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| peroxisome proliferator activated receptorsSummarySummary: TRANSCRIPTION FACTORS that are activated by ligands and heterodimerize with RETINOID X RECEPTORS and bind to peroxisome proliferator response elements in the promoter regions of target genes. Top Publications
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Publications
Effects of bezafibrate, PPAR pan-agonist, and GW501516, PPARdelta agonist, on development of steatohepatitis in mice fed a methionine- and choline-deficient dietTatsuya Nagasawa
Toxicology Research Laboratory, R and D, Kissei Pharmaceutical Co, Ltd, 2320 1 Maki, Hotaka, Azumino City, Nagano Pref, 399 8305, Japan
Eur J Pharmacol 536:182-91. 2006....
Molecular mechanisms of cross-talk between thyroid hormone and peroxisome proliferator activated receptors: focus on the heartOuti M Hyyti
Division of Cardiology, Department of Pediatrics, Childrens Hospital and Regional Medical Center, 4800 Sandpoint Way NE, 4G-1, Seattle, WA 98105, USA
Cardiovasc Drugs Ther 20:463-9. 2006Thyroid hormone receptors (TR) and peroxisome proliferator activated receptors (PPAR) regulate cardiac metabolism...
Peroxisome proliferator-activated receptor expression and activation in normal human colonic epithelial cells and tubular adenomasMads Wichmann Matthiessen
Department of Medical Gastroenterology C112, Herlev University Hospital, 2730 Herlev, Denmark
Scand J Gastroenterol 40:198-205. 2005..Moreover, they raise interest in investigation of PPAR alpha as a therapeutic target to prevent adenoma formation...
Polyunsaturated fatty acid regulation of genes of lipid metabolismHarini Sampath
Department of Nutritional Sciences, University of Wisconsin Madison, Madison, Wisconsin 53706, USA
Annu Rev Nutr 25:317-40. 2005..Working out the mechanisms by which these interactions and consequent effects occur is proving to be complicated but is invaluable to our understanding of the role that dietary fat can play in disease management and prevention...
Peroxisome proliferator-activated receptors as sensors of fatty acids and derivativesP A Grimaldi
Inserm U636, Centre de Biochimie, UFR Sciences, Universite de Nice Sophia Antipolis, Parc Valrose, 06108, Nice, France
Cell Mol Life Sci 64:2459-64. 2007....
Therapeutic roles of peroxisome proliferator-activated receptor agonistsBart Staels
Department of Atherosclerosis, Unité INSERM 545 Institut Pasteur, 1, rue du Professeur Calmette, 59019 Lille Cedex, France
Diabetes 54:2460-70. 2005..The functions of a third PPAR isoform, PPARdelta, and its potential as a therapeutic target are currently under investigation...
The human semaphorin 6B gene is down regulated by PPARsPhilippe Collet
EA 3446 Peroxisome Proliferators, Faculty of Sciences, BP 239, University Henri Poincaré Nancy 1, 54506 Vandoeuvre les Nancy, France
Genomics 83:1141-50. 2004..In addition, cross talk between the peroxisome proliferator and retinoic acid pathways is suggested...
Modulation of HepG2 cell net apolipoprotein B secretion by the citrus polymethoxyflavone, tangeretinElzbieta M Kurowska
KGK Synergize Inc, Research and Development Division, London, Ontario, Canada N6A 5R8
Lipids 39:143-51. 2004..control). The data suggest that tangeretin modulates apoB-containing lipoprotein metabolism through multiple mechanisms...
Dual and pan-peroxisome proliferator-activated receptors (PPAR) co-agonism: the bezafibrate lessonsAlexander Tenenbaum
Cardiac Rehabilitation Institute, Sheba Medical Center, 52621 Tel Hashomer, Israel
Cardiovasc Diabetol 4:14. 2005..More powerful new compounds with pan-PPAR activity and proven long-term safety should be highly effective in a clinical setting of patients with coexisting relevant lipid and glucose metabolism disorders...
Be fit or be sick: peroxisome proliferator-activated receptors are down the roadBeatrice Desvergne
Center for Integrative Genomics, University of Lausanne, Biology Building, CH 1015 Lausanne Dorigny, Switzerland
Mol Endocrinol 18:1321-32. 2004..This review presents a summary of the recent findings on their dual involvement in health and disease...
Identification and organ expression of peroxisome proliferator activated receptors in brown trout (Salmo trutta f. fario)Carla Batista-Pinto
Laboratory of Cell Biology, ICBAS Institute of Biomedical Sciences Abel Salazar, University of Porto, Portugal
Biochim Biophys Acta 1731:88-94. 2005Although widely studied in mammals, little information about fish peroxisome proliferator activated receptors (PPARs) is yet available...
International Union of Pharmacology. LXI. Peroxisome proliferator-activated receptorsLiliane Michalik
Center for Integrative Genomics, National Research Centre Frontiers in Genetics, University of Lausanne, Lausanne, Switzerland
Pharmacol Rev 58:726-41. 2006..Thus, selective action of PPARs in vivo results from the interplay at a given time point between expression levels of each of the three PPAR and RXR isotypes, affinity for a specific promoter PPRE, and ligand and cofactor availabilities...
