Glitazones: clinical effects and molecular mechanisms

References

• Matthaei S, Stumvoll M, Kellerer M, Haring HU. Pathoph-siology and pharmacological treatment of insulin resistance. Endocr Rev 2000; 21: 585–618.
   PubMed Web of Science ®Google Scholar
• Dinneen S, Gerich J, Rizza R. Carbohydrate metabolism in non-insulin-dependent diabetes mellitus. N Engl J Med 1992; 327: 707–13.
   PubMed Web of Science ®Google Scholar
• Groop LC, Bonadorma RC, DelPrato S, Ratheiser K, Zyck K, Ferrannini E, et al. Glucose and free fatty acid metabolism in non-insulin-dependent diabetes mellitus. Evi-dence for multiple sites of insulin resistance. J Clin Invest 1989; 84: 205–13.
   PubMed Web of Science ®Google Scholar
• Bruning JC, Gautam D, Burks DJ, Gillette J, Schubert M, Orban PC, et al. Role of brain insulin receptor in control of body weight and reproduction. Science 2000; 289: 2122–5.
   PubMed Web of Science ®Google Scholar
• Hsueh W, Law RE, Saad M, Dy J, Feener E, King G. Insulin resistance and macrovascular disease. Curr Opin Endocrinol Diab 1996; 3: 346–54.
   Google Scholar
• Taskinen M-R. Hyperlipidaemia in diabetes. Baillieres Best Pract Res Clin Endocrinol Metab 1990; 4: 743–75.
   PubMedGoogle Scholar
• Trovati M, Anfossi G. Insulin, insulin resistance and platelet function: similarities with insulin effects on cultured vascular smooth muscle cells. Diabetologia 1998; 41: 609–22.
   PubMed Web of Science ®Google Scholar
• Balletshofer BM, Rittig K, Enderle MD, Volk A, Maerker E, Jacob S, et al. Endothelial dysfunction is detectable in young normotensive first-degree relatives of subjects with type 2 diabetes in association with insulin resistance. Circulation 2000; 101: 1780–4.
   PubMed Web of Science ®Google Scholar
• Must A, Spadano J, Coakley EH, Field AE, Colditz G, Dietz WH. The disease burden associated with overweight and obesity. JAMA 1999; 282: 1523–9.
   PubMed Web of Science ®Google Scholar
• Boden G. Role of fatty acids in the pathogenesis of insulin resistance and NIDDM. Diabetes 1997; 46: 3–10.
   PubMed Web of Science ®Google Scholar
• Friedman JM, Halaas JL. Leptin and the regulation of body weight in mammals. Nature 1998; 395: 763–70.
   PubMed Web of Science ®Google Scholar
• Berti L, Kellerer M, Capp E, Haring HU. Leptin stimulates glucose transport and glycogen synthesis in C2C12 myotubes: evidence for a P13-kinase mediated effect. Diabetologia 1997; 40: 606–9.
   PubMed Web of Science ®Google Scholar
• Cohen B, Novick D, Rubinstein M. Modulaticn of insulin activities by leptin. Science 1996; 274: 1185–8.
   PubMed Web of Science ®Google Scholar
• Sempoux C, Guiot Y, Dubois D, Moulin P, Rahier J. Human type 2 diabetes: morphological evidence for abnormal beta-cell function. Diabetes 2001; 50 Suppl 1: S172–7.
   Google Scholar
• Hotamisligil GS, Amer P, Atkinson RL, Spiegelman BM. Differential regulation of the p80 tumor necrosis factor receptor in human obesity and insulin resistance. Diabetes 1997; 46: 451–5.
   PubMed Web of Science ®Google Scholar
• Hotamisligil GS, Shargill NS, Spiegelman BM. Adipose expression of tumor necrosis factor-alpha: direct role in obesity-linked insulin resistance. Science 1993; 259: 87–91.
   PubMed Web of Science ®Google Scholar
• Ofei F, Hurel S, Newkirk J, Sopwith M, Taylor R. Effects of an engineered human anti-TNF-alpha antibody (CDP571) on insulin sensitivity and glycemic control in patients with NIDDM. Diabetes 1996; 45: 881–5.
