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Endocrinology, Vol 137, 4189-4195, Copyright © 1996 by Endocrine Society

ARTICLES

Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-gamma: binding and activation correlate with antidiabetic actions in db/db mice

J Berger, P Bailey, C Biswas, CA Cullinan, TW Doebber, NS Hayes, R Saperstein, RG Smith and MD Leibowitz
Department of Molecular Endocrinology, Merck Research Laboratories, Rahway, New Jersey 07065, USA. Joel_Berger@Merck.com

The thiazolidinediones are novel insulin sensitizers that serve as orally active antidiabetic agents, in rodents, nonhuman primates, and man. We have examined the effects of 4-week oral administration of three thiazolidinediones (AD-5075, BRL 49653, and CS-045) on plasma glucose and triglyceride concentrations in obese hyperglycemic db/db mice. All three agents lower plasma glucose and triglyceride concentrations. Normal levels of glucose are achieved after treatment with AD-5075 (> 1.7 mg/kg) or BRL 49653 (> or = 30 mg/kg), whereas CS- 045 (100 or 300 mg/kg) produces only modest reductions in either parameter. Although the thiazolidinediones have demonstrated insulin- sensitizing activities both in vivo and in vitro, their primary molecular target has been unclear. We have compared the in vivo antidiabetic actions described above with the in vitro activities on peroxisomal proliferator-activated receptor-gamma (PPAR gamma). Hamster PPAR gamma 1 was transiently expressed in COS-1 cells to study the binding of [3H]AD-5075. The concentrations of compounds needed to displace radiolabeled AD-5075 from PPAR gamma correlate with their in vivo potency; the Ki values for displacement by cold AD-5075, BRL 49653, and CS-045 are 22, 68, and 1600 nM, respectively. To examine activation of the receptor, it was transiently cotransfected into COS-1 cells with a reporter plasmid containing two copies of a peroxisome proliferator response element. The EC50 values for activation are 2, 6, and 140 nM for AD-5075, BRL 49653, and CS-045, respectively. We have also analyzed limited proteolytic digests of in vitro translated hamster PPAR gamma. The thiazolidinediones produce a conformational change in PPAR gamma analogous to those produced by agonists of other nuclear hormone receptors. In the presence of saturating concentrations of either AD-5075 or BRL 49653, a receptor fragment of 27 kDa is protected from proteolysis by trypsin. These data support the conclusion that the antidiabetic actions of the thiazolidinediones are directly mediated through binding to PPAR gamma and the resulting active conformation of the receptor. Therefore, binding and transactivation assays using PPAR gamma should serve to identify other novel therapeutic agents with potential antidiabetic activities.


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Expression of peroxisomal proliferator-activated receptors and retinoid X receptors in the kidney
Am J Physiol Renal Physiol, December 1, 1999; 277(6): F966 - F973.
[Abstract] [Full Text] [PDF]

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 J. Immunol.Home page
S. Vaidya, E. P. Somers, S. D. Wright, P. A. Detmers, and V. S. Bansal
15-Deoxy-{Delta}12,1412,14-prostaglandin J2 Inhibits the {beta}2 Integrin-Dependent Oxidative Burst: Involvement of a Mechanism Distinct from Peroxisome Proliferator-Activated Receptor {gamma} Ligation
J. Immunol., December 1, 1999; 163(11): 6187 - 6192.
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 Am. J. Clin. Nutr.Home page
S. D Clarke, P. Thuillier, R. A Baillie, and X. Sha
Peroxisome proliferator-activated receptors: a family of lipid-activated transcription factors
Am. J. Clinical Nutrition, October 1, 1999; 70(4): 566 - 571.
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 Endocr. Rev.Home page
B. Desvergne and W. Wahli
Peroxisome Proliferator-Activated Receptors: Nuclear Control of Metabolism
Endocr. Rev., October 1, 1999; 20(5): 649 - 688.
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 Toxicol PatholHome page
M.A. Breider, A.W. Gough, J.R. Haskins, G. Sobocinski, and F.A. De La Iglesia
Troglitazone-Induced Heart and Adipose Tissue Cell Proliferation in Mice
Toxicol Pathol, September 1, 1999; 27(5): 545 - 552.
[Abstract] [PDF]

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 Mol. Cell. Biol.Home page
L. Fajas, K. Schoonjans, L. Gelman, J. B. Kim, J. Najib, G. Martin, J.-C. Fruchart, M. Briggs, B. M. Spiegelman, and J. Auwerx
Regulation of Peroxisome Proliferator-Activated Receptor gamma Expression by Adipocyte Differentiation and Determination Factor 1/Sterol Regulatory Element Binding Protein 1: Implications for Adipocyte Differentiation and Metabolism
Mol. Cell. Biol., August 1, 1999; 19(8): 5495 - 5503.
[Abstract] [Full Text] [PDF]

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 Mol. Endocrinol.Home page
F. F. Wiebel, K. R. Steffensen, E. Treuter, D. Feltkamp, and J.-A. Gustafsson
Ligand-Independent Coregulator Recruitment by the Triply Activatable OR1/Retinoid X Receptor-{alpha} Nuclear Receptor Heterodimer
Mol. Endocrinol., July 1, 1999; 13(7): 1105 - 1118.
[Abstract] [Full Text]

