glinides are found to fall into two groups: one exhibiting selectivity for beta cell sulphonylurea receptors (SUR1), and the other blocking cardiovascular and skeletal muscle sulphonylurea receptors (SUR2) with potencies similar to their action on SUR1. In seeking potential side effects of K_ATP channel inhibitors in humans, it is essential to take these drug differences into account, along with the probability (suggested by the studies on K_ATP channel knockout mice) that the effects of extrapancreatic K_ATP channel inhibition might be either subtle or rare. Further studies are still required before a final decision can be made on whether non-selective agents are appropriate for the therapy of Type 2 diabetes.

Aguilar-Bryan L, Nichols CG, Wechsler SW et al. (1995) Cloning of the beta cell high-affinity sulfonylurea receptor: a regulator of insulin secretion. Science 268:423–426PubMed

Inagaki N, Gonoi T, Clement JP et al. (1995) Reconstitution of IK_ATP—an inward rectifier subunit plus the sulfonylurea receptor. Science 270:1166–1170PubMed

Sakura H, Ammala C, Smith PA, Gribble FM, Ashcroft FM (1995) Cloning and functional expression of the cDNA encoding a novel ATP-sensitive potassium channel subunit expressed in pancreatic beta cells, brain, heart and skeletal muscle. FEBS Lett 377:338–344PubMed

Ashcroft FM, Gribble FM (1999) ATP-sensitive K⁺ channels in health and disease. Diabetologia 42:903–919PubMed

Aguilar-Bryan L, Bryan J (1999) Molecular biology of adenosine triphosphate-sensitive potassium channels. Endocr Rev 20:101–135PubMed

Seino S, Miki T (2003) Physiological and pathophysiological roles of ATP-sensitive K⁺ channels. Prog Biophys Mol Biol 81:133–176CrossRefPubMed

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

Nichols CG, Lederer WJ (1991) Adenosine triphosphate-sensitive potassium channels in the cardiovascular system. Am J Physiol 261:H1675–H1686PubMed

Quayle JM, Nelson MT, Standen NB (1997) ATP-sensitive and inwardly-rectifying potassium channels in smooth muscle. Physiol Rev 77:1165–1232PubMed

10.

Davis NW, Standen NB, Stanfield PR (1991) ATP-dependent potassium channels of muscle cells: their properties, regulation, and possible functions. J Bioenerg Biomembr 23:509–535PubMed

11.

Amoroso S, Schmid-Antomarchi H, Fosset M, Lazdunski M (1990) Glucose, sulfonylureas, and neurotransmitter release: role of ATP-sensitive K⁺ channels. Science 247:852–854PubMed

12.

Liss B, Bruns R, Roeper J (1999) Alternative sulfonylurea receptor expression defines metabolic sensitivity of K_ATP channels in dopaminergic midbrain neurons. EMBO J 18:833–846PubMed

13.

Spanswick D, Smith MA, Groppi VE, Logan SD, Ashford ML (1997) Leptin inhibits hypothalamic neurons by activation of ATP-sensitive potassium channels. Nature 390:521–525

14.

Rorsman P (1997) The pancreatic beta cell as a fuel sensor: an electrophysiologist's viewpoint. Diabetologia 40:487–495PubMed

15.

Ashcroft FM, Rorsman P (1989) Electrophysiology of the pancreatic beta cell. Prog Biophys Mol Biol 54:87–143PubMed

16.

Ashcroft SJ, Weerasinghe LC, Randle PJ (1973) Interrelationship of islet metabolism, adenosine triphosphate content and insulin release. Biochem J 132:223–231PubMed

17.

Mertz RJ, Worley JF, Spencer B, Johnson JH, Dukes ID (1996) Activation of stimulus-secretion coupling in pancreatic beta cells by specific products of glucose metabolism. Evidence for privileged signaling by glycolysis. J Biol Chem 271:4838–4845PubMed

18.

Eto K, Tsubamoto Y, Terauchi Y et al. (1999) Role of NADH shuttle system in glucose-induced activation of mitochondrial metabolism and insulin secretion. Science 283:981–985PubMed

19.

Smith PA, Sakura H, Coles B, Gummerson N, Proks P, Ashcroft FM (1997) Electrogenic arginine transport mediates stimulus-secretion coupling in mouse pancreatic beta cells. J Physiol 499:625–635PubMed

20.

Reimann F, Gribble FM (2002) Glucose-sensing in glucagon-like peptide-1-secreting cells. Diabetes 51:2757–2763PubMed

21.

Gribble FM, Williams L, Simpson AK, Reimann F (2003) A novel glucose-sensing mechanism contributing to Glucagon-Like Peptide-1 secretion from the GLUTag cell line. Diabetes 52:1147–1154PubMed

22.