Safety issues and prospects for future generations of PPAR modulatorsAnne Rubenstrunk
GENFIT, F 59006 Loos, France
Biochim Biophys Acta 1771:1065-81. 2007..The selective modulation of PPAR activities is a promising approach to develop new drugs with preserved efficacy but diminished adverse effects...
PPAR- and LXR-dependent pathways controlling lipid metabolism and the development of atherosclerosisAndrew C Li
Department of Cellular and Molecular Medicine, University of California, San Diego, La Jolla, CA 92093, USA
J Lipid Res 45:2161-73. 2004..Here, we review recent studies that provide new insights into the mechanisms by which these subclasses of nuclear receptors act to systemically influence lipid and glucose metabolism and regulate gene expression within the artery wall...
A PPAR response element regulates transcription of the gene for human adipose differentiation-related proteinPaul Targett-Adams
MRC Virology Unit, Institute of Virology, University of Glasgow, Church Street, Glasgow G11 5JR, UK
Biochim Biophys Acta 1728:95-104. 2005..These findings offer insight into the mechanisms which serve to regulate ADRP transcription and intracellular lipid storage...
Kinase signaling cascades that modulate peroxisome proliferator-activated receptorsLaurent Gelman
Center for Integrative Genomics, NCCR Frontiers in Genetics, University of Lausanne, Switzerland
Curr Opin Cell Biol 17:216-22. 2005..The study of this dual regulation mode, which allows PPARs to integrate signals conveyed by lipophilic ligands with those coming from the plasma membrane, may ultimately offer new therapeutic strategies...
Evaluation of polycyclic aromatic hydrocarbons in the activation of early growth response-1 and peroxisome proliferator activated receptorsJeong-Ho Kim
Department of Pathobiology, University of Tennessee, Knoxville, Tennessee 37996, USA
Toxicol Sci 85:585-93. 2005..In conclusion, PAHs activate PPAR alpha and PPAR beta/delta, and up-regulate EGR-1 expression in vitro as well as in vivo. These data may provide a diversity of PAH activity in several biological pathways...
Evolution of peroxisome proliferator-activated receptor agonistsFeng Chang
Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA
Ann Pharmacother 41:973-83. 2007..To discuss the evolution of peroxisome proliferator-activated receptor (PPAR) agonists from single site to multiple subtype or partial agonists for the treatment of type 2 diabetes, dyslipidemia, obesity, and the metabolic syndrome...
Multiple expression control mechanisms of peroxisome proliferator-activated receptors and their target genesNguan Soon Tan
Center for Integrative Genomics, NCCR Frontiers in Genetics, University of Lausanne, Biology Building, CH-1015 Lausanne, Switzerland
J Steroid Biochem Mol Biol 93:99-105. 2005..It is also becoming apparent that understanding the regulation of PPAR expression and activity, can itself have a significant influence on how the expression of subgroups of target genes is studied and integrated in current knowledge...
An overview on biological mechanisms of PPARsBhavani Prasad Kota
Faculty of Pharmacy, The University of Sydney, Sydney, NSW 2006, Australia
Pharmacol Res 51:85-94. 2005b>Peroxisome proliferator activated receptors (PPARs) are transcriptional factors belonging to the ligand-activated nuclear receptor superfamily. They are ubiquitously expressed throughout the body...
PPARs: therapeutic targets for metabolic diseaseJoel P Berger
Department of Metabolic Disorders, Merck Research Laboratories, Rahway, NJ 07065, USA
Trends Pharmacol Sci 26:244-51. 2005..Novel PPAR ligands are now being developed that possess broader efficacies and improved tolerability compared with currently available therapeutic agents...
Suppression of colitis-related mouse colon carcinogenesis by a COX-2 inhibitor and PPAR ligandsHiroyuki Kohno
Department of Oncologic Pathology, Kanazawa Medical University, Uchinada, Ishikawa 920 0293, Japan
BMC Cancer 5:46. 2005....
PPARs as drug targets to modulate inflammatory responses?Raphael Genolet
Center for Integrative Genomics, NCCR Frontiers in Genomics, University of Lausanne, CH 1015 Lausanne, Switzerland
Curr Drug Targets Inflamm Allergy 3:361-75. 2004..We also discuss the potential utilisation of PPAR specific ligands in the treatment of inflammatory diseases, such as inflammatory bowel diseases, atherosclerosis, Parkinson's and Alzheimer's diseases...
Cannabinoids go nuclear: evidence for activation of peroxisome proliferator-activated receptorsS E O'Sullivan
School of Biomedical Sciences, University of Notttingham, Queen s Medical Center, Nottingham, UK
Br J Pharmacol 152:576-82. 2007....
Differential responses of PPARalpha, PPARdelta, and PPARgamma reporter cell lines to selective PPAR synthetic ligandsMathieu Seimandi
, , 60 rue de Navacelles, 34090 Montpellier, France
Anal Biochem 344:8-15. 2005..We conclude that our stable models allow specific and sensitive measurement of PPAR ligand activities and are a high-throughput, cell-based screening tool for identifying and characterizing PPAR ligands...