   PubMed Web of Science ®Google Scholar
• Mohamed-Ali V, Goodridc S, Bulmer K, Holly JM, Yudlcin JS, Coppadc SW. Production of soluble tumor necrosis factor receptors by human subcutaneous adipose tissue in vivo. Am J Physiol Endocrinol Metab 1999; 277: E971–5.
   PubMed Web of Science ®Google Scholar
• Rui L, Aguirre V, Kim JK, Shulman GI, Lee A, Corbould A, et al. Insulin/IGF-1 and TNF-alpha stimulate phosphorylaticn of IRS-1 at inhibitory Ser307 via distinct pathways. J Clin Invest 2001; 107: 181–9.
   PubMed Web of Science ®Google Scholar
• Kroder G, Bossemnaier B, Kellerer M, Capp E, Stoyanov B, Muhlhofer A, et al. Tumor necrosis factor-alpha- and hyperglycemia-induced insulin resistance. Evidence for differ-ent mechanisms and different effects on insulin signaling. J Clin Invest 1996; 97: 1471–7.
   PubMed Web of Science ®Google Scholar
• Hotamisligil GS, Murray DL, Choy LN, Spiegelman BM. Tumor necrosis factor alpha inhibits signaling from the insulin receptor. Proc Nat! Acad Sci USA 1994; 91: 4854–8.
   PubMed Web of Science ®Google Scholar
• Steppan CM, Bailey ST, Bhat S, Brown EJ, Baernee RR, Wright CM, et al. The hormone resistin links obesity to diabetes. Nature 2001; 409: 307–12.
   PubMed Web of Science ®Google Scholar
• Hu E, Liang P, Spiegelman BM. AdipoQ is a novel adipose-specific gene dysregulated in obesity. J Biol Chem 1996; 271: 10697–703.
   PubMed Web of Science ®Google Scholar
• Scherer PE, Williams S, Fogliano M, Baldini G, Lodish HF. A novel serum protein similar to C1q, produced exclusively in adipocytes. J Biol Chem 1995; 270: 26746–9.
   PubMed Web of Science ®Google Scholar
• Weyer C, Funahashi T, Tanaka S, Hotta K, Matsuzawa Y, Pratley RE, et al. Hypoadiponectinemia in obesity and type 2 diabetes: close association with insulin resistance and hyper-insulinemia. J Clin Endocrinol Metab 2001; 86: 1930–5.
   PubMed Web of Science ®Google Scholar
• Takahashi M, Arita Y, Yamagata K, Matsukawa Y, Oku-tomi K, Hone M, et al. Genomic structure and mutations in adipose-specific gene, adiponectin. Int J Obes Relat Metab Disord 2000; 24: 861–8.
   PubMed Web of Science ®Google Scholar
• Yang WS, Lee WJ, Funahashi T, Tanaka S, Matsuzawa, Y, Chao CL, et al. Weight reduction increases plasma levels of an adipose-derived anti-inflammatory protein, adiponectin. J Clin Endocrinol Metab 2001; 86: 3815–9.
   PubMed Web of Science ®Google Scholar
• Yamauchi T, Kamon J, Waki H, Terauchi K, Kubota N, Hara K, et al. The fat-derived hormone adiponectin reverses insulin resistance associated with both lipoatrophy and obesity. Nat Med 2001; 7: 941–6.
   PubMed Web of Science ®Google Scholar
• Fujita T, Sugiyama Y, Taketomi S, Sohda T, Kawamatsu Y, Iwatsuka H, et al. Reduction of insulin resistance in obese and/or diabetic animals by 544- (1-methylcyclohexylmethoxy)-benzy1]-thiazolidine-2,4-dione (ADD-3878, U-63,287, ciglita-zone), a new antidiabetic agent. Diabetes 1983; 32: 804–10.
   PubMed Web of Science ®Google Scholar
• Fujiwara T, Okuno A, Yoshioka S, Horikoshi H. Suppres-sion of hepatic gluconeogenesis in long-term Troglitazone treated diabetic KK and C57BL/Ksj-db/db mice. Metabolism 1995; 44: 486–90.
   PubMedGoogle Scholar
• Stevenson RW, Hutson NJ, Krupp MN, Volkmann RA, Holland GF, Eggjer JF, et al. Actions of novel antidiabetic agent englitazone in hyperglycemic hyperinsulinemic ob/ob mice. Diabetes 1990; 39: 1218–27.
