Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor γ

Journal of Pharmacology and Experimental Therapeutics

Volumn 284, Issue 2, 1998, Pages 751-759

  Young, Paul W ^a   Buckle, Derek R ^a   Cantello, Barrie C C ^a   Chapman, Helen ^a   Clapham, John C ^a   Coyle, Paul J ^a   Haigh, David ^a   Hindley, Richard M ^a   Holder, Julie C ^a   Kallender, Howard ^a   Latter, Alison J ^a   Lawrie, Kenneth W M ^a   Mossakowska, Danuta ^a   Murphy, Gregory J ^a   Cox, Lynne Roxbee ^a   Smith, Stephen A ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; ANTIDIABETIC AGENT; GLUCOSE; GLUTATHIONE TRANSFERASE; HYBRID PROTEIN; INSULIN; ISOPROTEIN; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; PIOGLITAZONE; RADIOLIGAND; ROSIGLITAZONE; SB 217092; SB 219993; SB 219994; SB 236636; TROGLITAZONE; UNCLASSIFIED DRUG;

ADIPOCYTE; ADOLESCENT; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING COMPETITION; BINDING SITE; DRUG POTENCY; DRUG STRUCTURE; FEMALE; GLUCOSE TRANSPORT; HUMAN; HUMAN CELL; LIGAND BINDING; MALE; MOUSE; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR BINDING; STEREOCHEMISTRY;

3T3 CELLS; ADIPOCYTES; ANIMALS; BENZOXAZOLES; FEMALE; HUMANS; HYPOGLYCEMIC AGENTS; MALE; MICE; MICE, INBRED C57BL; MICE, OBESE; PHENYLPROPIONATES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZOLES; THIAZOLIDINEDIONES; TRANSCRIPTION FACTORS;

EID: 14444281382     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (30)

