The effect of PPARα, PPARδ, PPARγ, and PPARpan agonists on body weight, body mass, and serum lipid profiles in diet-induced obese AKR/J Mice

PPAR Research

Volumn , Issue , 2007, Pages

  Harrington, W Wallace ^a   Britt, Christy S ^a   Wilson, Joan G ^a   Milliken, Naphtali O ^a   Binz, Jane G ^a   Lobe, David C ^a   Oliver, William R ^a   Lewis, Michael C ^a   Ignar, Diane M ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [1 CARBOXY 2 [4 [2 (5 METHYL 2 PHENYL 4 OXAZOLYL)ETHOXY]PHENYL]ETHYLAMINO]BENZOIC ACID METHYL ESTER; 2 [4 [2 [3 (2,4 DIFLUOROPHENYL) 1 HEPTYLUREIDO]ETHYL]PHENYLTHIO] 2 METHYLPROPIONIC ACID; FAT; FATTY ACID; GW 0742; GW 4148; GW 9135; INSULIN; LIPID; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; RIMONABANT; UNCLASSIFIED DRUG;

AKR MOUSE; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BODY COMPOSITION; BODY MASS; BODY WEIGHT; CHEMISTRY; DIET; DOSE RESPONSE; DRUG ACTIVATION; DRUG EFFECT; FATTY ACID OXIDATION; FOOD INTAKE; INSULIN SENSITIVITY; LIPID BLOOD LEVEL; MALE; MONOTHERAPY; MOUSE; NONHUMAN; OBESITY; WEIGHT GAIN; WEIGHT REDUCTION;

EID: 42749108867     PISSN: 16874757     EISSN: 16874765     Source Type: Journal    
DOI: 10.1155/2007/97125     Document Type: Article

References (76)

1. WHO Obesity: preventing and managing the global epidemic: report of WHO consultation. WHO Consultation on Obesity Geneva, Switzerland 884 1999
2. S. Nammi nammi@rediffmail.com S. Koka k_saisudha@yahoo.com K. M. Chinnala chinnala_km@yahoo.com K. M. Boini krishnamurthyboini@yahoo.com Obesity: an overview on its current perspectives and treatment options. Nutrition Journal 3 2004 3
3. A. von Eckardstein G. Assmann Prevention of coronary heart disease by raising high-density lipoprotein cholesterol? Current Opinion in Lipidology 11 6 2000 627 637
4. P. T. James N. Rigby nrigby@iotf.org R. Leach The obesity epidemic, metabolic syndrome and future prevention strategies. European Journal of Cardiovascular Prevention and Rehabilitation 11 1 2004 3 8
5. E. N. Liberopoulos D. P. Mikhailidis M. S. Elisaf egepi@cc.uoi.gr Diagnosis and management of the metabolic syndrome in obesity. Obesity Reviews 6 4 2005 283 296
6. J. Korner jk181@columbia.edu L. J. Aronne Pharmacological approaches to weight reduction: therapeutic targets. Journal of Clinical Endocrinology and Metabolism 89 6 2004 2616 2621
7. D. Cota S. C. Woods steve.woods@psychiatry.uc.edu The role of the endocannabinoid system in the regulation of energy homeostasis. Current Opinion in Endocrinology and Diabetes 12 5 2005 338 351
8. R. M. Evans evans@salk.edu G. D. Barish Y.-X. Wang PPARs and the complex journey to obesity. Nature Medicine 10 4 2004 355 361
9. T. M. Willson tmw20653@glaxowellcome.com P. J. Brown D. D. Sternbach B. R. Henke The PPARs: from orphan receptors to drug discovery. Journal of Medicinal Chemistry 43 4 2000 527 550
10. H. E. Xu ex11957@glaxowellcome.com M. H. Lambert V. G. Montana Molecular recognition of fatty acids by peroxisome proliferator-activated receptors. Molecular Cell 3 3 1999 397 403
11. M. Guerre-Millo P. Gervois E. Raspé Peroxisome proliferator-activated receptor α activators improve insulin sensitivity and reduce adiposity. Journal of Biological Chemistry 275 22 2000 16638 16642