From molecular action to physiological outputs: peroxisome proliferator-activated receptors are nuclear receptors at the crossroads of key cellular functionsJerome N Feige
Center for Integrative Genomics, NCCR Frontiers in Genetics, Le Génopode, University of Lausanne, CH 1015 Lausanne, Switzerland
Prog Lipid Res 45:120-59. 2006..Finally, we discuss how the integration of various intra-cellular signaling pathways allows PPARs to participate to whole-body homeostasis by mediating regulatory crosstalks between organs...
Fluorescence imaging reveals the nuclear behavior of peroxisome proliferator-activated receptor/retinoid X receptor heterodimers in the absence and presence of ligandJerome N Feige
Center for Integrative Genomics, NCCR Frontiers in Genetics, University of Lausanne, CH 1015 Lausanne, Switzerland
J Biol Chem 280:17880-90. 2005....
Attenuation of progression of insulin resistance in patients with coronary artery disease by bezafibrateAlexander Tenenbaum
Cardiac Rehabilitation Institute, Tel-Hashomer, Israel
Arch Intern Med 166:737-41. 2006..001). CONCLUSIONS: In patients with coronary artery disease enrolled in our study, as represented by the placebo group, HOMA-IR increased over time. During the 2 years of the follow-up, bezafibrate significantly attenuated this process...
Interleukin-2 suppression by 2-arachidonyl glycerol is mediated through peroxisome proliferator-activated receptor gamma independently of cannabinoid receptors 1 and 2Cheryl E Rockwell
Department of Pharmacology and Toxicology, Michigan State University, 315 National Food Safety and Toxicology Building, East Lansing, MI 48824-1317, USA
Mol Pharmacol 70:101-11. 2006..Together, the aforementioned studies identify PPARgamma as a novel intracellular target of 2-AG, which mediates the suppression of IL-2 by 2-AG in a manner that is independent of CB1 and/or CB2...
Peroxisome proliferator-activated receptors as transcriptional nodal points and therapeutic targetsJonathan D Brown
Cardiovascular Division, Brigham and Women s Hospital, Boston, Mass, USA
Circulation 115:518-33. 2007..Such analysis of the existing PPAR data, the appropriate use of currently approved PPAR agonists, and continued progress in PPAR therapeutics will be predicated on a better understanding of PPAR biology...
Peroxisome proliferator-activated receptor structures: ligand specificity, molecular switch and interactions with regulatorsVincent Zoete
Swiss Institute of Bioinformatics SIB, Quartier Sorge, Batiment Genopode, CH 1015 Lausanne, Switzerland
Biochim Biophys Acta 1771:915-25. 2007..Finally, the interactions of PPARs LBD with co-activators or co-repressors, as well as with the retinoid X receptor (RXR) are described and considered in relation to PPARs activation...
Liver X receptor mediates hepatitis B virus X protein-induced lipogenesis in hepatitis B virus-associated hepatocellular carcinomaTae Young Na
College of Pharmacy, Seoul National University, Seoul, Korea
Hepatology 49:1122-31. 2009..CONCLUSION: Our results suggest a novel association between HBx and LXR that may represent an important mechanism explaining HBx-induced hepatic lipogenesis during HBV-associated hepatic carcinogenesis...
Peroxisome proliferator-activated receptor agonists modulate heart function in transgenic mice with lipotoxic cardiomyopathyReeba K Vikramadithyan
Department of Medicine, Columbia University, New York, NY 10032, USA
J Pharmacol Exp Ther 313:586-93. 2005..These changes were paralleled by alterations in heart lipid uptake. Overall, PPAR activators exhibit differential effects in this model of lipotoxic dilated cardiomyopathy...
Pan-PPAR agonist beneficial effects in overweight mice fed a high-fat high-sucrose dietCaroline Fernandes-Santos
Biomedical Center, Institute of Biology, State University of Rio de Janeiro, Brazil
Nutrition 25:818-27. 2009....
The insulin-like growth factor-binding protein 1 gene is a primary target of peroxisome proliferator-activated receptorsTatjana Degenhardt
Department of Biochemistry and A I Virtanen Institute, University of Kuopio, FIN 70211 Kuopio, Finland
J Biol Chem 281:39607-19. 2006..We also show that these additional PPAR binding genes contain a number of candidate PPREs and that their mRNA levels respond quickly to the presence of PPAR ligands, indicating that they are also primary PPAR target genes...
PPAR agonists modulate human osteoclast formation and activity in vitroB Y Chan
Department of Clinical Biochemistry, Royal Liverpool University Hospital, The University of Liverpool, Liverpool, L69 3GA, UK
Bone 40:149-59. 2007..In conclusion, this study highlights the potential of PPARs as therapeutic targets in diseases with accelerated osteoclast formation and resorption...
Genome-wide identification of peroxisome proliferator response elements using integrated computational genomicsDanielle G Lemay
United States Department of Agriculture, Agricultural Research Service, Western Human Nutrition Research Center, and Department of Nutrition, University of California-Davis, 95616, USA
J Lipid Res 47:1583-7. 2006..g., chromatin remodeling, DNA damage response, Wnt, and mitogen-activated protein kinase signaling). This first genome-wide library of high-confidence predicted PPAR target genes will be a valuable resource to PPAR biologists...
