PPAR γ partial agonist, KR-62776, inhibits adipocyte differentiation via activation of ERK

Cellular and Molecular Life Sciences

Volumn 66, Issue 10, 2009, Pages 1766-1781

  Kim, J ^a   Han, D C ^a   Kim, J M ^a   Lee, S Y ^a   Kim, S J ^a   Woo, J R ^a   Lee, J W ^a   Jung, S K ^a   Yoon, K S ^a   Cheon, H G ^b   Kim, S S ^b   Hong, S H ^c   Kwon, B M ^a  

^a Korea Research Institute of Bioscience and Biotechnology (KRIBB)   (South Korea)

^b Korea Research Institute of Chemical Technology   (South Korea)

^c Kyungpook National University   (South Korea)

Author keywords

Adipocyte; ERK; Indenone; Lipolysis; Peroxisome proliferators activated receptor ; Rosiglitazone

Indexed keywords

KR 62776; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA AGONIST; ROSIGLITAZONE; UNCLASSIFIED DRUG;

ADIPOGENESIS; ANIMAL CELL; ARTICLE; CELL DIFFERENTIATION; CONTROLLED STUDY; DRUG BINDING; DRUG EFFECT; DRUG MECHANISM; DRUG STRUCTURE; MOUSE; NONHUMAN; NUCLEOTIDE SEQUENCE; OBESITY; PROADIPOCYTE; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; X RAY CRYSTALLOGRAPHY;

3T3-L1 CELLS; ADIPOCYTES; ANIMALS; CELL DIFFERENTIATION; CRYSTALLOGRAPHY, X-RAY; EXTRACELLULAR SIGNAL-REGULATED MAP KINASES; GENE EXPRESSION REGULATION; INDANS; MICE; MODELS, MOLECULAR; MOLECULAR STRUCTURE; OXIMES; PPAR GAMMA; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; PROTEOME; THIAZOLIDINEDIONES;

ANIMALIA;

EID: 67650688956     PISSN: 1420682X     EISSN: 15691632     Source Type: Journal    
DOI: 10.1007/s00018-009-9169-4     Document Type: Article

References (34)