   PubMed Web of Science ®Google Scholar
• Kirsch DM, Bachmann W, Haring HU. Ciglitazone reverses cAMP-induced post-insulin receptor resistance in rat adipo-cytes. FEBS Lett 1984; 176: 49–54.
   Google Scholar
• Fujiwara T, Wada M, Fukuda K, Fukami M, Yoshioka S, Yoshioka T, et al. Characterization of CS-045, a new oral antidiabetic agent, II. Effects on glycemic control and pancreatic islet structure at a late stage of the diabetic syndrome in C57BL/KsJ-db/db mice. Metabolism 1991; 40: 1213–8.
   PubMed Web of Science ®Google Scholar
• Gale EA. Lessons from the glitazones: a story of drug development. Lancet 2001; 357: 1870–5.
   Google Scholar
• Raskin P, Rendell M, Riddle MC, Dole JF, Freed MI, Rosenstock J. A randomized trial of rosiglitazorr therapy in patients with inadequately controlled insulin-treated type 2 diabetes. Diabetes Care 2001; 24: 1226–32.
   PubMed Web of Science ®Google Scholar
• Aronoff S, Rosenblatt S, Braithwaite S, Egan JW, Mathisen AL, Schneider RI. Pioglitazorr hydrochloride monotherapy improves glycemic control in the treatment of patients with type 2 diabetes: a 6-month randomized placebo-controlled dose-response study. The Pioglitazone 001 Study Group. Diabetes Care 2000; 23: 1605–11.
   PubMed Web of Science ®Google Scholar
• Horton ES, Whitehouse F, Ghazzi MN, Venable TC, Whitcomb RW. Troglitazorr in combination with sulfony-lurea restores glycemic control in patients with type 2 diabetes. Diabetes Care 1998; 21: 1462–9.
   PubMed Web of Science ®Google Scholar
• Wang M, Wise SC, Leff T, Su T-Z. Troglitazone, an antidiabetic agent, inhibits cholesterol biosynthesis through a mechanism independent of peroxisome proliferator-activated receptor-gamma. Diabetes 1999; 48: 254–60.
   Google Scholar
• Buchanan TA, Meehan WP, Jeng YY, Yang D, Chan TM, Nadler JL, et al. Blood pressure lowering by pioglitazone. Evidence for a direct vascular effect. J Clin Invest 1995; 96: 354–60.
   PubMed Web of Science ®Google Scholar
• Cominacini L, Young MMR, Capriati A, Garbin U, Fratta Pasini A, Campagnola M, et al. Troglitazorr increases the resistance of low densitiy lipoprotein to oxidation in healthy volunteers. Diabetologia 1997; 40: 1211–8.
   PubMed Web of Science ®Google Scholar
• Steinberg D, Parthasarathy S, Carew TE, Khoo JC, Witztum JL. Beyond cholesterol. Modifications of low-density lipoprotein that increase its atherogenicity. N Engl J Med 1989; 320: 915–24.
   PubMed Web of Science ®Google Scholar
• Porte D, Jr., Kahn SE. beta-cell dysfunction and failure in type 2 diabetes: potential mechanisms. Diabetes 2001; 50 Suppl 1: S160–3.
   PubMedGoogle Scholar
• Suter SL, Nolan JJ, Wallace P, Gumbiner B, Olefsky JM. Metabolic effects of new oral hypoglycemic agent CS-045 in NIDDM subjects. Diabetes Care 1992; 15: 193–203.
   Google Scholar
• Antonucci T, Whitcomb R, McLain R, Lockwood D. Impaired glucose tolerance is normalized by treatment with the thiazolidinediom troglitazone. Diabetes Care 1997; 20: 188–93.
   PubMed Web of Science ®Google Scholar
• Kawamori R, Matsuhisa M, Kinoshita J, Mochizulci K, Niwa M, Arisaka T, et al. Pioglitazorr enhances splanchnic glucose uptake as well as peripheral glucose uptake in non-insulin-dependent diabetes mellitus. AD-4833 Clamp-OGL Study Group. Diabetes Res Clin Pract 1998; 41: 35–43.
   PubMed Web of Science ®Google Scholar
• Nolan JJ, Ludvik B, Beerdsen P, Joyce M, Olefsky J. Improvement in glucose tolerance and insulin resistance in obese subjects treated with troglitazone. N Engl J Med 1994; 331: 1188–93.