The emerging role of lipoproteins in atherogenesis: beyond LDL cholesterolStephen Nicholls
Heart Research Institute, Sydney, Australia
Semin Vasc Med 4:187-95. 2004..As such, these factors have become important targets in the development of effective strategies to prevent atherosclerotic cardiovascular disease...
Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligandsAlan M Warshawsky
Eli Lilly and Co, Indianapolis, IN 46285, USA
Bioorg Med Chem Lett 16:6328-33. 2006..Several compounds in this series have demonstrated potent plasma glucose and triglyceride lowering capability in rodent models of type 2 diabetes...
Nutrients, nuclear receptors, inflammation, immunity lipids, PPAR, and allergic asthmaAvery August
Center for Molecular Immunology and Infectious Disease, The Pennsylvania State University, University Park, 16802, USA
J Nutr 136:695-9. 2006..In vitro, T cells from ciglitazone-treated mice secreted significantly less IL-4 and IFN-gamma in response to restimulation. These data suggest that PPARgamma agonists may be useful for the treatment of allergic asthma...
Effects of peroxisome proliferator-activated receptor ligands in modulating tissue factor and tissue factor pathway inhibitor in acutely symptomatic carotid atheromasJonathan Golledge
Vascular Biology Unit, School of Medicine, James Cook University, Townsville, Queensland, Australia
Stroke 38:1501-8. 2007..We investigated the effect of peroxisome proliferator-activated receptor (PPAR) -alpha and -gamma ligands in acutely modifying tissue factor (TF) and tissue factor pathway inhibitor (TFPI) in unstable carotid atheromas...
Differential effects of peroxisome proliferator-activated receptor ligands and sulfonylurea plus statin treatment on plasma concentrations of adipokines in type 2 diabetes with dyslipidemiaW H Yin
Division of Cardiology, Department of Internal Medicine, Cheng Hsin General Hospital, and Institute of Clinical Medicine, Cardiovascular Research Center, National Yang Ming University, School of Medicine, Taipei, Taiwan
Diabetes Metab 32:229-35. 2006..We hypothesized that the combination of TZD+fibrate may be better than the sulfonylurea + statin approach regarding modifying the adipokine profile in diabetic patients with dyslipidemia...
PPARs and other nuclear receptors in inflammationGiovanni Rizzo
Department of Internal Medicine, University of Perugia, Via E dal Pozzo, 06122 Perugia, Italy
Curr Opin Pharmacol 6:421-7. 2006..In addition, peroxisome proliferator-activated receptors and liverXreceptors, in response to endogenous eicosanoids and oxysterols, respectively, modulate transcriptional pathways involved in inflammatory responses and lipid homeostasis...
Activation of mouse and human peroxisome proliferator-activated receptors (alpha, beta/delta, gamma) by perfluorooctanoic acid and perfluorooctane sulfonateMargy L Takacs
Reproductive Toxicology Division, National Health and Environmental Effects Research Laboratory, Office of Research and Development, US Environmental Protection Agency, Research Triangle Park, North Carolina 27711, USA
Toxicol Sci 95:108-17. 2007....
[Peroxisome proliferator activated receptor ligands and angiogenesis]Mayumi Sato
Medical R and D Center, Tokyo Metropolitan Institute for Medical Science
Nippon Rinsho 63:603-8. 2005..In this review, I highlight data concerning PPARs ligands involved in the biological mechanisms underlying antiangiogenesis...
PPAR-gamma expression in pituitary tumours and the functional activity of the glitazones: evidence that any anti-proliferative effect of the glitazones is independent of the PPAR-gamma receptorMichelle N Emery
Department of Endocrinology, St. Bartholomew's and the Royal London School of Medicine and Dentistry, London, UK
Clin Endocrinol (Oxf) 65:389-95. 2006..CONCLUSIONS :Our data suggest that the antiproliferative action of rosiglitazone is probably not via PPAR-gamma...
Modulation of PPAR activity via phosphorylationKatherine A Burns
Department of Veterinary and Biomedical Sciences and Center for Molecular Toxicology and Carcinogenesis, Penn State University, University Park, PA 16802, USA
Biochim Biophys Acta 1771:952-60. 2007..The review will summarize the known PPAR kinases that directly act on these receptors, the sites affected and the result of this modification on receptor activity...
Peroxisome proliferator-activated receptors and liver X receptors in atherosclerosis and immunityGrant D Barish
Gene Expression Laboratory, The Salk Institute for Biological Studies, La Jolla, CA 92037, USA
J Nutr 136:690-4. 2006....
Tetrahydroisoquinoline PPARgamma agonists: design of novel, highly selective non-TZD antihyperglycemic agentsJames R Henry
Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Bioorg Med Chem Lett 16:6293-7. 2006..Novel tetrahydroisoquinolines have been developed as potent PPAR ligands. Evaluation of these compounds in PPARgamma responsive models of type 2 diabetes is described...