Inagaki N, Tsuura Y, Namba N et al. (1995) Cloning and functional characterization of a novel ATP-sensitive potassium channel ubiquitously expressed in rat tissues, including pancreatic islets, pituitary, skeletal muscle, and heart. J Biol Chem 270:5691–5694CrossRefPubMed

23.

Shyng S-L, Nichols CG (1997) Octameric stochiometry of the K_ATP channel complex. J Gen Physiol 110:655–664CrossRefPubMed

24.

Clement JP, Kunjilwar K, Gonzalez G et al. (1997) Association and stoichiometry of K_ATP channel subunits. Neuron 18:827–838PubMed

25.

Yamada M, Isomoto S, Matsumoto S et al. (1997) Sulphonylurea receptor 2B and Kir6.1 form a sulphonylurea-sensitive but ATP-insensitive K⁺ channel. J Physiol 499:715–720PubMed

26.

Thomzig A, Wenzel M, Karschin C et al. (2001) Kir6.1 is the principal pore-forming subunit of astrocyte but not neuronal plasma membrane K_ATP channels. Mol Cell Neurosci 18:671–690CrossRefPubMed

27.

Takano M, Xie LH, Otani H, Horie M (1998) Cytoplasmic terminus domains of Kir6.x confer different nucleotide-dependent gating on the ATP-sensitive K⁺ channel. J Physiol 512:395–406PubMed

28.

Zerangue N, Schwappach B, Jan YN, Jan LY (1999) A new ER trafficking signal regulates the subunit stoichiometry of plasma membrane K_ATP channels. Neuron 22:537–548PubMed

29.

Tucker SJ, Gribble FM, Zhao C, Trapp S, Ashcroft FM (1997) Truncation of Kir6.2 produces ATP-sensitive K⁺ channels in the absence of the sulphonylurea receptor. Nature 387:179–183

30.

Tucker SJ, Gribble FM, Proks P et al. (1998) Molecular determinants of K_ATP channel inhibition by ATP. EMBO J 17:3290–3296CrossRefPubMed

31.

Lee K, Dixon AK, Richardson PJ, Pinnock RD (1999) Glucose-receptive neurones in the rat ventromedial hypothalamus express K_ATP channels composed of Kir6.1 and SUR1 subunits. J Physiol 515:439–452PubMed

32.

Liu M, Seino S, Kirchgessner AL (1999) Identification and characterization of glucoresponsive neurons in the enteric nervous system. J Neurosci 19:10305–10317

33.

Ibrahim N, Bosch MA, Smart JL et al. (2003) Hypothalamic proopiomelanocortin neurons are glucose responsive and express K_ATP channels. Endocrinology 144:1331–1340CrossRefPubMed

34.

Inagaki N, Gonoi T, Clement JP et al. (1996) A family of sulfonylurea receptors determines the pharmacological properties of ATP-sensitive K⁺ channels. Neuron 16:1011–1017PubMed

35.

Isomoto S, Kondo C, Yamada M et al. (1996) A novel sulfonylurea receptor forms with BIR (Kir6.2) a smooth muscle type ATP-sensitive K⁺ channel. J Biol Chem 271:24321–24324PubMed

36.

Chutkow WA, Makielski JC, Nelson DJ, Burant CF, Fan Z (1999) Alternative splicing of sur2 Exon 17 regulates nucleotide sensitivity of the ATP-sensitive potassium channel. J Biol Chem 274:13656–13665PubMed

37.

Chutkow WA, Simon MC, Le Beau MM, Burant CF (1996) Cloning, tissue expression, and chromosomal localization of SUR2, the putative drug-binding subunit of cardiac, skeletal muscle, and vascular K_ATP channels. Diabetes 45:1439–1445PubMed

38.

Gros L, Trapp S, Dabrowski M, Ashcroft FM, Bataille D, Blache P (2002) Characterization of two novel forms of the rat sulphonylurea receptor SUR1A2 and SUR1BDelta31. Br J Pharmacol 137:98–106CrossRefPubMed

39.

Hambrock A, Preisig-Muller R, Russ U et al. (2002) Four novel splice variants of sulfonylurea receptor 1. Am J Physiol Cell Physiol 283: C587-C598PubMed

40.

Sakura H, Trapp S, Liss B, Ashcroft FM (1999) Altered functional properties of K_ATP channel conferred by a novel splice variant of SUR1. J Physiol 521:337–350PubMed

41.

Tusnady GE, Bakos E, Varadi A, Sarkadi B (1997) Membrane topology distinguishes a subfamily of the ATP-binding cassette (ABC) transporters. FEBS Lett 402:1–3PubMed

42.

Conti LR, Radeke CM, Shyng SL, Vandenberg CA (2001) Transmembrane topology of the sulfonylurea receptor SUR1. J Biol Chem 276:41270–41278CrossRefPubMed

43.

Ashcroft FM, Gribble FM (2000) New windows on the mechanism of action of K_ATP channel openers. Trends Pharmacol Sci 21:439–445PubMed

44.

