PAM-1616, a selective peroxisome proliferator-activated receptor γ modulator with preserved anti-diabetic efficacy and reduced adverse effects

European Journal of Pharmacology

Volumn 650, Issue 2-3, 2011, Pages 673-681

  Kim, Mi Kyung ^a   Chae, Yu Na ^a   Choi, Song Hyen ^a   Moon, Ho Sang ^a   Son, Moon Ho ^a   Bae, Myung Ho ^b   Choi, Hyun Ho ^b   Hur, Youn ^b   Kim, Eunkyung ^b   Park, Yoo Hoi ^b   Park, Chan Sun ^b   Kim, Jae Gyu ^b   Lim, Joong In ^a   Shin, Chang Yell ^a  

^a Dong A Research Center   (South Korea)

^b Yuhan Research Institute   (South Korea)

Author keywords

Fluid retention; Insulin resistance; PAM 1616; Peroxisome proliferator activated receptor gamma modulator; Serum glucocorticoid regulated kinase

Indexed keywords

3 ETHOXY 3 [4 [[3 METHYL 5 [4 (3 METHYLISOXAZOL 5 YL)PHENYL]THIOPHEN 2 YL]METHOXY]PHENYL]PROPANOIC ACID; GLUCOSE TRANSPORTER 4; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR BINDING PROTEIN; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; ROSIGLITAZONE; UNCLASSIFIED DRUG;

ADIPOCYTE; ANIMAL CELL; ANIMAL CELL CULTURE; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CELL STRAIN 3T3; CONTROLLED STUDY; DOSE RESPONSE; DRUG BINDING; DRUG EFFICACY; DRUG SAFETY; EPITHELIUM CELL; GENE EXPRESSION; HOMEOSTASIS; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; HYPERGLYCEMIA; IC 50; INSULIN RESISTANCE; KIDNEY EPITHELIUM; LIPID DIET; MALE; MOUSE; NONHUMAN; NUCLEOTIDE SEQUENCE; OBESITY; PRIORITY JOURNAL;

3T3-L1 CELLS; ADIPOCYTES; ANIMALS; CELLS, CULTURED; HUMANS; HYPERGLYCEMIA; HYPOGLYCEMIC AGENTS; INSULIN RESISTANCE; MALE; MICE; MICE, INBRED C57BL; PHENYLPROPIONATES; PPAR ALPHA; PPAR DELTA; PPAR GAMMA; THIAZOLIDINEDIONES; THIOPHENES; WATER-ELECTROLYTE BALANCE;

EID: 78651075521     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2010.10.044     Document Type: Article

References (43)