The next generation of PPAR drugs: do we have the tools to find them?Barry G Shearer
GlaxoSmithKline Research and Development, 5 Moore Drive, Research Triangle Park, NC 27709, USA
Biochim Biophys Acta 1771:1082-93. 2007..In this review we will discuss the side effects associated the PPARs, how the current drugs in clinical development were discovered and new concepts in how to screen for PPAR drugs...
[PPAR family and its relationship to metabolic syndrome]Xiao-yan Zhang
Peking University Diabetes Center, Department of Physiology and Pathophysiology, Peking University Health Science Center, Beijing 100083
Sheng Li Ke Xue Jin Zhan 36:6-12. 2005..Particular emphasis is placed on their pathogenic roles in the metabolic syndrome and the therapeutic utility of PPAR modulators in the treatment of type II diabetes...
Nuclear receptors and autoimmune disease: the potential of PPAR agonists to treat multiple sclerosisMichael K Racke
Department of Neurology, University of Texas Southwestern Medical Center, Dallas, 75390, USA
J Nutr 136:700-3. 2006..The fact that PPARalpha agonists have been used as therapeutic agents in humans to treat metabolic conditions for over 25 years with little toxicity makes them attractive candidates for use as adjunctive therapies in MS...
Gaining weight: the Keystone Symposium on PPAR and LXRMichael Lehrke
Division of Endocrinology, Diabetes, and Metabolism, Department of Medicine, and The Institute for Diabetes, Obesity, and Metabolism, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
Genes Dev 19:1737-42. 2005..In recognition of this, a recent Keystone Symposium was devoted to these metabolic receptors. Here, we summarize some of the major highlights and future projections discussed at the meeting...
Regulation of adiponectin receptor 1 in human hepatocytes by agonists of nuclear receptorsMarkus Neumeier
Department of Internal Medicine I, University of Regensburg, D 93042 Regensburg, Germany
Biochem Biophys Res Commun 334:924-9. 2005..Elevated AdipoR1 induced by hepatotoxic troglitazone may indicate a role of this receptor in adiponectin-mediated beneficial effects in liver damage...
Peroxisome proliferator-activated receptors (PPARs) in skin health, repair and diseaseLiliane Michalik
Center for Integrative Genomics, National Research Center Frontiers in Genetics, University of Lausanne, Genopode Building, CH 1015 Lausanne, Switzerland
Biochim Biophys Acta 1771:991-8. 2007..Due to their collective diverse functions in skin biology, PPARs represent a major research target for the understanding and treatment of many skin diseases, such as benign epidermal tumors, papillomas, acne vulgaris and psoriasis...
Caloric restriction results in decreased expression of peroxisome proliferator-activated receptor superfamily in muscle of normal and long-lived growth hormone receptor/binding protein knockout miceMichal M Masternak
Department of Internal Medicine, Geriatrics Research, Southern Illnois University School of Medicine, Springfield, 62794 9628, USA
J Gerontol A Biol Sci Med Sci 60:1238-45. 2005..This suggested metabolic change clearly does not affect whole-body insulin action. These findings suggest that whole-animal insulin sensitivity is not regulated through skeletal muscle insulin action...
Peroxisome proliferator-activated receptor alpha, delta, gamma1 and gamma2 expressions are present in human monocyte-derived dendritic cells and modulate dendritic cell maturation by addition of subtype-specific ligandsM A Jakobsen
Department of Clinical Immunology, Odense University Hospital, Odense, Denmark
Scand J Immunol 63:330-7. 2006..Our data suggest that naturally occurring PPAR ligands like fatty acids and fatty acid derivates have anti-inflammatory effects by redirecting DC into a less stimulatory mode...
LXR and PPAR activators stimulate cholesterol sulfotransferase type 2 isoform 1b in human keratinocytesYan J Jiang
Department of Medicine, University of California San Francisco, San Francisco, CA 94121, USA
J Lipid Res 46:2657-66. 2005..Thus, LXR and PPAR activators regulate the expression of SULT2B1b, the key enzyme in the synthesis of CS, which is a potent regulator of epidermal differentiation and corneocyte desquamation...
The peroxisome proliferator-activated receptor N-terminal domain controls isotype-selective gene expression and adipogenesisSarah Hummasti
Howard Hughes Medical Institute, Department of Pathology and Laboratory Medicine, University of California, Los Angeles, California 90095-1662, USA
Mol Endocrinol 20:1261-75. 2006..A more detailed understanding of the mechanisms by which the individual PPARs differentially regulate gene expression should aid in the design of more effective drugs, including tissue- and target gene-selective PPAR modulators...
Mitochondria, ciglitazone and liver: a neglected interaction in biochemical pharmacologyRoberto Scatena
Istituto di Biochimica e Biochimica Clinica, Universita Cattolica, Rome, Italy
Eur J Pharmacol 567:50-8. 2007b>Peroxisome proliferator activated receptors (PPARs) are a class of nuclear receptors now actively investigated for their involvement in lipid and glucidic metabolism, immune regulation and cell differentiation...