Gribble FM, Tucker SJ, Seino S, Ashcroft FM (1998) Tissue specificity of sulphonylureas: studies on cloned cardiac and beta cell K_ATP channels. Diabetes 47:1412–1418PubMed

45.

Gribble FM, Ashcroft FM (1999) Differential sensitivity of β-cell and extrapancreatic K_ATP channels to gliclazide. Diabetologia 42:845–848CrossRefPubMed

46.

Song DK, Ashcroft FM (2001) Glimepiride block of cloned β-cell, cardiac and smooth muscle K-ATP channels. Brit J Pharmacol 133:193–199

47.

Dabrowski M, Wahl P, Holmes WE, Ashcroft FM (2001) Effect of repaglinide on cloned beta cell, cardiac and smooth muscle types of ATP-sensitive potassium channel. Diabetologia 44:747–756CrossRefPubMed

48.

Reimann F, Proks P, Ashcroft FM (2001) Effects of mitiglinide (S 21403) on Kir6.2/SUR1, Kir6.2/SUR2A and Kir6.2/SUR2B types of ATP-sensitive potassium channel. Br J Pharmacol 132:1542–1548PubMed

49.

Hansen AM, Christensen IT, Hansen JB, Carr RD, Ashcroft FM, Wahl P (2002) Differential interactions of nateglinide and repaglinide on the human beta cell sulphonylurea receptor 1. Diabetes 51:2789–95PubMed

50.

Chachin M, Yamada M, Fujita A, Matsuoka T, Matsushita K, Kurachi Y (2003) Nateglinide, a D-phenylalanine derivative lacking either a sulfonylurea or benzamido moiety, specifically inhibits pancreatic beta cell-type K_ATP channels. J Pharmacol Exp Ther 304:1025–1032CrossRefPubMed

51.

Reimann F, Ashcroft FM, Gribble FM (2001) Structural basis for the interference between nicorandil and sulfonylurea action. Diabetes 50:2253–2259PubMed

52.

Uhde I, Toman A, Gross I, Schwanstecher C, Schwanstecher M (1999) Identification of the potassium channel opener site on sulfonylurea receptors. J Biol Chem 274:28079–28082CrossRefPubMed

53.

Gribble FM, Tucker SJ, Haug T, Ashcroft FM (1998) MgATP activates the beta cell K_ATP channel by interaction with its SUR1 subunit. Proc Natl Acad Sci USA 95:7185–7190CrossRefPubMed

54.

Gribble FM, Tucker SJ, Ashcroft FM (1997) The essential role of the Walker A motifs of SUR1 in K-ATP channel activation by Mg-ADP and diazoxide. EMBO J 16:1145–1152CrossRefPubMed

55.

Shyng S, Ferrigni T, Nichols CG (1997) Regulation of K_ATP channel activity by diazoxide and MgADP. Distinct functions of the two nucleotide binding folds of the sulfonylurea receptor. J Gen Physiol 110:643–654CrossRefPubMed

56.

Nichols CG, Shyng SL, Nestorowicz A et al. (1996) Adenosine diphosphate as an intracellular regulator of insulin secretion. Science 272:1785–1787PubMed

57.

Babenko AP, Gonzalez G, Bryan J (2000) Pharmaco-topology of sulfonylurea receptors. Separate domains of the regulatory subunits of K_ATP channel isoforms are required for selective interaction with K⁺ channel openers. J Biol Chem 275:717–720CrossRefPubMed

58.

Senior AE, al-Shawi MK, Urbatsch IL (1995) The catalytic cycle of P-glycoprotein. FEBS Lett 377:285–289CrossRefPubMed

59.

Higgins CF (1992) ABC transporters: from microorganisms to man. Annu Rev Cell Biol 8:67–113PubMed

60.

Ueda K, Inagaki N, Seino S (1997) MgADP antagonism to Mg²⁺-independent ATP binding of the sulfonylurea receptor SUR1. J Biol Chem 272:22983–22986CrossRefPubMed

61.

Ueda K, Komine J, Matsuo M, Seino S, Amachi T (1999) Cooperative binding of ATP and MgADP in the sulfonylurea receptor is modulated by glibenclamide. Proc Natl Acad Sci USA 96:1268–1272CrossRefPubMed

62.

Zingman LV, Alekseev AE, Bienengraeber M et al. (2001) Signaling in channel/enzyme multimers: ATPase transitions in SUR module gate ATP-sensitive K⁺ conductance. Neuron 31:233–245PubMed

63.

Matsuo M, Dabrowski M, Ueda K, Ashcroft FM (2002) Mutations in the linker domain of NBD2 of SUR inhibit transduction but not nucleotide binding. EMBO J 21:4250–4258CrossRefPubMed

64.