1. Shih, D. Q. and Stoffel, M. (2002) Molecular etiologies of mody and other early-onset forms of diabetes. Current Diabetes Report 2,125-134.
2. MacDougald, O. A. and Lane, M. D. (1995) Transcriptional Regulation of Gene Expression During Adipocyte Differentiation. Ann. Rev. Biochem. 64, 345-373.
3. Ricote, M., Li, A. C., Willson, T. M., Kelly, C.J. and Glass, C. K. (1998) The peroxisome proliferator-activated receptor-gamma is a negative regulator of macrophage activation. Nature 391, 79-82.
4. Lehmann, J. M., Moore, L. B., Smith-Oliver, T. A., Wilkison, W. O., Wilkison and T. M., Kliewer, S. A. (1995) An Antidiabetic thiazolidinedione is a high, affinity ligand for peroxisome proliferator-activated receptor gamma. J. Biol. Chem. 270,12953-12956.
5. Saltiel, A. and Olefsky, J. M. (1996) Thiazolidinediones in the treatment of insulin resistance and type 2 diabetes. Diabetes; 45,1661-1669.
6. Olefsky, J. M. (2000) Treatment of insulin resistance with peroxisome proliferator-activated receptor y agonists. J. Clin. Invest. 106, 467-472.
7. Cavaghan, M. K., Ehrmann, D. A. and Polonsky, K. S. (2000) Interactions between insulin resistance and insulin secretion in the development of glucose intolerance. J. Clin. Invest. 106, 329-333.
8. Kletzien, R. F., Clarke, S. D. and Ulrich, R. G. (1992) Enhancement of adipocyte differentiation by an insulinsensitizing agent. Mol. Pharm. 41,393-398.
9. Ahn, J. H., Shin, M.S., Jung, S.H., Kim, J. A., Kim, H.M., Kim, S. H., Kang, S. K., Kim, K. R., Rhee, S. D, Park, S. D., Lee, J. M., Lee, J. H., Cheon, H. G. and Kim, S. S. (2007) Synthesis and structure-activity relationship of novel, indene N-oxide derivatives as potent peroxisome proliferator activated receptor y (PPARy) agonists. Bioorg. Med. Chem. Lett. 17, 5239-5244.
10. Kim, K. R., Lee, J. H., Kim, S. J., Rhee, S. D., Jung, W. H., Yang, S. D., Kim, S. S., Ahn, J. H. and Cheon, H. G. (2006) KR-62980: a novel peroxisome proliferator-activated receptor gamma agonist with, weak adipogenic effects. Biochem. Pharm. 72, 446-454.
11. Oberfield, J. L., Collins, J. L., Holmes, C. P., Goreham, D. M., Cooper, J. P., Cobb, J. E., Lenhard, J. M., Hull-Ryde, E. A., Mohr, C. P., Blanchard, S. G., Parks, D. J., Moore, L, B., Lehmann, J. M., Plunket, K., Miller, A. B., Milburn, M. V., Kliewer, S. A. and Willson, T M. (1999) A peroxisome proliferator-activated receptor gamma ligand inhibits adipocyte differentiation. Proc. Natl. Acad. Sci. USA 96,6102-6106.
12. Wright, H. M., Clish, C. B., Mikami, T., Hauser, S., Yanagi, K., Hiramatsu, R., Serhan, C. N. and Spiegelman, B. M. (2000) A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation. J. Biol. Chem. 275, 1873-1877.
13. Mukherjee, R., Hoener, P. A., Jow, L., Bilakovics, J., Klausing, K., Mais, D. E., Faulkner, A., Croston, G. E. and Paterniti, J. R. (2000) A Selective Peroxisome Proliferator-Activated Receptor-γ (PPARγ) Modulator Blocks Adipocyte Differentiation but Stimulates Glucose Uptake in 3T3-L1 Adipocytes. Mol. Endo. 14, 1425-1433.
14. Hu, E., Kim, J. B., Sarraf, P. and Spiegelman, B. M. (1996) Inhibition of Adipogenesis Through MAP Kinase-Mediated Phosphorylation of PPARγ. Science 274, 2100-2103.
15. Burgermeister, E., Chuderland, D., Hanoch, T., Meyer, M., Liscovitch, M. and Seger, R. (2007) Interaction with MEK causes nuclear export and downregulation of peroxisome proliferator-activated receptor gamma. Mol. Cell. Biol. 27, 803-817.
16. Uppenberg, J.,Svensson, C. Jaki, M., Bertilsson, G. Jendeberg, L. and Berkenstam, A. (1998) Crystal, structure of the ligand binding domain of the human nuclear receptor PPARgamma. J. Biol. Chem. 273, 31108-31112.
17. Leslie, A. G. (1999) Integration of macromolecular diffraction data. Acta Crystaliogr. D Biol. Crystaliogr. 55,1696-702.
18. Jones, T. A., Zou, J-. Y., Cowan, S. W. and Kjeldgaard, M. (1991) Improved methods for building protein models in electron density maps and the location of errors in these models. Acta Crystaliogr. A 47, 110-119.
19. Green, H. and Kehinde, O. (1975) An established preadipose cell line and its differentiation in culture. II. Factors affecting the adipose conversion. Cell. 5, 19-27.
20. Görg, A., Obermaier, C., Boguth, G., Harder, A., Scheibe, B. R., Wildgruber, R. W. and Weiss, W. (2000) The current state of two-dimensional electrophoresis with immobilized pH gradients. Electrophoresis 21, 1037-1053.
21. Jensen, O. N., Wilm, M., Shevchenko, A. and Mann, M. (1999) Sample preparation methods for mass spectrometric peptide mapping directly from 2-DE gels. Methods Mol. Biol. 112, 513-530.
22. Meunier, C., Bordereaux, D., Porteu, F., Gisselbrecht, S., Chretien, S. and Courtois, G. (2002) Cloning and characterization of a family of proteins associated with Mpl. J. Biol. Chem. 277, 9139-9147.
23. Wilson-Fritch, L., Burkart, A., Bell, G., Mendelson, K., Leszyk, J., Nicoloro, S., Czech, M. and Corvera, S. (2003) Mitochondrial biogenesis and remodeling during adipogenesis and in response to the insulin sensitizer rosiglitazone. Mol. Cell. Biol. 23,1085-1094.
24. Kao, A. W., Noda, Y., Johnson, J. H., Pessin, J. E. and Saltiel, A. R. (1999) Aldolase mediates the association of F-actin with the insulin-responsive glucose transporter GLUT4. J. Biol. Chem, 274,17742-17747.
25. Wolfsgruber, W., Feil, S., Brummer, S., Kuppinger, O., Hofmann and F., Feil, R. (2003) A proatherogenic role for cGMP-dependent protein kinase in vascular smooth muscle cells. Proc. Natl. Acad. Sci. USA 100, 13519-13524.
26. Spiegelman, B. M. and Flier, J. S. (1996) Adipogenesis and obesity: rounding out the big picture. Cell 87,377-389.
27. Camp, H. S. and Tafuri, S. R. (1997) Regulation of peroxisome proliferator-activated receptor gamma activity by mitogenactivated protein kinase. J. Biol. Chem. 272,10811-10816.
28. Diradourian, C., Girard, J. and Pegorier, J. P. (2005) Phosphorylation of PPARs: from molecular characterization to physiological relevance. Biochimie 87,33-38.
29. McFarland-Mancini M., Hugo E., Loftus J. and Ben-Jonathan H (2006) Induction of prolactin expression and release in human preadipocytes by cAMP activating ligands. Biochem. Biophys. Res. Comm. 344, 9-16.
30. Czech, M. P. and Corvera, S. (1999) Signaling mechanisms that regulate glucose transport. J. Biol. Chem. 274,1865-1868.
31. 31.Burgermeister, E. and Seger, R. (2007) MAPK- Kinases as Nucleo-Cytoplasmic Shuttles for PPARy. Cell Cycle 6,15391548.
32. Park, J. Y., Bae, M. A., Cheon, H. K., Kim, S. S., Hong, J. M., Kim, T. H., Choi, J. Y., Kim, S. H., Lim, J., Choi, C. H., Shin, H. I., Kim, S. Y. and Park, E. K. (2008) A novel PPARc agonist, KR62776, suppresses RANKL-induced osteoclast differentiation and activity by inhibiting MAP kinase pathways. Biochem. Biophys. Res. Comm. 378, 645-649.
33. Prusty, D., Park, B. H., Davis, K. E. and Farmer, S. R. (2002) Activation of MEK/ERK signaling promotes adipogenesis by enhancing peroxisome proliferator-activated receptor gamma and C/EBPalpha gene expression during the differentiation of 3T3-L1 preadipocytes. J. Biol. Chem. 277, 46226-4632.
34. Nanbu-Wakao, R., Fujitani, Y., Masuho, Y., Muramatu, M. and Wakao, H. (2000) Prolactin enhances CCAAT enhancer-binding protein-beta and peroxisome proliferator-activated receptor gamma messenger RNA expression and stimulates adipogenic conversion of NIH-3T3 cells. Mol. Endocrinol. 14, 307316.