Oxidative stress influences cholesterol efflux in THP-1 macrophages: role of ATP-binding cassette A1 and nuclear factorsValérie Marcil
Centre de Recherche, CHU Sainte Justine, Universite de Montreal, 3175, Cote Ste Catherine, Montreal Quebec, Canada H3T 1C5
Cardiovasc Res 72:473-82. 2006..Our aim was to characterize the effects of oxidative stress on key receptors of macrophage cholesterol homeostasis, on the nuclear transcription factors PPAR and LXR regulating their expression, and on macrophage cholesterol handling...
Rational drug design and PPAR agonistsRiccardo Perfetti
Department of Medical Sciences, Amgen Inc, One Amgen Center Drive, Mail Stop 38 3 A, Thousand Oaks, CA 91320 1799, USA
Curr Diab Rep 5:340-5. 2005....
Peroxisome-proliferator-activated receptors and the control of levels of prostaglandin-endoperoxide synthase 2 by arachidonic acid in the bovine uterusE Linda R Sheldrick
Division of Animal Physiology, School of Biosciences, University of Nottingham, Sutton Bonington Campus, Loughborough LE12 5RD, UK
Biochem J 406:175-83. 2007..The results are consistent with the hypothesis that arachidonic acid acts via PPARalpha to increase PTGS2 levels in bovine endometrial stromal cells...
Gender and genetic differences in bladder smooth muscle PPAR mRNA in a porcine model of the metabolic syndromeHeather M Mattern
Department of Medical Pharmacology and Physiology, University of Missouri, MA415 Medical Sciences Building, Columbia, MO 65212, USA
Mol Cell Biochem 302:43-9. 2007..We conclude that PPAR profiles in BSM may contribute to the susceptibility of BSM to lipotoxicity in the metabolic syndrome...
Changes in expression levels of genes involved in fatty acid metabolism: upregulation of all three members of the PPAR family (alpha, gamma, delta) and the newly described adiponectin receptor 2, but not adiponectin receptor 1 during neonatal cardiac deveMichael Steinmetz
Department of Pediatric Cardiology and Intensive Care Medicine, Georg August University Gottingen, Robert Koch Str 40, 37075 Gottingen, Germany
Basic Res Cardiol 100:263-9. 2005..The aim of this study was to investigate the changes in mRNA expression levels of genes involved in the control of cardiac fatty acid metabolism in the transition from neonatal to adult life...
Induction of adiponectin by natural and synthetic phenolamides in mouse and human preadipocytes and its enhancement by docosahexaenoic acidYoshimitsu Yamazaki
Institute for Biological Resources and Functions, National Institute of Advanced Industrial Science and Technology, 1 1 1 Higashi, Tsukuba, Ibaraki 305 8566, Japan
Life Sci 82:290-300. 2008....
Nuclear hormone receptors and intestinal inflammationGary D Wu
Gastroenterology 133:1068. 2007
Dissociation of oxidant production by peroxisome proliferator-activated receptor ligands from cell death in human cell linesElisa B Atarod
Division of Pharmacology and Toxicology, College of Pharmacy, University of Texas at Austin, Austin, TX 78712-0125, USA
Free Radic Biol Med 37:36-47. 2004..These data also suggest that oxidant production induced by PPARalpha ligands originates in the mitochondria...
PPARalpha agonists stimulate progastrin production in human colorectal carcinoma cellsShamilah Lachal
Department of Surgery ARMC, University of Melbourne, Department of Surgery, Austin Health, Heidelberg, Victoria 3084, Australia
Regul Pept 120:243-51. 2004..These studies have revealed a relationship between PPARs and gastrin, two regulatory molecules implicated in the pathogenesis of CRC...
Novel oxazole containing phenylpropane derivatives as peroxisome proliferator activated receptor agonists with hypolipidemic activityH Pingali
Zydus Research Centre, Sarkhej Bavla N H 8A Moraiya, Ahmedabad, India
Pharmazie 63:497-502. 2008..Compounds 3c and 3d showed the desired predominant PPARalpha activity and excellent tryiglyceride reduction in vivo and were selected as lead compounds for further development as hypolipidemic agents...
Tissue-specific expression of PPAR mRNAs in diabetic rats and divergent effects of cilostazolFurong Wang
Provincial Hospital affiliated to Shandong University, Jinan, Shandong 250021, China
Can J Physiol Pharmacol 86:465-71. 2008..In conclusion, mRNA expression of PPARs is tissue-specific in diabetes and may be differently affected by cilostazol, possibly because of its tissue-specific effects on cAMP content...
PPAR agonists: multimodal drugs for the treatment of type-2 diabetesBarbara Gross
Institut Pasteur de Lille, 1 rue du Prof Calmette, Lille, F 59019, France
Best Pract Res Clin Endocrinol Metab 21:687-710. 2007..This chapter focuses on the PPAR agonists currently used in the clinic, as well as on the discovery and development of the next generation of PPAR agonists...