12. E. Erol L. S. Kumar G. W. Cline G. I. Shulman D. P. Kelly B. Binas Liver fatty acid binding protein is required for high rates of hepatic fatty acid oxidation but not for the action of PPARα in fasting mice. The FASEB Journal 18 2 2004 347 349
13. O. Braissant F. Foufelle C. Scotto M. Dauca W. Wahli Differential expression of peroxisome proliferator-activated receptors (PPARs): tissue distribution of PPAR-α, -β, and -γ in the adult rat. Endocrinology 137 1 1996 354 366
14. W. R. Oliver J. L. Shenk M. R. Snaith A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport. Proceedings of the National Academy of Sciences of the United States of America 98 9 2001 5306 5311
15. Y.-X. Wang C.-H. Lee S. Tiep Peroxisome-proliferator-activated receptor δ activates fat metabolism to prevent obesity. Cell 113 2 2003 159 170
16. Y. X. Wang C. L. Zhang R. T. Yu Regulation of muscle fiber type and running endurance by PPARδ PLoS Biology 2 10 2004 e294
17. B. M. Spiegelman bruce_spiegelman@dfci.harvard.edu PPAR-γ: adipogenic regulator and thiazolidinedione receptor. Diabetes 47 4 1998 507 514
18. L. Fajas J.-C. Fruchart J. Auwerx Johan.Auwerx@pasteur-lille.fr Transcriptional control of adipogenesis. Current Opinion in Cell Biology 10 2 1998 165 173
19. M. Lehrke M. A. Lazar lazar@mail.med.upenn.edu The many faces of PPARγ Cell 123 6 2005 993 999
20. J. E. Cecil jc100@st-andrews.ac.uk P. Watt C. N. Palmer M. Hetherington Energy balance and food intake: the role of PPARγ gene polymorphisms. Physiology and Behavior 88 3 2006 227 233
21. S. Mudaliar A. R. Chang R. R. Henry Thiazolidinediones, peripheral edema, and type 2 diabetes: incidence, pathophysiology, and clinical implications. Endocrine Practice 9 5 2003 406 416
22. Y. Guan C. Hao D. R. Cha Thiazolidinediones expand body fluid volume through PPARγ stimulation of ENaC-mediated renal salt absorption. Nature Medicine 11 8 2005 861 866
23. M. C. Lewis J. G. Wilson D. M. Ignar W. R. Oliver The effects of PPARα, δ and PPARpan agonist on diet-induced obesity in fat-fed AKR mice. Diabetes 53, supplement 2 2004 A134
24. B. Pourcet J.-C. Fruchart B. Staels Bart.Staels@pasteur-lille.fr C. Glineur Corine.Glineur@pasteur-lille.fr Selective PPAR modulators, dual and pan PPAR agonists: multimodal drugs for the treatment of type 2 diabetes and atherosclerosis. Expert Opinion on Emerging Drugs 11 3 2006 379 401
25. U. Ramachandran umaram54@yahoo.com R. Kumar A. Mittal Fine tuning of PPAR ligands for type 2 diabetes and metabolic syndrome. Mini-Reviews in Medicinal Chemistry 6 5 2006 563 573
26. P. J. Brown pjb5890@glaxowellcome.com D. A. Winegar K. D. Plunket A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARα agonist with potent lipid-lowering activity. Journal of Medicinal Chemistry 42 19 1999 3785 3788
27. B. Yang K. K. Brown L. Chen Serum adiponectin as a biomarker for in vivo PPARγ activation and PPARγ agonist-induced efficacy on insulin sensitization/lipid lowering in rats. BMC Pharmacology 4 1 2004 23
28. B. R. Henke brh14990@glaxowellcome.com S. G. Blanchard M. F. Brackeen N-(2-benzoylphenyl)-L-tyrosine PPARγ agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. Journal of Medicinal Chemistry 41 25 1998 5020 5036
