Testing the bipartite model of the sulfonylurea receptor binding site: Binding of A-, B-, and a + B-site ligands

Journal of Pharmacology and Experimental Therapeutics

Volumn 322, Issue 2, 2007, Pages 701-708

  Winkler, Marcus ^a   Stephan, Damian ^a   Bieger, Susanne ^a   Kühner, Petra ^a   Wolff, Felix ^a   Quast, Ulrich ^a  

^a UNIVERSITY OF TÜBINGEN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

4 [2 (3,4 DIHYDRO 7 METHOXY 4,4 DIMETHYL 1,3 DIOXO 2(1H) ISOQUINOLYL)ETHYL]BENZOIC ACID; 4 [[2 (1 PIPERIDYL)BENZHYDRYL]CARBAMOYLMETHYL]BENZOIC ACID; ADENOSINE TRIPHOSPHATE SENSITIVE POTASSIUM CHANNEL; BENZENE DERIVATIVE; BENZOIC ACID DERIVATIVE; GLIBENCLAMIDE; GLIBENCLAMIDE H 3; GLIBORNURIDE; GLICLAZIDE; GLIMEPIRIDE; GLIQUIDONE; INWARDLY RECTIFYING POTASSIUM CHANNEL SUBUNIT KIR6.2; MEGLITINIDE; NATEGLINIDE; RADIOPHARMACEUTICAL AGENT; REPAGLINIDE; SERINE; SULFONYLUREA; SULFONYLUREA RECEPTOR; SULFONYLUREA RECEPTOR 1; SULFONYLUREA RECEPTOR 2; TYROSINE; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; DRUG RECEPTOR BINDING; EMBRYO; GENE MUTATION; HUMAN; HUMAN CELL; INSULIN BINDING; INSULIN RELEASE; NUCLEOTIDE SEQUENCE; PANCREAS ISLET BETA CELL; PRIORITY JOURNAL;

AMINO ACID SUBSTITUTION; ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BINDING SITES; BINDING, COMPETITIVE; CARBAMATES; CELL LINE; CYCLOHEXANES; DOSE-RESPONSE RELATIONSHIP, DRUG; GLYBURIDE; HYPOGLYCEMIC AGENTS; LIGANDS; MICE; MOLECULAR STRUCTURE; PHENYLALANINE; PIPERIDINES; POTASSIUM CHANNELS; POTASSIUM CHANNELS, INWARDLY RECTIFYING; PROTEIN BINDING; RADIOLIGAND ASSAY; RATS; RECEPTORS, DRUG; SULFONYLUREA COMPOUNDS; TRANSFECTION;

EID: 34547116194     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.107.123224     Document Type: Article

References (35)

1. Aguilar-Bryan L and Bryan J (1999) Molecular biology of adenosine triphosphate-sensitive potassium channels. Endocr Rev 20:101-135.
2. ATP channel. Diabetes 48:1341-1347.
3. ATP channel closure. FEBS Lett 459: 367-376.
4. Berg JM, Tymoczko JL, and Stryer L (2002) Biochemistry, W.H. Freeman and Company, New York.
5. Bevington PR (1969) Data Reduction and Error Analysis for the Physical Sciences, McGraw-Hill, New York.
6. Brown GR and Foubister AJ (1984) Receptor binding sites of hypoglycemic sulfonylureas and related [(acylamino)alkyl]benzoic acids. J Med Chem 27:79-81.
7. ATP channels. Curr Pharm Design 11:2699-2716.
8. ATP channels. J Pharmacol Exp Ther 304:1025-1032.
9. 50) of an enzymatic reaction. Biochem Pharmacol 22:3099-3108.
10. Christopoulos A (1998) Assessing the distribution of parameters in models of ligand-receptor interaction: to log or not to log. Trends Pharmacol Sci 19:351-357.
11. Dabrowski M, Wahl P, Holmes WE, and Ashcroft FM (2001) Effect of repaglinide on cloned beta cell, cardiac and smooth muscle types of ATP-sensitive potassium channels. Diabetologia 44:747-756.
12. Giblin JP, Leaney JL, and Tinker A (1999) The molecular assembly of ATP-sensitive potassium channels: determinants on the pore forming subunit. J Biol Chem 274:22652-22659.
13. ATP channels to gliclazide. Diabetologia 42:845-848.
14. Gribble FM and Reimann F (2003) Sulphonylurea action revisited: the post-cloning era. Diabetologia 46:875-891.
15. ATP channels. Diabetes 47:1412-1418.
16. ATP channel modulator binding to the recombinant sulphonylurea receptor, SUR2B. Br J Pharmacol 125:577-583.
17. Hambrock A, Löffler-Walz C, and Quast U (2002) Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides. Br J Pharmacol 136:995-1004.
18. Hambrock A, Löffler-Walz C, Russ U, Lange U, and 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 60:190-199.
19. Hansen AMK, Christensen IT, Hansen JB, Carr RD, Ashcroft FM, and Wahl P (2002) Differential interactions of nateglinide and repaglinide on the human β-cell sulphonylurea receptor 1. Diabetes 51:2789-2795.
20. ATP channels. Br J Pharmacol 144:551-557.
21. ATP channel modulators with sulfonylurea receptor SUR2B: implication for tetramer formation and allosteric coupling of subunits. Mol Pharmacol 61:407-414.
22. 3H-glibenclamide binding in rat aortic rings. Naunyn Schmiedebergs Arch Pharmacol 357:183-185.
23. ATP channels by SUR1 and SUR2A. J Mol Cell Cardiol 39:491-501.
24. Mikhailov MV, Mikhailova EA, and Ashcroft SJH (2001) Molecular structure of the glibenclamide binding site of the β-cell K-ATP channel. FEBS Lett 499:154-160.
25. Proks P, Reimann F, Green N, Gribble F, and Ashcroft F (2002) Sulfonylurea stimulation of insulin secretion. Diabetes 51 (Suppl 3):S368-S376.
26. + channel subtype selectivity of insulin secretagogues for the coronary vasculature and the myocardium. Diabetes 53:S156-S164.
27. ATP) channels by Mg-nucleotides. J Physiol 547:159-168.
28. Rufer C and Losert W (1979) Blood glucose lowering sulfonamides with asymmetric carbon atoms: III. Related N-substituted carbamoylbenzoic acids. J Med Chem 22:750-752.
29. + channel Kir6.1 increases the affinity of the vascular sulfonylurea receptor SUR2B for glibenclamide. Mol Pharmacol 56:955-961.
30. + channels. Prog Biophys Mol Biol 81:133-176.
31. Stephan D, Stauß, Lange U, Felsch H, Löffler-Walz C, Hambrock A, Russ U, and Quast U (2005) The mutation Y1206S increases the affinity of the sulphonylurea receptor SUR2A for glibenclamide and enhances the effects of coexpression with Kir6.2. Br J Pharmacol 144:1078-1088.
32. ATP channels. Diabetologia 49:2039-2048.
33. Sturgess NC, Ashford ML, Cook DL, and Hales CN (1985) The sulphonylurea receptor may be an ATP-sensitive potassium channel. Lancet 2:474-475.
34. Uhde I, Toman A, Gross I, Schwanstecher C, and Schwanstecher M (1999) Identification of the potassium channel opener site on sulfonylurea receptors. J Biol Chem 274:28079-28082.
35. Vila-Carriles WH, Zhao G, and Bryan J (2007) Defining a binding pocket for sulfonylureas in ATP-sensitive potassium channels. FASEB J 21:18-25.