Carrasco AJ, Dzeja PP, Alekseev AE et al. (2001) Adenylate kinase phosphotransfer communicates cellular energetic signals to ATP-sensitive potassium channels. Proc Natl Acad Sci USA 98:7623–7628PubMed

65.

Crawford RM, Ranki HJ, Botting CH, Budas GR, Jovanovic A (2002) Creatine kinase is physically associated with the cardiac ATP-sensitive K⁺ channel in vivo. FASEB J 16:102–104PubMed

66.

Matsuo M, Kioka N, Amachi T, Ueda K (1999) ATP binding properties of the nucleotide-binding folds of SUR1. J Biol Chem 274:37479–37482CrossRefPubMed

67.

Bienengraeber M, Alekseev AE, Abraham MR et al. (2000) ATPase activity of the sulfonylurea receptor: a catalytic function for the K_ATP channel complex. FASEB J 14:1943–1952PubMed

68.

Matsuo M, Tanabe K, Kioka N, Amachi T, Ueda K (2000) Different binding properties and affinities for ATP and ADP among sulfonylurea receptor subtypes, SUR1, SUR2A, and SUR2B. J Biol Chem 275:28757–28763CrossRefPubMed

69.

Thomas PM, Cote GJ, Wohllk N et al. (1995) Mutations in the sulfonylurea receptor gene in familial persistent hyperinsulinemic hypoglycemia of infancy. Science 268:426–429PubMed

70.

Kane C, Shepherd RM, Squires PE et al. (1996) Loss of functional K_ATP channels in pancreatic β-cells causes persistent hyperinsulinemic hypoglycemia of infancy. Nature Med 2:1344–1347PubMed

71.

Huopio H, Shyng SL, Otonkoski T, Nichols CG (2002) K_ATP channels and insulin secretion disorders. Am J Physiol 283:E207–E216

72.

Glaser B, Thornton P, Otonkoski T, Junien C (2000) Genetics of neonatal hyperinsulinism. Arch Dis Child Fetal Neonatal Ed 82:F79–F86PubMed

73.

Lonlay P de, Fournet JC, Touati G et al. (2002) Heterogeneity of persistent hyperinsulinaemic hypoglycaemia. A series of 175 cases. Eur J Pediatr 161:37–48PubMed

74.

Cartier EA, Conti LR, Vandenberg CA, Shyng SL (2001) Defective trafficking and function of K_ATP channels caused by a sulfonylurea receptor 1 mutation associated with persistent hyperinsulinemic hypoglycemia of infancy. Proc Natl Acad Sci 98:2882–2887CrossRefPubMed

75.

Tanizawa Y, Matsuda K, Matsuo M et al. (2000) Genetic analysis of Japanese patients with persistent hyperinsulinemic hypoglycemia of infancy: nucleotide-binding fold-2 mutation impairs cooperative binding of adenine nucleotides to sulfonylurea receptor 1. Diabetes 49:114–120PubMed

76.

Shyng SL, Ferrigni T, Shepard JB et al. (1998) Functional analyses of novel mutations in the sulfonylurea receptor 1 associated with persistent hyperinsulinemic hypoglycemia of infancy. Diabetes 47:1145–1151PubMed

77.

Reimann F, Huopio H, Dabrowski M et al. (2003) Characterisation of new K_ATP-channel mutations associated with congenital hyperinsulinism in the Finnish population Diabetologia 46:241–249

78.

Huopio H, Reimann F, Ashfield R et al. (2000) Dominantly inherited hyperinsulinism caused by a mutation in the sulfonylurea receptor type 1. J Clin Invest 106:897–906PubMed

79.

Huopio H, Otonkoski T, Vauhkonen I, Reimann F, Ashcroft FM, Laakso M (2003) A new subtype of autosomal dominant diabetes attributable to a mutation in the gene for sulfonylurea receptor 1. Lancet 361:301–307CrossRefPubMed

80.

Hani EH, Boutin P, Durand E et al. (1998) Missense mutations in the pancreatic islet beta cell inwardly rectifying K⁺ channel gene (KIR6.2/BIR): a meta-analysis suggests a role in the polygenic basis of Type II diabetes mellitus in Caucasians. Diabetologia 41:1511–1515CrossRefPubMed

81.

Gloyn AL, Weedon MN, Owen KR et al. (2003) Large-Scale Association Studies of Variants in Genes Encoding the Pancreatic beta cell K_ATP Channel Subunits Kir6.2 (KCNJ11) and SUR1 (ABCC8) Confirm That the KCNJ11 E23K Variant Is Associated With Type 2 Diabetes. Diabetes 52:568–572PubMed

82.

Love-Gregory L, Wasson J, Lin J, Skolnick G, Suarez B, Permutt MA (2003) An E23K single nucleotide polymorphism in the islet ATP-sensitive potassium channel gene (Kir6.2) contributes as much to the risk of Type II diabetes in Caucasians as the PPAR Pro12Ala variant. Diabetologia 46:136–137PubMed

83.