1. Peroxisome proliferator-activated receptor gamma (PPARgamma) ligands and their therapeutic utilityBrad R Henke
Metabolic and Viral Diseases Drug Discovery Research, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA
Prog Med Chem 42:1-53. 2004
[Nuclear receptor PPAR and hepatology: pathophysiological and therapeutical aspects]S Dharancy
INSERM U795, Boulevard du Professeur Jules Leclercq, 59037 Lille, France
Gastroenterol Clin Biol 32:339-50. 2008..In terms of therapy, animal studies and human trials have been conducted in steatopathies. However, clinicians have to be aware of potential specific side effects related to glitazones especially on cardiovascular system...
Peroxisome proliferator-activated receptors mediate host cell proinflammatory responses to Pseudomonas aeruginosa autoinducerAruna Jahoor
Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, 3601 4th St, Lubbock, TX 79430, USA
J Bacteriol 190:4408-15. 2008..These data identify PPARbeta/delta and PPARgamma as putative mammalian 3OC(12)-HSL receptors and suggest that PPARgamma agonists may be employed as anti-inflammatory therapeutics for P. aeruginosa infections...
In vivo imaging reveals selective peroxisome proliferator activated receptor modulator activity of the synthetic ligand 3-(1-(4-chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)Andrea Biserni
Center of Excellence on Neurodegenerative Diseases, Department of Pharmacological Sciences, University of Milan, Via Balzaretti 9, 20133 Milan, Italy
Mol Pharmacol 73:1434-43. 2008..The results of this study, demonstrating the usefulness of reporter mice, may open new avenues for the development of innovative drugs for cardiovascular, endocrine, neural, and skeletal systems characterized by limited side effects...
Effect of medium- and long-chain fatty acid diets on PPAR and SREBP-1 expression and glucose homeostasis in ACBP-overexpressing transgenic ratsS Oikari
Department of Biotechnology and Molecular Medicine, A I Virtanen Institute for Molecular Sciences, Kuopio, Finland
Acta Physiol (Oxf) 194:57-65. 2008..As the physiological relevance of ACBP in the regulation of lipid metabolism under high fat diets is unclear, we investigated the influence of such diets on the metabolic responses in ACBP-overexpressing rats...
Transcriptome analysis of endometrial cancer identifies peroxisome proliferator-activated receptors as potential therapeutic targetsCathrine M Holland
Department of Pathology, University of Cambridge, The Rosie Hospital, Box 223, Level 2, Robinson Way, Cambridge CB2 2SW, United Kingdom
Mol Cancer Ther 3:993-1001. 2004..These results support further investigation of members of the PPAR/retinoid X receptor pathway as novel therapeutic targets in endometrial cancer...
Lipid synthesis in macrophages during inflammation in vivo: effect of agonists of peroxisome proliferator activated receptors alpha and gamma and of retinoid X receptorsE N Posokhova
Institute of Internal Medicine, Siberian Branch of the Russian Academy of Medical Sciences, Novosibirsk, Russia
Biochemistry (Mosc) 73:296-304. 2008The effects of peroxisome proliferator activated receptors alpha and gamma (PPAR-alpha and PPAR-gamma) and retinoid X receptor (RXR) agonists upon synthesis and accumulation of lipids in murine C57Bl macrophages during inflammation ..
Preventing the progression of diabetes mellitusBrian V Reamy
Am Fam Physician 71:425. 2005
PPAR and LXR activators regulate ABCA12 expression in human keratinocytesYan J Jiang
Metabolism Section, Department of Veterans Affairs Medical Center, Northern California Institute for Research and Education, University of California at San Francisco, San Francisco, California 94121, USA
J Invest Dermatol 128:104-9. 2008..Together, our data demonstrate that PPAR and LXR activators increase ABCA12 expression, providing an additional mechanism by which PPAR and LXR activators promote epidermal permeability barrier homeostasis...
A PPARs cross-talk concertedly commits C6 glioma cells to oligodendrocytes and induces enzymes involved in myelin synthesisAndrea V Leisewitz
Facultad de Ciencias Biologicas, Department of Cellular and Molecular Biology, Centro de Regulación Celular y Patología CRCP, Millennium Institute for Fundamental and Applied Biology, P Universidad Catolica de Chile, Alameda, Santiago, Chile
J Cell Physiol 217:367-76. 2008b>Peroxisome proliferator activated receptors (PPARs, alpha, beta/delta, gamma) control lipid homeostasis and differentiation in various tissues and tumor cells...
PPARs and their metabolic modulation: new mechanisms for transcriptional regulation?W Ahmed
Cardiovascular Division, Harvard Medical School, Brigham and Women s Hospital, Boston, MA, USA
J Intern Med 262:184-98. 2007....
Synthesis and biological activity of benzoxazole containing thiazolidinedione derivativesRaok Jeon
College of Pharmacy, Sookmyung Women s University, Chungpa dong 2 Ka, Yongsan Ku, Seoul 140 742, Korea
Arch Pharm Res 27:1099-105. 2004..Most compounds tested were identified as potent PPARgamma agonists...