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 J. Biol. Chem.Home page
A. Elbrecht, Y. Chen, A. Adams, J. Berger, P. Griffin, T. Klatt, B. Zhang, J. Menke, G. Zhou, R. G. Smith, 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., March 19, 1999; 274(12): 7913 - 7922.
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 J. Biol. Chem.Home page
J. Berger, M. D. Leibowitz, T. W. Doebber, A. Elbrecht, B. Zhang, G. Zhou, C. Biswas, C. A. Cullinan, N. S. Hayes, Y. Li, et al.
Novel Peroxisome Proliferator-activated Receptor (PPAR) gamma  and PPARdelta Ligands Produce Distinct Biological Effects
J. Biol. Chem., March 5, 1999; 274(10): 6718 - 6725.
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 J. Biol. Chem.Home page
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., December 4, 1998; 273(49): 32679 - 32684.
[Abstract] [Full Text] [PDF]

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 J. Lipid Res.Home page
P. Thuillier, R. Baillie, X. Sha, and S. D. Clarke
Cytosolic and nuclear distribution of PPAR{gamma}2 in differentiating 3T3-L1 preadipocytes
J. Lipid Res., December 1, 1998; 39(12): 2329 - 2338.
[Abstract] [Full Text]

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 EndocrinologyHome page
L. J. Kelly, P. P. Vicario, G. M. Thompson, M. R. Candelore, T. W. Doebber, J. Ventre, M. S. Wu, R. Meurer, M. J. Forrest, M. W. Conner, et al.
Peroxisome Proliferator-Activated Receptors {gamma} and {alpha} Mediate in Vivo Regulation of Uncoupling Protein (UCP-1, UCP-2, UCP-3) Gene Expression
Endocrinology, December 1, 1998; 139(12): 4920 - 4927.
[Abstract] [Full Text] [PDF]

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 EndocrinologyHome page
J. R. Zierath, J. W. Ryder, T. Doebber, J. Woods, M. Wu, J. Ventre, Z. Li, C. McCrary, J. Berger, B. Zhang, et al.
Role of Skeletal Muscle in Thiazolidinedione Insulin Sensitizer (PPAR{gamma} Agonist) Action
Endocrinology, December 1, 1998; 139(12): 5034 - 5041.
[Abstract] [Full Text] [PDF]

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 EndocrinologyHome page
L. S. Liu, H. Tanaka, S. Ishii, and J. Eckel
The New Antidiabetic Drug MCC-555 Acutely Sensitizes Insulin Signaling in Isolated Cardiomyocytes
Endocrinology, November 1, 1998; 139(11): 4531 - 4539.
[Abstract] [Full Text] [PDF]

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 Mol. Endocrinol.Home page
G. Zhou, R. Cummings, Y. Li, S. Mitra, H. A. Wilkinson, A. Elbrecht, J. D. Hermes, J. M. Schaeffer, R. G. Smith, and D. E. Moller
Nuclear Receptors Have Distinct Affinities for Coactivators: Characterization by Fluorescence Resonance Energy Transfer
Mol. Endocrinol., October 1, 1998; 12(10): 1594 - 1604.
[Abstract] [Full Text]

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 Mol. Pharmacol.Home page
T. Barkhem, B. Carlsson, Y. Nilsson, E. Enmark, J.-A. Gustafsson, and S. Nilsson
Differential Response of Estrogen Receptor alpha  and Estrogen Receptor beta  to Partial Estrogen Agonists/Antagonists
Mol. Pharmacol., July 1, 1998; 54(1): 105 - 112.
[Abstract] [Full Text]

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 Mol. Pharmacol.Home page
I. Wiesenberg, M. Chiesi, M. Missbach, C. Spanka, W. Pignat, and C. Carlberg
Specific Activation of the Nuclear Receptors PPARgamma and RORA by the Antidiabetic Thiazolidinedione BRL 49653 and the Antiarthritic Thiazolidinedione Derivative CGP 52608
Mol. Pharmacol., June 1, 1998; 53(6): 1131 - 1138.
[Abstract] [Full Text]

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 J. Biol. Chem.Home page
C. Mascaro, E. Acosta, J. A. Ortiz, P. F. Marrero, F. G. Hegardt, and D. Haro
Control of Human Muscle-type Carnitine Palmitoyltransferase I Gene Transcription by Peroxisome Proliferator-activated Receptor
J. Biol. Chem., April 10, 1998; 273(15): 8560 - 8563.
[Abstract] [Full Text] [PDF]

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 EndocrinologyHome page
T.-Z. Su, M. Wang, D. L. Oxender, and A. R. Saltiel
Troglitazone Increases System A Amino Acid Transport in 3T3-L1 Cells
Endocrinology, March 1, 1998; 139(3): 832 - 837.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
L. Fajas, D. Auboeuf, E. Raspe, K. Schoonjans, A.-M. Lefebvre, R. Saladin, J. Najib, M. Laville, J.-C. Fruchart, S. Deeb, et al.
The Organization, Promoter Analysis, and Expression of the Human PPARgamma Gene
J. Biol. Chem., July 25, 1997; 272(30): 18779 - 18789.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
J. Berger, M. Tanen, A. Elbrecht, A. Hermanowski-Vosatka, D. E. Moller, S. D. Wright, and R. Thieringer
Peroxisome Proliferator-activated Receptor-gamma Ligands Inhibit Adipocyte 11beta -Hydroxysteroid Dehydrogenase Type 1 Expression and Activity
J. Biol. Chem., April 13, 2001; 276(16): 12629 - 12635.
[Abstract] [Full Text] [PDF]

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 J. Biol. Chem.Home page
W. Arlt, R. J. Auchus, and W. L. Miller
Thiazolidinediones but Not Metformin Directly Inhibit the Steroidogenic Enzymes P450c17 and 3beta -Hydroxysteroid Dehydrogenase
J. Biol. Chem., May 11, 2001; 276(20): 16767 - 16771.
[Abstract] [Full Text] [PDF]


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