Schwanstecher C, Neugebauer B, Schulz M, Schwanstecher M (2002) The common single nucleotide polymorphism E23K in Kir6.2 sensitizes pancreatic beta cell ATP-sensitive potassium channels toward activation through nucleoside diphosphates. Diabetes 51 (Suppl 3):S363–S367PubMed

84.

Schwanstecher C, Meyer U, Schwanstecher M (2002) Kir6.2 polymorphism predisposes to type 2 diabetes by inducing overactivity of pancreatic beta cell ATP-sensitive K⁺ channels. Diabetes 51:875–879PubMed

85.

Hart LM 't, Haeften TW van, Dekker JM, Bot M, Heine RJ, Maassen JA (2002) Variations in insulin secretion in carriers of the E23K variant in the KIR6.2 subunit of the ATP-sensitive K⁺ channel in the beta cell. Diabetes 51:3135–3138PubMed

86.

Nielsen EM, Hansen L, Carstensen B et al. (2003) The E23K variant of Kir6.2 associates with impaired post-OGTT serum insulin response and increased risk of Type 2 diabetes. Diabetes 52:573–577PubMed

87.

Gribble FM, Tucker SJ, Ashcroft FM (1997) The interaction of nucleotides with the tolbutamide block of K-ATP currents: a reinterpretation. J Physiol 504:35–45PubMed

88.

Gros L, Virsolvy A, Salazar G, Bataille D, Blache P (1999) Characterization of low-affinity binding sites for glibenclamide on the Kir6.2 subunit of the beta cell K_ATP channel. Biochem Biophys Res Commun 257:766–770CrossRefPubMed

89.

Proks P, Reimann F, Green N, Gribble FM, Ashcroft FM (2002) Sulphonylurea stimulation of insulin secretion. Diabetes 51 [Suppl 3]:S368–S376

90.

Schmid-Antomarchi H, De Weille J, Fosset M, Lazdunski M (1987) The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K⁺ channel in insulin-secreting cells. J Biol Chem 262:15840–15844PubMed

91.

Ashfield R, Gribble FM, Ashcroft SJH, Ashcroft FM (1999) Identification of the high-affinity tolbutamide site on the SUR1 subunit of the K_ATP channel. Diabetes 48:1341–1347PubMed

92.

Hambrock A, Löffler-Walz C, Russ U, Lange U, Quast U (2001) Characterization of a mutant sulfonylurea receptor SUR2B with high affinity for sulfonylureas and openers: differences in the coupling to Kir6.x subtypes. Mol Pharmacol 60:190–199PubMed

93.

Muller G, Hartz D, Punter J, Okonomopulos R, Kramer W (1994) Differential interaction of glimepiride and glibenclamide with the beta cell sulfonylurea receptor. I. Binding characteristics. Biochim Biophys Acta 1191:267–277PubMed

94.

Hu S, Wang S, Fanelli B et al. (2000) Pancreatic beta cell K_ATP channel activity and membrane-binding studies with nateglinide: a comparison with sulfonylureas and repaglinide. J Pharmacol Exp Ther 293:444–452

95.

UK Prospective Diabetes Study Group (1995) United Kingdom Prospective Diabetes Study (UKPDS). 13: Relative efficacy of randomly allocated diet, sulphonylurea, insulin, or metformin in patients with newly diagnosed non-insulin dependent diabetes followed for three years. BMJ 310:83–88PubMed

96.

Clarke BF, Campbell IW (1975) Long-term comparative trial of glibenclamide and chlorpropamide in diet-failed, maturity-onset diabetics. Lancet 1:246–248PubMed

97.

Jennings AM, Wilson RM, Ward JD (1989) Symptomatic hypoglycemia in NIDDM patients treated with oral hypoglycemic agents. Diabetes Care 12:203–208PubMed

98.

Drouin P (2000) Diamicron MR once daily is effective and well tolerated in type 2 diabetes: a double-blind, randomized, multinational study. J Diabetes Complications 14:185–191CrossRefPubMed

99.

Sunaga Y, Gonoi T, Shibasaki T et al. (2001) The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K⁺ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol 431:119–125CrossRefPubMed

100.

Mikhailov MV, Mikhailova EA, Ashcroft SJ (2000) Investigation of the molecular assembly of beta cell K_ATP channels. FEBS Lett 482:59–64CrossRefPubMed

101.

Mikhailov MV, Mikhailova EA, Ashcroft SJ (2001) Molecular structure of the glibenclamide binding site of the beta cell K_ATP channel. FEBS Lett 499:154–160CrossRefPubMed

102.

Russ U, Hambrock A, Artunc F et al. (1999) Coexpression with the inward rectifier K⁺ channel Kir6.1 increases the affinity of the vascular sulfonylurea receptor SUR2B for glibenclamide. Mol Pharmacol 56:955–961PubMed

103.