1. Altan N, Altan VM, Mikolay L, Larner J and Schwartz CFW (1985) Insulin-like and insulin-enhancing effects of the sulfonylurea glyburide on rat adipose glycogen synthase. Diabetes 34:281-287.
2. Berlan M and Lafontan M (1982) The alpha2-adrenergic receptor of receptor of human fat cell: Comparative studies of alpha2-adrenergic radioligand binding and biological response. J Physiol 78:279-287.
3. Bocos C, Gottlicher M, Geearing K, Banner C, Enmark E, Teboul M, Crickmore A and Gustafsson J (1995) Fatty acid activation of peroxisome proliferator-activated receptor (PPAR). J Steroid Biochem Mol Biol 53:467-473.
4. Buckle DR, Cantello BCC, Cawthorne MA, Coyle PJ, Dean DK, Faller A, Haigh D, Hindley RM, Jefcott LJ, Lister CA, Pinto IL, Rami HK, Smith DG and Smith SA (1996) Non-thiazolidinedione antihyperglycaemic agents. 2: α-Carbon substituted β-phenylpropanoic acids. Bioorg Med Chem Lett 6:2127-2130.
5. Cantello BCC, Cawthorne MA, Cottam GP, Duff PT, Haigh D, Hindley RM, Lister CA, Smith SA and Thurlby PL (1994) ([ω-(Heterocyclylamino)alkoxy]benzyl]-24-thiazolidinediones as potent antihyperglycaemic agents. J Med Chem 37:3977-3985.
6. Clapham JC, Smith SA, Moore GBT, Hughes MG, Azam H, Scott A and Jung RT (1997) Plasma leptin concentrations and OB gene expression in subcutaneous adipose tissue are not regulated acutely by physiological hyperinsulinaemia in lean and obese humans. Int J Obes 21:179-183.
7. 4 pathway to inflammation control. Nature 384:39-43.
8. 2. Biochem Biophys Res Commun 224:431-437.
9. 2 is a ligand for the adipocyte determination factor PPARgamma. Cell 83:803-812.
10. Frost SC and Lane MD (1985) Evidence for the involvement of vicinal sulfhydryl groups in insulin activated hexose transport by 3T3-L1 adipocytes. J Biol Chem 260:2646-2652.
11. Gibbs EM, Genereux PE, Andrews NJ and Stevenson RW (1989) A novel antidiabetic agent, CP-68,722, increases levels of glucose transport and glucose transporter protein in 3T3-L1 adipocytes (Abstract). Diabetologia 32:491a.
12. Green A (1983) Catecholamines inhibit insulin-stimulated glucose transport in adipocytes in the presence of adenosine deaminase. FEBS Lett 153:261-264.
13. Hulin B, McCarthy PA and Gibbs EM (1996) The glitazone family of antidiabetic agents. Curr Pharmaceut Design 2:85-102.
14. Ibrahimi A, Teboul L, Gaillard D, Amri EZ, Ailhaud G, Young PW, Cawthorne MA and Grimaldi PA (1994) Evidence for a common mechanism of action for fatty acids and thiazolidinedione antidiabetic agents on gene expression in preadipose cells. Mol Pharmacol 46:1070-1076.
15. Inoue A, Yamakawa J, Yukioka M and Morisawa S (1983) Filter-binding assay procedure for thyroid hormone receptors. Anal Biochem 134:176-183.
16. Kletzien RF, Clarke SD and Ulrich RG (1992) Enhancement of adipocyte differentiation by an insulin-sensitizing agent. Mol Pharmacol 41:393-398.
17. Kliewer SA, Forman BM, Blumberg B, Ong ES, Borgmeyer U, Mangelsdorf DJ, Umesono K and Evans RM (1994) Differential expression and activation of a family of murine peroxisome proliferator-activated receptors. Proc Natl Acad Sci USA 91:7344-7359.
18. 2 metabolite binds peroxisome proliferator activated receptor gamma and promotes adipocyte differentiation. Cell 83:813-819.
19. Larrouy D, Galitzky J and Lafontan M (1991) A1 adenosine receptors in the human fat cell: Tissue distribution and regulation of radioligand binding. Eur J Pharmacol 206:139-147.
20. Lehmann JM, Moore LB, Smith Oliver TA, Wilkinson WO, Willson TM and Kliewer SA (1995) An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator activated receptor gamma (PPARgamma). J Biol Chem 270:12963-12966.
21. Lenhard JM, Harnacher L, Paulik M, Beck K, Kliewer SA, Lehmann JM, Cobb J, Henke B, Wilson T, Parks D and Blanchard SG (1996) Analysis of thiazolidinedione biguanide and retinoid effects on adipogenesis and the nuclear receptors PPARgamma and RXR (Abstract). Diabetologia 39: suppl 1, A234.
22. O'Reilly DR, Miller LK and Luckow VA (1994) Baculovirus Expression Vectors. Oxford University Press, New York/Oxford.
23. Rodbell M (1964) Metabolism of isolated fat cells. I. Effects of hormones on glucose metabolism and lipolysis. J Biol Chem 239:375-380.
24. Sheppard KE and Funder JW (1996) Specific nuclear localization of 11-dehydrocorticosterone in rat colon: Evidence for a novel corticosteroid receptor. Endocrinology 137:3274-3278.
25. Tontonez P, Hu E, Graves RA, Budavari AI and Spiegelman BM (1994) mPPARgamma2: Tissue-specific regulator of an adipocyte enhancer. Genes Dev 8:1224-1234.
26. Willson TM, Cobb JE, Cowan DJ, Weithe RW, Correa IT, Prakash SR, Beck KD, Moore LB, Kliewer SA and Lehmann JM (1996) The structure-activity relationship between peroxisome-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem 39:665-668.
27. Young PW, Cawthorne MA, Coyle PJ, Holder JC, Holman GD, Kozka IJ, Lister CA and Smith SA (1995) Repeat treatment of obese mice with BRL 49653, a novel and potent insulin sensitiser, enhances insulin action in white adipocytes: Association with increased insulin binding and cell-surface glucose transporter (GLUT-4) as measured by photoaffinity labelling. Diabetes 44:1087-1092.
28. Yu K, Bayona W, Kallens CB, Harding HP, Ravera CP, McMahon G, Brown M and Lazar MA (1995) Differential activation of peroxisome proliferator-activated receptors by eicosanoids. J Biol Chem 270:23975-23983.
29. Zhu Y, Chao Q, Korenberg JR, Chen X, Noya D, Rao SM and Reddy JK (1997) Structural organization of mouse peroxisome proliferator-activated receptor gamma (mPPARgamma) gene: Alternative promoter use and different splicing yield two mPPARgamma isoforms. Proc Natl Acad Sci USA 92:7921-7925.
30. Zuber MX, Wang S, Thammavaram KV, Reed DK and Reed BC (1985) Elevation of the number of cell-surface insulin receptors and the rate of 2-deoxyglucose uptake by exposure of 3T3-L1 adipocytes to tolbutamide. J Biol Chem 260:14045-14062.