   PubMed Web of Science ®Google Scholar
• Maggs DG, Buchanan TA, Burant CF, Cline G, Gumbiner B, Hsueh WA, et al. Metabolic effects of troglitazone monotherapy in type 2 diabetes mellitus. A randomized, double-blind, placebo-controlled trial. Ann Intern Med 1998; 128: 176–85.
   PubMedGoogle Scholar
• Tominaga M, Igarashi M, Daimon M, Eguchi H, Matsu-moto M, Sekikawa A, et al. Thiazolidinediones (AD-4833 and CS-045) improve hepatic insulin resistance in streptozo-tocin-induced diabetic rats. Endocr J 1993; 40: 343–9.
   PubMed Web of Science ®Google Scholar
• Lee MK, Olefsky JM. Acute effects of troglitazone on in vivo insulin action in normal rats. Metabolism 1995; 44: 1166–9.
   Google Scholar
• Desvergne B, Wahli W. Peroxisome proliferator-activated receptors: nuclear control of metabolism. Endocr Rev 1999; 20: 649–88.
   PubMed Web of Science ®Google Scholar
• Forman BM, Tontonoz P, Chen J, Brun RP, Spiegelman BM, Evans RM. 15-Deoxy-delta 12,14-prostaglandin J2 is a ligand for the adipocyte determination factor PPAR gamma. Cell 1995; 83: 803–12.
   PubMed Web of Science ®Google Scholar
• Tafuri SR. Troglitazone enhances differentiation, basal glucose uptake, and Glut1 protein levels in 3T3-L1 adipocytes. Endocrinology 1996; 137: 4706–12.
   PubMed Web of Science ®Google Scholar
• Teboul L, Gaillard D, Staccini L, Inadera H, Amri EZ, Grimaldi PA. Thiazolidinediones and fatty acids convert myogenic cells into adipose-like cells. J Biol Chem 1995; 270: 28183–7.
   PubMed Web of Science ®Google Scholar
• Tontonoz P, Hu E, Spiegehnan BM. Stimulation of adipo-genesis in fibroblasts by PPAR gamma 2, a lipid-activated transcription factor. Cell 1994; 79: 1147–56.
   PubMed Web of Science ®Google Scholar
• Loviscach M, Rehman N, Carter L, Mudaliar S, Mohadeen P, Ciaraldi TP, et al. Distributicn of peroxisome proliferator-activated receptors (PPARs) in human skeletal muscle and adipose tissue: relation to insulin action. Diabetologia 2000; 43: 304–11.
   PubMed Web of Science ®Google Scholar
• Park KS, Ciaraldi TP, Abrams Carter L, Mudaliar S, Nikoulina SE, Henry RR. Troglitazone regulation of glucose metabolism in human skeletal muscle cultures from obese type II diabetic subjects. J Clin Endocrinol Metab 1998; 83: 1636–43.
   PubMed Web of Science ®Google Scholar
• Burant CF, Sreenan S, Hirano K, Tai TA, Lohmiller J, Lukens J, et al. Troglitazorr action is independent of adipose tissue. J Clin Invest 1997; 100: 2900–8.
   Google Scholar
• Yamauchi T, Kamon J, Waki H, Murakami K, Motojima K, Komeda K, et al. The mechanisms by which both hetero-zygous PPARgamma deficiency and PPARgamma agonist improve insulin resistance. J Biol Chem 2001; 276: 41245–54.
   PubMed Web of Science ®Google Scholar
• Oakes ND, Thalen PG, Jacinto SM, Ljung B. Thiazolidine-diones increase plasma-adipo tissue FFA exchange capacity and enhance insulin-mediated control of systemic FFA avail-ability. Diabetes 2001; 50: 1158–65.
   PubMed Web of Science ®Google Scholar
• Schoonjans K, Martin G, Staels B, Auwerx J. Peroxisome proliferator-activated receptors, orphans with ligands and functions. Curr Opin Lipidol 1997; 8: 159–66.
   PubMed Web of Science ®Google Scholar
• Miyazaki Y, Glass L, Triplitt C, Matsuda M, Cusi K, Mahankali A, et al. Effect of rosiglitazone on glucose and non-esterified fatty acid metabolism in Type II diabetic patients. Diabetologia 2001; 44: 2210–9.
