Diabetes
HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow Purchase Article
Right arrow View Shopping Cart
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Right arrow Request Permissions
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Staels, B.
Right arrow Articles by Fruchart, J.-C.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Staels, B.
Right arrow Articles by Fruchart, J.-C.
Social Bookmarking
Add to CiteULike   Add to Del.icio.us   Add to Digg   Add to Reddit   Add to Technorati  
What's this?

Diabetes 54:2460-2470, 2005
© 2005 by the American Diabetes Association, Inc.

Therapeutic Roles of Peroxisome Proliferator–Activated Receptor Agonists

Bart Staels, and Jean-Charles Fruchart

Department of Atherosclerosis, INSERM (Institut National de la Santé et de la Recherche Médicale) Unit 545, Institut Pasteur and Université de Lille, Lille, France

Peroxisome proliferator–activated receptors (PPARs) play key roles in the regulation of energy homeostasis and inflammation, and agonists of PPAR{alpha} and -{gamma} are currently used therapeutically. Fibrates, first used in the 1970s for their lipid-modifying properties, were later shown to activate PPAR{alpha}. These agents lower plasma triglycerides and VLDL particles and increase HDL cholesterol, effects that are associated with cardiovascular benefit. Thiazolidinediones, acting via PPAR{gamma}, influence free fatty acid flux and thus reduce insulin resistance and blood glucose levels. PPAR{gamma} agonists are therefore used to treat type 2 diabetes. PPAR{alpha} and -{gamma} agonists also affect inflammation, vascular function, and vascular remodeling. As knowledge of the pleiotropic effects of these agents advances, further potential indications are being revealed, including roles in the management of cardiovascular disease (CVD) and the metabolic syndrome. Dual PPAR{alpha}/{gamma} agonists (currently in development) look set to combine the properties of thiazolidinediones and fibrates, and they hold considerable promise for improving the management of type 2 diabetes and providing an effective therapeutic option for treating the multifactorial components of CVD and the metabolic syndrome. The functions of a third PPAR isoform, PPAR{delta}, and its potential as a therapeutic target are currently under investigation.

Address correspondence and reprint requests to Prof. Bart Staels, Unité INSERM 545-Institut Pasteur, 1, rue du Professeur Calmette, 59019 Lille Cedex, France. E-mail: bart.staels{at}pasteur-lille.fr


Add to CiteULike CiteULike   Add to Del.icio.us Del.icio.us   Add to Digg Digg   Add to Reddit Reddit   Add to Technorati Technorati    What's this?


This article has been cited by other articles:


Home page
 DiabetesHome page
M. Clemenz, N. Frost, M. Schupp, S. Caron, A. Foryst-Ludwig, C. Bohm, M. Hartge, R. Gust, B. Staels, T. Unger, et al.
Liver-Specific Peroxisome Proliferator-Activated Receptor {alpha} Target Gene Regulation by the Angiotensin Type 1 Receptor Blocker Telmisartan
Diabetes, May 1, 2008; 57(5): 1405 - 1413.
[Abstract] [Full Text] [PDF]

Home page
 JAMAHome page
S. E. Nissen, S. J. Nicholls, K. Wolski, R. Nesto, S. Kupfer, A. Perez, H. Jure, R. De Larochelliere, C. S. Staniloae, K. Mavromatis, et al.
Comparison of Pioglitazone vs Glimepiride on Progression of Coronary Atherosclerosis in Patients With Type 2 Diabetes: The PERISCOPE Randomized Controlled Trial
JAMA, April 2, 2008; 299(13): 1561 - 1573.
[Abstract] [Full Text] [PDF]

Home page
 DiabetesHome page
K. L. Han, J. S. Choi, J. Y. Lee, J. Song, M. K. Joe, M. H. Jung, and J.-K. Hwang
Therapeutic Potential of Peroxisome Proliferators-Activated Receptor-{alpha}/{gamma} Dual Agonist With Alleviation of Endoplasmic Reticulum Stress for the Treatment of Diabetes
Diabetes, March 1, 2008; 57(3): 737 - 745.
[Abstract] [Full Text] [PDF]

Home page
 Nephrol Dial TransplantHome page
P. Korantzopoulos, M. Elisaf, and H. J. Milionis
Multifactorial intervention in metabolic syndrome targeting at prevention of chronic kidney disease ready for prime time?
Nephrol. Dial. Transplant., October 1, 2007; 22(10): 2768 - 2774.
[Full Text] [PDF]

Home page
 JAMAHome page
A. M. Lincoff, K. Wolski, S. J. Nicholls, and S. E. Nissen
Pioglitazone and Risk of Cardiovascular Events in Patients With Type 2 Diabetes Mellitus: A Meta-analysis of Randomized Trials
JAMA, September 12, 2007; 298(10): 1180 - 1188.
[Abstract] [Full Text] [PDF]

Home page
 J Am Coll CardiolHome page
D. Aguilar, B. Bozkurt, A. Pritchett, N. J. Petersen, and A. Deswal
The Impact of Thiazolidinedione Use on Outcomes in Ambulatory Patients With Diabetes Mellitus and Heart Failure
J. Am. Coll. Cardiol., July 3, 2007; 50(1): 32 - 36.
[Abstract] [Full Text] [PDF]