1. J.J. Acton III, R.M. Black, A.B. Jones, D.E. Moller, L. Colwell, T.W. Doebber, K.L. Macnaul, J. Berger, and H.B. Wood Benzoyl 2-methyl indoles as selective PPARgamma modulators Bioorg. Med. Chem. Lett. 15 2005 357 362
2. T. Albrektsen, K.S. Frederiksen, W.E. Holmes, E. Boel, K. Taylor, and J. Fleckner Novel genes regulated by the insulin sensitizer rosiglitazone during adipocyte differentiation Diabetes 51 2002 1042 1051
3. T. Allen, F. Zhang, S.A. Moodie, L.E. Clemens, A. Smith, F. Gregoire, A. Bell, G.E. Muscat, and T.A. Gustafson Halofenate is a selective peroxisome proliferator-activated receptor gamma modulator with antidiabetic activity Diabetes 55 2006 2523 2533
4. M. Bajaj, S. Suraamornkul, L.J. Hardies, L. Glass, N. Musi, and R.A. DeFronzo Effects of peroxisome proliferator-activated receptor (PPAR)-alpha and PPAR-gamma agonists on glucose and lipid metabolism in patients with type 2 diabetes mellitus Diabetologia 50 2007 1723 1731
5. J.P. Berger, A.E. Petro, K.L. Macnaul, L.J. Kelly, B.B. Zhang, K. Richards, A. Elbrecht, B.A. Johnson, G. Zhou, T.W. Doebber, C. Biswas, M. Parikh, N. Sharma, M.R. Tanen, G.M. Thompson, J. Ventre, A.D. Adams, R. Mosley, R.S. Surwit, and D.E. Moller Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator Mol. Endocrinol. 17 2003 662 676
6. J.P. Berger, T.E. Akiyama, and P.T. Meinke PPARs: therapeutic targets for metabolic disease Trends Pharmacol. Sci. 26 2005 244 251
7. L. Chen, B. Yang, J.A. McNulty, L.G. Clifton, J.G. Binz, A.M. Grimes, J.C. Strum, W.W. Harrington, Z. Chen, T.W. Balon, S.A. Stimpson, and K.K. Brown GI262570, a peroxisome proliferator-activated receptor gamma agonist, changes electrolytes and water reabsorption from the distal nephron in rats J. Pharmacol. Exp. Ther. 312 2005 718 725
8. B. Desvergne, and W. Wahli Peroxisome proliferator-activated receptors: nuclear control of metabolism Endocr. Rev. 20 1999 649 688
9. D. Dey, S. Medicherla, P. Neogi, M. Gowri, J. Cheng, C. Gross, S.D. Sharma, G.M. Reaven, and B. Nag A novel peroxisome proliferator-activated gamma (PPAR gamma) agonist, CLX-0921, has potent antihyperglycemic activity with low adipogenic potential Metabolism 52 2003 1012 1018
10. A. Elbrecht, Y. Chen, A. Adams, J. Berger, P. Griffin, T. Klatt, B. Zhang, J. Menke, G. Zhou, R.G. Smith, and D.E. Moller L-764406 is a partial agonist of human peroxisome proliferator-activated receptor gamma. The role of Cys313 in ligand binding J. Biol. Chem. 274 1999 7913 7922
11. Y. Guan, C. Hao, D.R. Cha, R. Rao, W. Lu, D.E. Kohan, M.A. Magnuson, R. Redha, Y. Zhang, and M.D. Breyer Thiazolidinediones expand body fluid volume through PPARgamma stimulation of ENaC-mediated renal salt absorption Nat. Med. 11 2005 861 866
12. M. Gurnell, D.B. Savage, V.K. Chatterjee, and S. O'Rahilly The metabolic syndrome: peroxisome proliferator-activated receptor gamma and its therapeutic modulation J. Clin. Endocrinol. Metab. 88 2003 2412 2421
13. L.S. Higgins, and C.S. Mantzoros The development of INT131 as a Selective PPARgamma modulator: approach to a safer insulin sensitizer PPAR Res. 2008 2008 936906
14. G. Hong, A. Lockhart, B. Davis, H. Rahmoune, S. Baker, L. Ye, P. Thompson, Y. Shou, K. O'Shaughnessy, P. Ronco, and J. Brown PPARgamma activation enhances cell surface ENaCalpha via up-regulation of SGK1 in human collecting duct cells FASEB J. 17 2003 1966 1968