   PubMed Web of Science ®Google Scholar
• Hofmann C, Lorenz K, Braithwaite SS, Colca JR, Palazuk BJ, Hotamisligil GS, et al. Altered gene expression for tumor necrosis factor-? and its receptor during drug and dietary modulation of insulin resistance. Endocrinology 1994; 134: 264–70.
   PubMed Web of Science ®Google Scholar
• De Vos P, Lefebvre AM, Miller SG, Guerre-Millo M, Wong K, Saladin R, et al. Thiazolidinediones repress ob gene expression in rodents via activation of peroxisome prolifera-tor-activated receptor gamma. J Clin Invest 1996; 98: 1004–9.
   PubMed Web of Science ®Google Scholar
• Kallen CB, Lazar MA. Antidiabetic thiazolidinediones inhibit leptin (ob) gene expression in 3T3-L1 adipocytes. Proc Nat! Acad Sci USA 1996; 93: 5793–6.
   PubMed Web of Science ®Google Scholar
• Maeda N, Takahashi M, Funahashi T, Kihara S, Nishizawa H, Kishida K, et al. PPARgamma ligands increase expression and plasma concentrations of adiponectin, an adipose-derived protein. Diabetes 2001; 50: 2094–9.
   PubMed Web of Science ®Google Scholar
• Scheen AJ. Thiazolidinediones and liver toxicity. Diabetes Metab 2001; 27: 305–13.
   PubMed Web of Science ®Google Scholar
• Maeda K. Hepatocellular injury in a patient receiving pioglitazone. Ann Intern Med 2001; 135: 306.
   PubMed Web of Science ®Google Scholar
• Al Sahnan J, Arjomand H, Kemp DG, Mittal M. Hepato-cellular injury in a patient receiving rosiglitazone. A case report. Ann Intern Med 2000; 132: 121–4.
   Google Scholar
• Forman LM, Simmons DA, Diamond RH. Hepatic failure in a patient taking rosiglitazone. Ann Intern Med 2000; 132: 118–21.
   PubMed Web of Science ®Google Scholar
• Baldwin SJ, Clarke SE, Chenery RJ. Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of rosiglitazone. Br J Clin Pharmacol 1999; 48: 424–32.
   PubMed Web of Science ®Google Scholar
• Isley WL, Oki JC. Rosiglitazone and liver failure. Ann Intern Med 2000; 133: 393.
   PubMed Web of Science ®Google Scholar
• Dunaif A, Scott D, Finegood D, Quintana B, Whitcomb R. The insulin-sensitizing agent troglitazom improves metabolic and reproductive abnormalities in the polycystic ovary syndrome. J Clin Endocrinol Metab 1996; 81: 3299–306.
   PubMed Web of Science ®Google Scholar
• Patel J, Anderson RJ, Rappaport EB. Rosiglitazorr mono-therapy improves glycemic control in patients with type 2 diabetes: a twelve-week, randomized, placebo-controlled study. Diab Obes Metab 1999; 1: 165–72.
   Google Scholar
• Adams M, Montague CT, Prins JB, Holder JC, Smith SA, Sanders L, et al. Activators of peroxisome proliferator-activated receptor gamma have depot-specific effects on human preadipocyte differentiation. J Clin Invest 1997; 100: 3149–53.
   Google Scholar
• Akazawa S, Sun F, Ito M, Kawasaki E, Eguchi K. Efficacy of troglitazone on body fat distributicn in type 2 diabetes. Diabetes Care 2000; 23: 1067–71.
   PubMed Web of Science ®Google Scholar
• Kawai T, Takei I, Oguma Y, Ohashi N, Tokui M, Oguchi S, et al. Effects of troglitazorr on fat distributicn in the treatment of male type 2 diabetes. Metabolism 1999; 48: 1102–7.
   PubMed Web of Science ®Google Scholar
• Kelly IE, Han TS, Walsh K, Lean ME. Effects of a thiazolidinediorr compound on body fat and fat distributicn of patients with type 2 diabetes [published erratum appears in Diabetes Care 1999 Mar;22(3):536]. Diabetes Care 1999; 22: 288–93.