Home page
 Endocr. Rev.Home page
B. L. Wajchenberg
{beta}-Cell Failure in Diabetes and Preservation by Clinical Treatment
Endocr. Rev., April 1, 2007; 28(2): 187 - 218.
[Abstract] [Full Text] [PDF]

Home page
 J. Pharmacol. Exp. Ther.Home page
V. Labinskyy, M. Bellomo, M. P. Chandler, M. E. Young, V. Lionetti, K. Qanud, F. Bigazzi, T. Sampietro, W. C. Stanley, and F. A. Recchia
Chronic Activation of Peroxisome Proliferator-Activated Receptor-{alpha} with Fenofibrate Prevents Alterations in Cardiac Metabolic Phenotype without Changing the Onset of Decompensation in Pacing-Induced Heart Failure
J. Pharmacol. Exp. Ther., April 1, 2007; 321(1): 165 - 171.
[Abstract] [Full Text] [PDF]

Home page
 J. Clin. Endocrinol. Metab.Home page
A. Grey, M. Bolland, G. Gamble, D. Wattie, A. Horne, J. Davidson, and I. R. Reid
The Peroxisome Proliferator-Activated Receptor-{gamma} Agonist Rosiglitazone Decreases Bone Formation and Bone Mineral Density in Healthy Postmenopausal Women: A Randomized, Controlled Trial
J. Clin. Endocrinol. Metab., April 1, 2007; 92(4): 1305 - 1310.
[Abstract] [Full Text] [PDF]

Home page
 Diabetes CareHome page
C. A. Stuart, M. E.A. Howell, and D. Yin
Overexpression of GLUT5 in Diabetic Muscle Is Reversed by Pioglitazone
Diabetes Care, April 1, 2007; 30(4): 925 - 931.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
L. A. Stoddart, A. J. Brown, and G. Milligan
Uncovering the Pharmacology of the G Protein-Coupled Receptor GPR40: High Apparent Constitutive Activity in Guanosine 5'-O-(3-[35S]thio)triphosphate Binding Studies Reflects Binding of an Endogenous Agonist
Mol. Pharmacol., April 1, 2007; 71(4): 994 - 1005.
[Abstract] [Full Text] [PDF]

Home page
 JAMAHome page
S. E. Nissen, S. J. Nicholls, K. Wolski, D. C. Howey, E. McErlean, M.-D. Wang, E. V. Gomez, and J. M. Russo
Effects of a Potent and Selective PPAR-{alpha} Agonist in Patients With Atherogenic Dyslipidemia or Hypercholesterolemia: Two Randomized Controlled Trials
JAMA, March 28, 2007; 297(12): 1362 - 1373.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
M. Scarsi, M. Podvinec, A. Roth, H. Hug, S. Kersten, H. Albrecht, T. Schwede, U. A. Meyer, and C. Rucker
Sulfonylureas and Glinides Exhibit Peroxisome Proliferator-Activated Receptor {gamma} Activity: A Combined Virtual Screening and Biological Assay Approach
Mol. Pharmacol., February 1, 2007; 71(2): 398 - 406.
[Abstract] [Full Text] [PDF]

Home page
 Mol. Pharmacol.Home page
S. Chintharlapalli, S. Papineni, and S. Safe
1,1-Bis(3'-Indolyl)-1-(p-substitutedphenyl)methanes Inhibit Growth, Induce Apoptosis, and Decrease the Androgen Receptor in LNCaP Prostate Cancer Cells through Peroxisome Proliferator-Activated Receptor {gamma}-Independent Pathways
Mol. Pharmacol., February 1, 2007; 71(2): 558 - 569.
[Abstract] [Full Text] [PDF]

Home page
 CirculationHome page
J. D. Brown and J. Plutzky
Peroxisome Proliferator Activated Receptors as Transcriptional Nodal Points and Therapeutic Targets
Circulation, January 30, 2007; 115(4): 518 - 533.
[Abstract] [Full Text] [PDF]

Home page
 Clin. Chem.Home page
Y. Wang, K. S. L. Lam, E. W. Kraegen, G. Sweeney, J. Zhang, A. W.K. Tso, W.-S. Chow, N. M.S. Wat, J. Y. Xu, R. L.C. Hoo, et al.
Lipocalin-2 Is an Inflammatory Marker Closely Associated with Obesity, Insulin Resistance, and Hyperglycemia in Humans
Clin. Chem., January 1, 2007; 53(1): 34 - 41.
[Abstract] [Full Text] [PDF]

Home page
 Pharmacol. Rev.Home page
L. Michalik, J. Auwerx, J. P. Berger, V. K. Chatterjee, C. K. Glass, F. J. Gonzalez, P. A. Grimaldi, T. Kadowaki, M. A. Lazar, S. O'Rahilly, et al.
International Union of Pharmacology. LXI. Peroxisome Proliferator-Activated Receptors
Pharmacol. Rev., December 1, 2006; 58(4): 726 - 741.
[Abstract] [Full Text] [PDF]