15. Y.J. Hung, S.H. Lin, D. Pei, S.W. Kuo, C.H. Hsieh, C.T. He, C. Hsing Lee, S.C. Fan, and W.H. Sheu Rosiglitazone improves insulin sensitivity in nonobese subjects with impaired glucose tolerance: the role of adiponectin and C-reactive protein Metabolism 55 2006 439 444
16. K. Iwasaki, R. Zhang, M.A. Perhonen, J.H. Zuckerman, and B.D. Levine Reduced baroreflex control of heart period after bed rest is normalized by acute plasma volume restoration Am. J. Physiol. Regul. Integr. Comp. Physiol. 287 2004 R1256 R1262
17. K.R. Kim, J.H. Lee, S.J. Kim, S.D. Rhee, W.H. Jung, S.D. Yang, S.S. Kim, J.H. Ahn, and H.G. Cheon KR-62980: a novel peroxisome proliferator-activated receptor gamma agonist with weak adipogenic effects Biochem. Pharmacol. 72 2006 446 454
18. M.K. Kim, Y.N. Chae, M.H. Son, S.H. Kim, J.K. Kim, H.S. Moon, C.S. Park, M.H. Bae, E. Kim, T. Han, H.H. Choi, Y.A. Shin, B.N. Ahn, C.H. Lee, J.I. Lim, and C.Y. Shin PAR-5359, a well-balanced PPARalpha/gamma dual agonist, exhibits equivalent antidiabetic and hypolipidemic activities in vitro and in vivo Eur. J. Pharmacol. 595 2008 119 125
19. M.A. Knepper Proteomics and the kidney J. Am. Soc. Nephrol. 13 2002 1398 1408
20. C. Knouff, and J. Auwerx Peroxisome proliferator-activated receptor-gamma calls for activation in moderation: lessons from genetics and pharmacology Endocr. Rev. 25 2004 899 918
21. H.A. Koomans, and W.H. Boer Causes of edema in the intensive care unit Kidney Int. Suppl. 59 1997 S105 S110
22. P.J. Larsen, K. Lykkegaard, L.K. Larsen, J. Fleckner, P. Sauerberg, K. Wassermann, and E.M. Wulff Dissociation of antihyperglycaemic and adverse effects of partial perioxisome proliferator-activated receptor (PPAR-gamma) agonist balaglitazone Eur. J. Pharmacol. 596 2008 173 179
23. H.E. Lebovitz Differentiating members of the thiazolidinedione class: a focus on safety Diab. Metab. Res. Rev. 18 Suppl 2 2002 S23 S29
24. D.C. Merrill, and A.W. Cowley Jr. Chronic effects of vasopressin on fluid volume distribution in conscious dogs Am. J. Physiol. 252 1987 F26 F31
25. P. Misra, R. Chakrabarti, R.K. Vikramadithyan, G. Bolusu, S. Juluri, J. Hiriyan, C. Gershome, A. Rajjak, P. Kashireddy, S. Yu, S. Surapureddi, C. Qi, Y.J. Zhu, M.S. Rao, J.K. Reddy, and R. Ramanujam PAT5A: a partial agonist of peroxisome proliferator-activated receptor gamma is a potent antidiabetic thiazolidinedione yet weakly adipogenic J. Pharmacol. Exp. Ther. 306 2003 763 771
26. S. Mittra, G. Sangle, R. Tandon, S. Sharma, S. Roy, V. Khanna, A. Gupta, J. Sattigeri, L. Sharma, P. Priyadarsiny, S.K. Khattar, R.S. Bora, K.S. Saini, and V.S. Bansal Increase in weight induced by muraglitazar, a dual PPARalpha/gamma agonist, in db/db mice: adipogenesis/or oedema? Br. J. Pharmacol. 150 2007 480 487
27. H. Moon, M. Yoo, S. Kim, J. Lim, M. Son, M. Kim, C. Shin, J. Kim, S. Park, Y. Chae, H. Shim, S. Jeon, H. Kim, G. Wie, D. Kim, B. Lee, C. Park, B. Ahn, E. Kim, B. Bae, Y. Shin, Y. Hur, C. Lee, B. Kim, and W. Chong The Novel Phenylpropionic Acid Derivatives as Peroxisome Proliferator-activated Gamma Receptor Modulators, Method of the Same, and Pharmaceutical Composition Comprising the Same 2008 WO08/108602
28. R. Mukherjee, P.A. Hoener, L. Jow, J. Bilakovics, K. Klausing, D.E. Mais, A. Faulkner, G.E. Croston, and J.R. Paterniti Jr. A selective peroxisome proliferator-activated receptor-gamma (PPARgamma) modulator blocks adipocyte differentiation but stimulates glucose uptake in 3T3-L1 adipocytes Mol. Endocrinol. 14 2000 1425 1433