   PubMed Web of Science ®Google Scholar
• Mori Y, Murakawa Y, Okada K, Horikoshi H, Yokoyama J, Tajima N, et al. Effect of troglitazorr on body fat distribution in type 2 diabetic patients. Diabetes Care 1999; 22: 908–12.
   PubMed Web of Science ®Google Scholar
• Gimble JM, Robinson CE, Wu X, Kelly KA, Rodriguez BR, Kliewer SA, et al. Peroxisome proliferator-activated receptor-gamma activation by thiazolidinediones induces adipogenesis in bone marrow stromal cells. Mol Pharmacol 1996; 50: 1087–94.
   PubMed Web of Science ®Google Scholar
• Tontonoz P, Nagy L, Alvarez JGA, Thomazy VA, Evans RM. PPAR gamma promotes monocyte/macrophage differ-entiation and uptake of oxidized LDL. Cell 1998; 93: 241–52.
   PubMed Web of Science ®Google Scholar
• Kato K, Satoh H, Endo Y, Yamada D, Midorikawa S, Sato W, et al. Thiazolidinediones down-regulate plasminogen activator inhibitor type 1 expression in human vascular endothelial cells: A possible role for PPARgamma in endothe-lial function. Biochem Biophys Res Commun 1999; 258: 431–5.
   PubMed Web of Science ®Google Scholar
• Saez E, Tontonoz P, Nelson MC, Alvarez JG, Ming UT, Baird SM, et al. Activators of the nuclear receptor PPAR-gamma enhance colon polyp formation. Nat Med 1998; 4: 1058–61.
   PubMed Web of Science ®Google Scholar
• Lefebvre AM, Chen I, Desreumaux P, Najib J, Fruchart JC, Geboes K, et al. Activaticn of the peroxisome proliferator-activated receptor gamma promotes the development of colon tumors in C57BL/6J- APCMin/+ mice. Nat Med 1998; 4: 1053–7.
   PubMed Web of Science ®Google Scholar
• Sarraf P, Mueller E, Jones D, King FJ, DeAngelo DJ, Partridge JB, et al. Differentiaticn and reversal of malignant changes in colon cancer through PPARgamma. Nat Med 1998; 4: 1046–52.
   PubMed Web of Science ®Google Scholar
• Zhu L, Gong B, Bisgaier CL, Aviram M, Newton RS. Induction of PPARgamma1 expression in human THP-1 monocytic leukemia by 9-cis-retinoic acid is associated with cellular growth suppression. Biochem Biophys Res Commun 1998; 251: 842–8.
   Google Scholar
• Imano E, Kanda T, Kawamori R, Kajimoto Y, Yamasaki Y. Pioglitazone-reduced insulin resistance in patient with Werner syndrome. Lancet 1997; 350: 1365.
   PubMed Web of Science ®Google Scholar
• Adler A, Turner RC. The diabetes prevention program. Diabetes Care 1999; 22: 543–5.
   PubMed Web of Science ®Google Scholar
• Elbrecht A, Chen Y, Adams A, Berger J, Griffin P, Klatt T, et al. L-764406 is a partial agonist of human peroxisome proliferator-activated receptor gamma. The role of Cys313 in ligand binding. J Biol Chem 1999; 274: 7913–22.
   PubMed Web of Science ®Google Scholar
• Mukherjee R, Hoener PA, Jow L, Bilakovics J, Klausing K, Mias DE, et al. A selective peroxisome proliferator-activated receptor-gamma (PPARgamma) modulator blocks adipocyte differentiaticn but stimulates glucose uptake in 3T3-L1 adipocytes. Mol Endocrinol 2000; 14: 1425–33.
   PubMed Web of Science ®Google Scholar
• Oberfield JL, Collins JL, Holmes CP, Goreham DM, Cooper JP, Cobb JE, et al. A peroxisome proliferator-activated receptor gamma ligand inhibits adipocyte differen-tiation. Proc Nat! Acad Sci USA 1999; 96: 6102–6.
   PubMed Web of Science ®Google Scholar
• Reginato MJ, Bailey ST, Krakow SL, Minami C, Ishii S, Tanaka H, et al. A potent antidiabetic thiazolidinedione with unique peroxisome proliferator-activated receptor gamma-activating properties. J Biol Chem 1998; 273: 32679–84.
   PubMed Web of Science ®Google Scholar