Home page
 J Biomol ScreenHome page
V. M. Nayagam, X. Wang, Y. C. Tan, A. Poulsen, K. C. Goh, T. Ng, H. Wang, H. Y. Song, B. Ni, M. Entzeroth, et al.
SIRT1 Modulating Compounds from High-Throughput Screening as Anti-Inflammatory and Insulin-Sensitizing Agents
J Biomol Screen, December 1, 2006; 11(8): 959 - 967.
[Abstract] [PDF]

Home page
 Am. J. Physiol. Endocrinol. Metab.Home page
S. Subramanian, M. A. DeRosa, C. Bernal-Mizrachi, N. Laffely, W. T. Cade, K. E. Yarasheski, P. E. Cryer, and C. F. Semenkovich
PPAR{alpha} activation elevates blood pressure and does not correct glucocorticoid-induced insulin resistance in humans
Am J Physiol Endocrinol Metab, December 1, 2006; 291(6): E1365 - E1371.
[Abstract] [Full Text] [PDF]

Home page
 Am. J. Physiol. Endocrinol. Metab.Home page
D. G. Haider, F. Mittermayer, G. Schaller, M. Artwohl, S. M. Baumgartner-Parzer, G. Prager, M. Roden, and M. Wolzt
Free fatty acids normalize a rosiglitazone-induced visfatin release
Am J Physiol Endocrinol Metab, November 1, 2006; 291(5): E885 - E890.
[Abstract] [Full Text] [PDF]

Home page
 J Am Coll CardiolHome page
A. J. Gilde, J.-C. Fruchart, and B. Staels
Peroxisome Proliferator-Activated Receptors at the Crossroads of Obesity, Diabetes, and Cardiovascular Disease
J. Am. Coll. Cardiol., October 27, 2006; 48(9_Suppl_A): A24 - A32.
[Abstract] [Full Text] [PDF]

Home page
 J Am Coll CardiolHome page
D. J. Angiolillo, E. Bernardo, C. Ramirez, M. A. Costa, M. Sabate, P. Jimenez-Quevedo, R. Hernandez, R. Moreno, J. Escaned, F. Alfonso, et al.
Insulin Therapy Is Associated With Platelet Dysfunction in Patients With Type 2 Diabetes Mellitus on Dual Oral Antiplatelet Treatment
J. Am. Coll. Cardiol., July 18, 2006; 48(2): 298 - 304.
[Abstract] [Full Text] [PDF]

Home page
 Eur J EndocrinolHome page
P. Iglesias and J. J Diez
Peroxisome proliferator-activated receptor gamma agonists in renal disease.
Eur. J. Endocrinol., May 1, 2006; 154(5): 613 - 621.
[Abstract] [Full Text] [PDF]

Home page
 J EndocrinolHome page
P Froment, F Gizard, D Defever, B Staels, J Dupont, and P Monget
Peroxisome proliferator-activated receptors in reproductive tissues: from gametogenesis to parturition.
J. Endocrinol., May 1, 2006; 189(2): 199 - 209.
[Abstract] [Full Text] [PDF]

Home page
 Arch Intern MedHome page
H. E. Bloomfield
The role of fibrates in a statin world.
Arch Intern Med, April 10, 2006; 166(7): 715 - 716.
[Full Text] [PDF]

Home page
 Arterioscler. Thromb. Vasc. Bio.Home page
F. Meisner, D. Walcher, F. Gizard, X. Kapfer, R. Huber, A. Noak, L. Sunder-Plassmann, H. Bach, C. Haug, M. Bachem, et al.
Effect of Rosiglitazone Treatment on Plaque Inflammation and Collagen Content in Nondiabetic Patients: Data From a Randomized Placebo-Controlled Trial
Arterioscler. Thromb. Vasc. Biol., April 1, 2006; 26(4): 845 - 850.
[Abstract] [Full Text] [PDF]

Home page
 HypertensionHome page
M. Schupp, L. D. Lee, N. Frost, S. Umbreen, B. Schmidt, T. Unger, and U. Kintscher
Regulation of Peroxisome Proliferator-Activated Receptor {gamma} Activity by Losartan Metabolites
Hypertension, March 1, 2006; 47(3): 586 - 589.
[Abstract] [Full Text] [PDF]

Home page
 DiabetesHome page
M. Schupp, M. Clemenz, R. Gineste, H. Witt, J. Janke, S. Helleboid, N. Hennuyer, P. Ruiz, T. Unger, B. Staels, et al.
Molecular Characterization of New Selective Peroxisome Proliferator-Activated Receptor {gamma} Modulators With Angiotensin Receptor Blocking Activity
Diabetes, December 1, 2005; 54(12): 3442 - 3452.
[Abstract] [Full Text] [PDF]

Home page
 JAMAHome page
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, November 23, 2005; 294(20): 2581 - 2586.
[Abstract] [Full Text] [PDF]


HOME HELP FEEDBACK SUBSCRIPTIONS ARCHIVE SEARCH TABLE OF CONTENTS
Diabetes Diabetes Care Clinical Diabetes Diabetes Spectrum
Copyright © 2005 by the American Diabetes Association.