Dorschner H, Brekardin E, Uhde I, Schwanstecher C, Schwanstecher M (1999) Stoichiometry of sulfonylurea-induced ATP-sensitive potassium channel closure. Mol Pharmacol 55:1060–1066PubMed

104.

Reimann F, Tucker SJ, Proks P, Ashcroft FM (1999) Involvement of the N-terminus of Kir6.2 in coupling to the sulphonylurea receptor. J Physiol 518:325–336PubMed

105.

Koster JC, Sha Q, Nichols CG (1999) Sulfonylurea and K⁺-channel opener sensitivity of K_ATP channels. Functional coupling of Kir6.2 and SUR1 subunits. J Gen Physiol 114:203–213CrossRefPubMed

106.

Babenko AP, Bryan J (2002) SUR-dependent modulation of K_ATP channels by an N-terminal Kir6.2 peptide. Defining intersubunit gating interactions. J Biol Chem 277:43997–44004CrossRefPubMed

107.

Zunkler BJ, Lins S, Ohno-Shosaku T, Trube G, Panten U (1988) Cytosolic ADP enhances the sensitivity to tolbutamide of ATP-dependent K⁺ channels from pancreatic B-cells. FEBS Lett 239:241–244CrossRefPubMed

108.

Schwanstecher C, Dickel C, Panten U (1992) Cytosolic nucleotides enhance the tolbutamide sensitivity of the ATP-dependent K⁺ channel in mouse pancreatic B cells by their combined actions at inhibitory and stimulatory receptors. Mol Pharmacol 41:480–486PubMed

109.

Reimann F, Dabrowski M, Jones P, Gribble F, Ashcroft FM (2003) Analysis of the differential modulation of sulphonylurea block of β-cell and cardiac K_ATP channels by Mg-nucleotides. J Physiol 547:159–168CrossRefPubMed

110.

Venkatesh N, Lamp ST, Weiss JN (1991) Sulfonylureas, ATP-sensitive K⁺ channels, and cellular K⁺ loss during hypoxia, ischemia, and metabolic inhibition in mammalian ventricle. Circ Res 69:623–637PubMed

111.

Findlay I (1993) Sulphonylurea drugs no longer inhibit ATP-sensitive K⁺ channels during metabolic stress in cardiac muscle. J Pharmacol Exp Ther 266:456–467PubMed

112.

Niki I, Nicks JL, Ashcroft SJ (1990). The beta cell glibenclamide receptor is an ADP-binding protein. Biochem J 268:713–718PubMed

113.

Schwanstecher M, Loser S, Brandt C, Scheffer K, Rosenberger F, Panten U (1992) Adenine nucleotide-induced inhibition of binding of sulphonylureas to their receptor in pancreatic islets. Br J Pharmacol 105:531–534PubMed

114.

Hambrock A, Loffler-Walz C, Kurachi Y, Quast U (1998) Mg²⁺ and ATP dependence of K_ATP channel modulator binding to the recombinant sulphonylurea receptor, SUR2B. Br J Pharmacol 125:577–583PubMed

115.

Loffler-Walz C, Hambrock A, Quast U (2002) Interaction of K_ATP channel modulators with sulfonylurea receptor SUR2B: implication for tetramer formation and allosteric coupling of subunits. Mol Pharmacol 61:407–614CrossRefPubMed

116.

Hambrock A, Loffler-Walz C, Quast U (2002) Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides. Br J Pharmacol 136:995–1004CrossRefPubMed

117.

Patel DJ, Purcell HJ, Fox KM (1999) Cardioprotection by opening of the K_ATP channel in unstable angina. Is this a clinical manifestation of myocardial preconditioning? Results of a randomized study with nicorandil. CESAR 2 investigation. Clinical European studies in angina and revascularization. Eur Heart J 20:51–57CrossRefPubMed

118.

D'hahan N, Moreau C, Prost AL et al. (1999) Pharmacological plasticity of cardiac ATP-sensitive potassium channels toward diazoxide revealed by ADP. Proc Natl Acad Sci USA 96:12162–12167PubMed

119.

Moreau C, Jacquet H, Prost AL, D'hahan N, Vivaudou M (2000) The molecular basis of the specificity of action of K_ATP channel openers. EMBO J 19:6644–6651CrossRefPubMed

120.

Bray KM, Quast U (1992) A specific binding site for K⁺ channel openers in rat aorta. J Biol Chem 267:11689–11692PubMed

121.

Terzic A, Jahangir A, Kurachi Y (1995). Cardiac ATP-sensitive K⁺ channels: regulation by intracellular nucleotides and K⁺ channel-opening drugs. Am J Physiol 269:C525–C545PubMed

122.

Reimann F, Gribble FM, Ashcroft FM (2000) Differential response of K_ATP channels containing SUR2A or SUR2B subunits to nucleotides and pinacidil. Mol Pharmacol 58:1318–1325PubMed

123.