29. J. M. Lehmann L. B. Moore T. A. Smith-Oliver W. O. Wilkison T. M. Willson S. A. Kliewer An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor γ (PPARγ). Journal of Biological Chemistry 270 22 1995 12953 12956
30. J. S. Nichols D. J. Parks T. G. Consler S. G. Blanchard Development of a scintillation proximity assay for peroxisome proliferator-activated receptor γ ligand binding domain. Analytical Biochemistry 257 2 1998 112 119
31. G. L. Dohm R. L. Huston E. W. Askew P. C. Weiser Effects of exercise on activity of heart and muscle mitochondria. The American Journal of Physiology 223 4 1972 783 787
32. H. R. Scholte Y. Yu J. D. Ross I. I. Oosterkamp A. M. C. Boonman H. F. M. Busch Rapid isolation of muscle and heart mitochondria, the lability of oxidative phosphorylation and attempts to stabilize the process in vitro by taurine, carnitine and other compounds. Molecular and Cellular Biochemistry 174 1-2 1997 61 66
33. D. M. Muoio P. S. MacLean D. B. Lang Fatty acid homeostasis and induction of lipid regulatory genes in skeletal muscles of peroxisome proliferator-activated receptor (PPAR) α knock-out mice: evidence for compensatory regulation by PPARδ Journal of Biological Chemistry 277 29 2002 26089 26097
34. P. J. Brown pjb5890@glaxowellcome.com T. A. Smith-Oliver P. S. Charifson Identification of peroxisome proliferator-activated receptor ligands from a biased chemical library. Chemistry and Biology 4 12 1997 909 918
35. D. C. Dey R. P. Bronson J. Dahl J. P. Carroll T. L. Benjamin Accelerated development of polyoma tumors and embryonic lethality: different effects of p53 loss on related mouse backgrounds. Cell Growth & Differentiation 11 5 2000 231 237
36. M. L. Sznaidman C. D. Haffner P. R. Maloney Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) - synthesis and biological activity. Bioorganic and Medicinal Chemistry Letters 13 9 2003 1517 1521
37. D. B. West C. N. Boozer D. L. Moody R. L. Atkinson Dietary obesity in nine inbred mouse strains. American Journal of Physiology 262 6, part 2 1992 R1025 R1032
38. B. K. Smith D. B. West D. A. York Carbohydrate versus fat intake: differing patterns of macronutrient selection in two inbred mouse strains. The American Journal of Physiology 272 1, part 2 1997 R357 R362
39. V. Prpic P. M. Watson I. C. Frampton M. A. Sabol G. E. Jezek T. W. Gettys Adaptive changes in adipocyte gene expression differ in AKR/J and SWR/J mice during diet-induced obesity. Journal of Nutrition 132 11 2002 3325 3332
40. B. Künnecke basil.kuennecke@roche.com P. Verry A. Bénardeau M. von Kienlin Quantitative body composition analysis in awake mice and rats by magnetic resonance relaxometry. Obesity Research 12 10 2004 1604 1615
41. E. E. Jobst jobste@pacificu.edu P. J. Enriori P. Sinnayah M. A. Cowley Hypothalamic regulatory pathways and potential obesity treatment targets. Endocrine 29 1 2006 33 48
42. P. Escher W. Wahli walter.wahli@iba.unil.ch Peroxisome proliferator-activated receptors: insight into multiple cellular functions. Mutation Research 448 2 2000 121 138
43. D. E. Moller david_moller@merck.com J. P. Berger Role of PPARs in the regulation of obesity-related insulin sensitivity and inflammation. International Journal of Obesity 27, supplement 3 2003 S17 S21
44. Y. Iwamoto K. Kosaka T. Kuzuya Y. Akanuma Y. Shigeta T. Kaneko Effects of troglitazone: a new hypoglycemic agent in patients with NIDDM poorly controlled by diet therapy. Diabetes Care 19 2 1996 151 156