29. R.W. Nesto, D. Bell, R.O. Bonow, V. Fonseca, S.M. Grundy, E.S. Horton, M. Le Winter, D. Porte, C.F. Semenkovich, S. Smith, L.H. Young, and R. Kahn Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association and American Diabetes Association October 7, 2003 Circulation 108 2003 2941 2948
30. R.W. Nesto, D. Bell, R.O. Bonow, V. Fonseca, S.M. Grundy, E.S. Horton, M. Le Winter, D. Porte, C.F. Semenkovich, S. Smith, L.H. Young, and R. Kahn Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association and American Diabetes Association Diab. Care 27 2004 256 263
31. S.E. Nissen, K. Wolski, and E.J. Topol Effect of muraglitazar on death and major adverse cardiovascular events in patients with type 2 diabetes mellitus JAMA 294 2005 2581 2586
32. J.M. Olefsky Treatment of insulin resistance with peroxisome proliferator-activated receptor gamma agonists J. Clin. Invest. 106 2000 467 472
33. F. Picard, and J. Auwerx PPAR(gamma) and glucose homeostasis Annu. Rev. Nutr. 22 2002 167 197
34. S.M. Rangwala, and M.A. Lazar Peroxisome proliferator-activated receptor gamma in diabetes and metabolism Trends Pharmacol. Sci. 25 2004 331 336
35. M.J. Reginato, S.T. Bailey, S.L. Krakow, C. Minami, S. Ishii, H. Tanaka, and M.A. Lazar A potent antidiabetic thiazolidinedione with unique peroxisome proliferator-activated receptor gamma-activating properties J. Biol. Chem. 273 1998 32679 32684
36. R.C. Ribeiro, P.J. Kushner, and J.D. Baxter The nuclear hormone receptor gene superfamily Annu. Rev. Med. 46 1995 443 453
37. C.S. Rubin, A. Hirsch, C. Fung, and O.M. Rosen Development of hormone receptors and hormonal responsiveness in vitro. Insulin receptors and insulin sensitivity in the preadipocyte and adipocyte forms of 3T3-L1 cells J. Biol. Chem. 253 1978 7570 7578
38. S. Saad, D.J. Agapiou, X.M. Chen, V. Stevens, and C.A. Pollock The role of Sgk-1 in the upregulation of transport proteins by PPAR-{gamma} agonists in human proximal tubule cells Nephrol. Dial. Transplant. 24 2009 1130 1141
39. Y. Takahashi, M. Kushiro, K. Shinohara, and T. Ide Dietary conjugated linoleic acid reduces body fat mass and affects gene expression of proteins regulating energy metabolism in mice Comp. Biochem. Physiol. B Biochem. Mol. Biol. 133 2002 395 404
40. C.M. Tyree, and K. Klausing The mammalian two-hybrid assay for detection of coactivator-nuclear receptor interactions Meth. Mol. Med. 85 2003 175 183
41. J.M. Way, W.W. Harrington, K.K. Brown, W.K. Gottschalk, S.S. Sundseth, T.A. Mansfield, R.K. Ramachandran, T.M. Willson, and S.A. Kliewer Comprehensive messenger ribonucleic acid profiling reveals that peroxisome proliferator-activated receptor gamma activation has coordinate effects on gene expression in multiple insulin-sensitive tissues Endocrinology 142 2001 1269 1277
42. H. Zhang, A. Zhang, D.E. Kohan, R.D. Nelson, F.J. Gonzalez, and T. Yang Collecting duct-specific deletion of peroxisome proliferator-activated receptor gamma blocks thiazolidinedione-induced fluid retention Proc. Nat. Acad. Sci. U.S.A. 102 2005 9406 9411
43. F. Zhang, B.E. Lavan, and F.M. Gregoire Selective Modulators of PPAR-gamma Activity: Molecular Aspects Related to Obesity and Side-Effects PPAR Res. 2007 2007 32696