Matsuoka T, Matsushita K, Katayama Y et al. (2000) C-terminal tails of sulfonylurea receptors control ADP-induced activation and diazoxide modulation of ATP-sensitive K⁺ channels. Circ Res 87:873–880PubMed

124.

Cogolludo AL, Perez-Vizcaino F, Fajardo S, Ibarra M, Tamargo J (1999) Effects of nicorandil as compared to mixtures of sodium nitroprusside and levcromakalim in isolated rat aorta. Br J Pharmacol 126:1025–1033PubMed

125.

Bijlstra PJ, Lutterman JA, Russel FGM, Thien T, Smits P (1996) Interaction of sulphonylurea derivatives with vascular ATP-sensitive potassium channels in humans. Diabetologia 39:1083–1090CrossRefPubMed

126.

Lawrence CL, Proks P, Rodrigo GC et al. (2001) Gliclazide produces high-affinity block of K_ATP channels in mouse isolated pancreatic β-cells but not rat heart or arterial smooth muscle cells. Diabetologia 44:1019–1025CrossRefPubMed

127.

Hata N, Takano M, Kunimi T, Kishida H, Takano T (2001) Lack of antagonism between nicorandil and sulfonylurea in stable angina pectoris. Int J Clin Pharmacol Res 21:59–63PubMed

128.

Carrasco AJ, Dzeja PP, Alekseev AE et al. (2002) M-LDH serves as a sarcolemmal K_ATP channel subunit essential for cell protection against ischemia. EMBO J 21:3936–3948CrossRefPubMed

129.

Fan Z, Makielski JC (1999) Phosphoinositides decrease ATP sensitivity of the cardiac ATP-sensitive K⁺ channel. A molecular probe for the mechanism of ATP-sensitive inhibition. J Gen Physiol 114:251–269.CrossRefPubMed

130.

Shyng SL, Nichols CG (1998) Membrane phospholipid control of nucleotide sensitivity of K_ATP channels. Science 282:1138–1141PubMed

131.

Krauter T, Ruppersberg JP, Baukrowitz T (2001) Phospholipids as modulators of K_ATP channels: distinct mechanisms for control of sensitivity to sulphonylureas, K⁺ channel openers, and ATP. Mol Pharmacol 59:1086–1093PubMed

132.

Inoue I, Nagase H, Kishi K, Higuti T (1991) ATP-sensitive K⁺ channel in the mitochondrial inner membrane. Nature 352:244–247PubMed

133.

Garlid KD (1996) Cation transport in mitochondria—the potassium cycle. Biochim Biophys Acta 1275:123–126CrossRefPubMed

134.

Grover GJ, Garlid KD (2000) ATP-sensitive potassium channels: a review of their cardioprotective pharmacology. J Mol Cell Cardiol 32:677–695PubMed

135.

Ozanne SE, Guest PC, Hutton JC, Hales CN (1995) Intracellular localization and molecular heterogeneity of the sulphonylurea receptor in insulin-secreting cells. Diabetologia 38:277–282CrossRefPubMed

136.

Geng X, Li L, Watkins S, Robbins PD, Drain P (2003) The insulin secretory granule is the major site of K_ATP channels of the endocrine pancreas. Diabetes 52:767–776PubMed

137.

Ozaki N, Shibasaki T, Kashima Y et al. (2000) cAMP-GEFII is a direct target of cAMP in regulated exocytosis. Nat Cell Biol 2:805–811CrossRefPubMed

138.

Kashima Y, Miki T, Shibasaki T et al. (2001) Critical role of cAMP-GEFII–Rim2 complex in incretin-potentiated insulin secretion. J Biol Chem 276:46046–46053CrossRefPubMed

139.

Kang G, Chepurny OG, Holz GG (2001) cAMP-regulated guanine nucleotide exchange factor II (Epac2) mediates Ca²⁺-induced Ca²⁺ release in INS-1 pancreatic beta cells. J Physiol 536:375–385PubMed

140.

Barg S, Eliasson L, Renstrom E, Rorsman P (2002) A subset of 50 secretory granules in close contact with L-type Ca2⁺ channels accounts for first-phase insulin secretion in mouse beta cells. Diabetes 51 Suppl 1:S74–S82

141.

UK Prospective Diabetes Study Group (1998) Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet 352:837–853PubMed

142.

Miki T, Nagashima K, Tashiro F et al. (1998) Defective insulin secretion and enhanced insulin action in K_ATP channel-deficient mice. Proc Natl Acad Sci USA 95:10402–10406.CrossRefPubMed

143.

Miki T, Iwanaga T, Nagashima K, Ihara Y, Seino S (2001) Roles of ATP-sensitive K⁺ channels in cell survival and differentiation in the endocrine pancreas. Diabetes 50 (Suppl 1):S48–S51PubMed

144.