45. M. Narce J.-P. Poisson jppoiss@u-buorgogne.fr Novel PPARγ-dependent and independent effects for thiazolidinediones. Current Opinion in Lipidology 14 6 2003 651 652
46. R. Chakrabarti ranjanchakrabarti@drreddys.com R. K. Vikramadithyan P. Misra Ragaglitazar: a novel PPARα & PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. British Journal of Pharmacology 140 3 2003 527 537
47. F. Törüner fusunbalostoruner@yahoo.com E. Akbay N. Çakir Effects of PPARγ and PPARα agonists on serum leptin levels in diet-induced obese rats. Hormone and Metabolic Research 36 4 2004 226 230
48. M. Rossmeisl J. S. Rim R. A. Koza L. P. Kozak kozaklp@pbrc.edu Variation in type 2 diabetes - related traits in mouse strains susceptible to diet-induced obesity. Diabetes 52 8 2003 1958 1966
49. L. C. Pickavance lucyp@liverpool.ac.uk C. L. Brand K. Wassermann J. P. H. Wilding The dual PPARα/γ agonist, ragaglitazar, improves insulin sensitivity and metabolic profile equally with pioglitazone in diabetic and dietary obese ZDF rats. British Journal of Pharmacology 144 3 2005 308 316
50. E. H. Koh M.-S. Kim J.-Y. Park Peroxisome proliferator-activated receptor (PPAR)-α activation prevents diabetes in OLETF rats: comparison with PPAR-γ activation. Diabetes 52 9 2003 2331 2337
51. M. K. Gee L. Zhang S. E. Rankin J. N. Collins R. F. Kauffman J. D. Wagner Rosiglitazone treatment improves insulin regulation and dyslipidemia in type 2 diabetic cynomolgus monkeys. Metabolism 53 9 2004 1121 1125
52. I. W. Campbell jackie.wallace@faht.scot.nhs.uk The clinical significance of PPAR γ agonism. Current Molecular Medicine 5 3 2005 349 363
53. C. G. Gegick gegick@mindspring.com M. D. Altheimer Thiazolidinediones: comparison of long-term effects on glycemic control and cardiovascular risk factors. Current Medical Research and Opinion 20 6 2004 919 930
54. M. W. Stolar mstolar@nwinternist.com R. J. Chilton Type 2 diabetes, cardiovascular risk, and the link to insulin resistance. Clinical Therapeutics 25, supplement 2 2003 B4 B31
55. H. Duez J.-C. Fruchart B. Staels PPARs in inflammation, atherosclerosis and thrombosis. Journal of Cardiovascular Risk 8 4 2001 187 194
56. J. M. Way W. W. Harrington K. K. Brown Comprehensive messenger ribonucleic acid profiling reveals that peroxisome proliferator-activated receptor γ activation has coordinate effects on gene expression in multiple insulin-sensitive tissues. Endocrinology 142 3 2001 1269 1277
57. S. Hummasti B. A. Laffitte M. A. Watson Liver X receptors are regulators of adipocyte gene expression but not differentiation: identification of apoD as a direct target. Journal of Lipid Research 45 4 2004 616 625
58. G. Martin K. Schoonjans B. Staels J. Auwerx Johan.Auwerx@pasteur-lille.fr PPARγ activators improve glucose homeostasis by stimulating fatty acid uptake in the adipocytes. Atherosclerosis 137, supplement 1 1998 S75 S80
59. V. Bocher I. Pineda-Torra J.-C. Fruchart B. Staels PPARS: transcription factors controlling lipid and lipoprotein metabolism. Annals of the New York Academy of Sciences 967 2002 7 18
60. S. Rocchi J. Auwerx auwerx@igbmc.u-strasbg.fr Peroxisome proliferator-activated receptor-γ: a versatile metabolic regulator. Annals of Medicine 31 5 1999 342 351