Seghers V, Nakazaki M, DeMayo F, Aguilar-Bryan L, Bryan J (2000) Sur1 knockout mice. A model for K_ATP channel-independent regulation of insulin secretion. J Biol Chem 275:9270–9277CrossRefPubMed

145.

Nakazaki M, Crane A, Hu M et al. (2002) cAMP-activated protein kinase-independent potentiation of insulin secretion by cAMP is impaired in SUR1 null islets. Diabetes 51:3440–3449PubMed

146.

Shiota C, Larsson O, Shelton KD et al. (2002) Sulfonylurea receptor type 1 knock-out mice have intact feeding-stimulated insulin secretion despite marked impairment in their response to glucose. J Biol Chem 277:37176–37183CrossRefPubMed

147.

Chutkow WA, Samuel V, Hansen PA et al. (2001) Disruption of Sur2-containing K_ATP channels enhances insulin-stimulated glucose uptake in skeletal muscle. Proc Natl Acad Sci USA 98:11760–11764CrossRefPubMed

148.

Miki T, Minami K, Zhang L et al. (2002) ATP-sensitive potassium channels participate in glucose uptake in skeletal muscle and adipose tissue. Am J Physiol 283:E1178–E1184

149.

Miki T, Liss B, Minami K et al. (2001) ATP-sensitive K⁺ channels in the hypothalamus are essential for the maintenance of glucose homeostasis. Nat Neurosci 4:507–512PubMed

150.

Gross GJ, Fryer RM (1999) Sarcolemmal versus mitochondrial ATP-sensitive K⁺ channels and myocardial preconditioning. Circ Res 84:973–979PubMed

151.

Suzuki M, Li RA, Miki T et al. (2001) Functional roles of cardiac and vascular ATP-sensitive potassium channels clarified by Kir6.2-knockout mice. Circ Res 88:570–577PubMed

152.

Suzuki M, Sasaki N, Miki T et al. (2002) Role of sarcolemmal K_ATP channels in cardioprotection against ischemia/reperfusion injury in mice. J Clin Invest 109:509–516CrossRefPubMed

153.

Li RA, Leppo M, Miki T, Seino S, Marban E (2000) Molecular basis of electrocardiographic ST-segment elevation. Circ Res 87:837–839PubMed

154.

Miki T, Suzuki M, Shibasaki T et al. (2002) Mouse model of Prinzmetal angina by disruption of the inward rectifier Kir6.1. Nat Med 8:466–472CrossRefPubMed

155.

Chutkow WA, Pu J, Wheeler MT et al. (2002) Episodic coronary artery vasospasm and hypertension develop in the absence of Sur2 K_ATP channels. J Clin Invest 110:203–208CrossRefPubMed

156.

Zingman LV, Hodgson DM, Bast PH et al. (2002) Kir6.2 is required for adaptation to stress. Proc Natl Acad Sci USA 99:13278–13283CrossRefPubMed

157.

Tomai F, Crea F, Gaspardone A et al. (1994) Ischemic preconditioning during coronary angioplasty is prevented by glibenclamide, a selective ATP-sensitive K⁺ channel blocker. Circulation 90:700–705PubMed

158.

Kondo T, Kubota I, Tachibana H, Yamaki M, Tomoike H (1996) Glibenclamide attenuates peaked T wave in early phase of myocardial ischemia. Cardiovasc Res 31:683–687CrossRefPubMed

159.

Wilde AA (1996) ATP-sensitive potassium channels, transmural ischemia and the ECG implications for the non-insulin dependent diabetic patient? Cardiovasc Res 31:688–690

160.

Dhein S, Pejman P, Krusemann K (2000) Effects of the I_K.ATP blockers glibenclamide and HMR1883 on cardiac electrophysiology during ischemia and reperfusion. Eur J Pharmacol 398:273–284CrossRefPubMed

161.

Gong B, Miki T, Seino S, Renaud JM (2000) A K_ATP channel deficiency affects resting tension, not contractile force, during fatigue in skeletal muscle. Am J Physiol 279:C1351–C1358

162.

Yamada K, Ji JJ, Yuan H et al. (2001) Protective role of ATP-sensitive potassium channels in hypoxia-induced generalized seizure. Science 292:1543–1546PubMed

163.

Chang G, Roth CB (2001) Structure of MsbA from E. coli: a homolog of the multidrug resistance ATP binding cassette (ABC) transporters. Science 293:1793–1800CrossRefPubMed

Titel: Sulphonylurea action revisited: the post-cloning era
verfasst von: Dr. F. M. Gribble
F. Reimann
Publikationsdatum: 01.07.2003
Verlag: Springer-Verlag
Erschienen in: Diabetologia / Ausgabe 7/2003
Print ISSN: 0012-186X
Elektronische ISSN: 1432-0428
DOI: https://doi.org/10.1007/s00125-003-1143-3

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