61. F. Picard J. Auwerx PPARγ and glucose homeostasis. Annual Review of Nutrition 22 2002 167 197
62. F. Zhang B. Lavan F. M. Gregoire fmgregoire@metabolex.com Peroxisome proliferator-activated receptors as attractive antiobesity targets. Drug News and Perspectives 17 10 2004 661 669
63. A. Fredenrich fredenrich.a@chu-nice.fr P. A. Grimaldi PPAR δ: an uncompletely known nuclear receptor. Diabetes and Metabolism 31 1 2005 23 27
64. S. Luquet J. Lopez-Soriano D. Holst Roles of peroxisome proliferator-activated receptor δ (PPARδ) in the control of fatty acid catabolism. A new target for the treatment of metabolic syndrome. Biochimie 86 11 2004 833 837
65. H. D. Shin B. L. Park L. H. Kim Genetic polymorphisms in peroxisome proliferator-activated receptor δ associated with obesity. Diabetes 53 3 2004 847 851
66. M. Muurling R. P. Mensink H. Pijl J. A. Romijn L. M. Havekes P. J. Voshol Rosiglitazone improves muscle insulin sensitivity, irrespective of increased triglyceride content, in ob/ob mice. Metabolism 52 8 2003 1078 1083
67. M. D. Leibowitz mleibowitz@ligand.com C. Fiévet N. Hennuyer Activation of PPARδ alters lipid metabolism in db/db mice. FEBS Letters 473 3 2000 333 336
68. C.-H. Lee P. Olson A. Hevener PPARδ regulates glucose metabolism and insulin sensitivity. Proceedings of the National Academy of Sciences of the United States of America 103 9 2006 3444 3449
69. Y. Fukui S.-I. Masui S. Osada K. Umesono K. Motojima motojima@phar.toho- u.ac.jp A new thiazolidinedione, NC-2100, which is a weak PPAR-γ activator, exhibits potent antidiabetic effects and induces uncoupling protein 1 in white adipose tissue of KKAy obese mice. Diabetes 49 5 2000 759 767
70. N. L. Bodkin nbodkin678@aol.com J. Pill K. Meyer B. C. Hansen The effects of K-111, a new insulin-sensitizer, on metabolic syndrome in obese prediabetic rhesus monkeys. Hormone and Metabolic Research 35 10 2003 617 624
71. E. H. Koh M.-S. Kim J.-Y. Park Peroxisome proliferator-activated receptor (PPAR)-α activation prevents diabetes in OLETF rats: comparison with PPAR-γ activation. Diabetes 52 9 2003 2331 2337
72. P. J. Larsen pjl@rheoscience.com P. B. Jensen R. V. Sørensen Differential influences of peroxisome proliferator-activated receptors γ and -α on food intake and energy homeostasis. Diabetes 52 9 2003 2249 2259
73. J. C. Corton ccorton@msn.com U. Apte S. P. Anderson Mimetics of caloric restriction include agonists of lipid-activated nuclear receptors. Journal of Biological Chemistry 279 44 2004 46204 46212
74. P. Ferré pferre@bhdc.jussieu.fr The biology of peroxisome proliferator-activated receptors: relationship with lipid metabolism and insulin sensitivity. Diabetes 53, supplemnet 1 2004 S43 S50
75. V. Navarro A. Fernández-Quintela I. Churruca M. P. Portillo mariapuy.portillo@ehu.es The body fat-lowering effect conjugated linoleic acid: a comparison between animal and human studies. Journal of Physiology and Biochemistry 62 2 2006 137 147
76. F. Djouadi J. M. Brandt C. J. Weinheimer T. C. Leone F. J. Gonzalez D. P. Kelly dkelly@imgate.wustl.edu The role of the peroxisome proliferator-activated receptor α (PPARα) in the control of cardiac lipid metabolism. Prostaglandins Leukotrienes and Essential Fatty Acids 60 5-6 1999 339 343