PPARs special issue: anchoring the present to explore the futureBeatrice Desvergne
University of Lausanne, Genopode, 1015 Lausanne, Switzerland
Biochim Biophys Acta 1771:913-4. 2007
Phosphorylation of PPARs: from molecular characterization to physiological relevanceClaire Diradourian
, Institut Cochin, INSERM U567 CNRS UMR8104, , 24, rue du Faubourg Saint Jacques 75014 Paris, France
Biochimie 87:33-8. 2005..Molecular consequences are multiple, including changes in ligand affinity, DNA binding, recruitment of transcriptional cofactors, proteasome degradation... Finally, the physiological relevance of PPAR phosphorylation is discussed...
Modulation of PPAR in aging, inflammation, and calorie restrictionBokyung Sung
College of Pharmacy, Aging Tissue Bank, Pusan National University, Busan, Korea
J Gerontol A Biol Sci Med Sci 59:997-1006. 2004..Based on these findings, we conclude that the altered expression of PPARs may be due to increased oxidative stress with age, and that CR prevents these decreases through its antioxidative action...
An overview of the effect of linoleic and conjugated-linoleic acids on the growth of several human tumor cell linesMarina Maggiora
Dipartimento di Medicina e Oncologia Sperimentale, , Torino, Italy
Int J Cancer 112:909-19. 2004..In conclusion, CLA may be regarded as a component of the diet that exerts antineoplastic activity and its effect may be antiproliferative or pro-apoptotic...
Rosiglitazone induces interleukin-1 receptor antagonist in interleukin-1beta-stimulated rat synovial fibroblasts via a peroxisome proliferator-activated receptor beta/delta-dependent mechanismDavid Moulin
UMR 7561 CNRS Université Henri Poincaré Nancy 1, Vandoeuvre les Nancy, France
Arthritis Rheum 52:759-69. 2005....
Effects of cold stress on the messenger ribonucleic acid levels of peroxisome proliferator-activated receptor-{gamma} in spleen, thymus, and bursa of Fabricius of chickensJ T Wang
College of Veterinary Medicine, Northeast Agricultural University, Harbin 150030, P R China
Poult Sci 88:2549-54. 2009..The magnitude and direction of change in PPAR-gamma gene expression differs with the type of cold stress applied and also varies by tissue...
[Effect of peroxisome proliferators activated receptor gamma and its ligand on airway mucus hypersecretion in rats]Wei Jia Liu
Department of Respiratory Medicine, Sichuan University West China Hospital, Chengdu 610041, China
Zhonghua Jie He He Hu Xi Za Zhi 32:282-6. 2009..To explore the effect and the molecular mechanisms of peroxisome proliferators activated receptor gamma (PPAR-gamma) and its ligand on airway mucus hypersecretion...
Peroxisomal beta-oxidation and steatohepatitisM S Rao
Department of Pathology, Northwestern University Medical School, Chicago, Illinois, USA
Semin Liver Dis 21:43-55. 2001....
Peroxisome proliferator-activated receptors, coactivators, and downstream targetsC Qi
Department of Pathology, Northwestern University Medical School, Chicago, Illinois 60611, USA
Cell Biochem Biophys 32:187-204. 2000....
Relationship between different stages of the corpus luteum and the expression of the peroxisome proliferator-activated receptor gamma protein in bovine large lutein cellsT Viergutz
Research Institute for the Biology of Farm Animals, Dummerstorf, Germany
J Reprod Fertil 118:153-61. 2000....
Modulation of peroxisome proliferator-activated receptors (PPARs) by PPAR(alpha)- and PPAR(gamma)-specific ligands and by 17beta-estradiol in isolated zebrafish hepatocytesA Ibabe
Biologia Zelularra eta Histologia Laborategia, Zoologia eta Animali Biologia Zelularra Saila, Zientzia eta Teknologia Fakultatea, Euskal Herriko Unibertsitatea Universidad del País Vasco, 644 PK, Bilbao E 48080, Basque Country, Spain
Toxicol In Vitro 19:725-35. 2005..Further studies are needed to identify how the expression of different PPAR subtypes is regulated and to elucidate the implication of PPAR subtypes in zebrafish cell functions...
Regulation of the peroxisomal beta-oxidation-dependent pathway by peroxisome proliferator-activated receptor alpha and kinasesN Latruffe
LBMC, University of Burgundy, 21000 Dijon, France
Biochem Pharmacol 60:1027-32. 2000..Eur J Biochem 230:316-321, 1995). From all these findings, PPAR alpha and kinases appear to play an important role in lipid homeostasis...
Potent and selective PPAR-alpha agonist LY518674 upregulates both ApoA-I production and catabolism in human subjects with the metabolic syndromeJohn S Millar
Departments of Pharmacology, University of Pennsylvania, 652 BRB II III, 421 Curie Blvd, Philadelphia, PA 19104, USA
Arterioscler Thromb Vasc Biol 29:140-6. 2009..We sought to determine the effect of a potent and highly specific PPAR-alpha agonist, LY518674, on apoA-I, apoA-II, and apoB-100 kinetics in humans with metabolic syndrome and low levels of HDL cholesterol (C)...
Physiological difference between obese (fa/fa) Zucker rats and lean Zucker rats concerning adiponectinFumiki Oana
Division of Discovery Research, Kissei Pharmaceutical Co Ltd, 4365 1, Hotaka, Nagano 399 8304, Japan
Metabolism 54:995-1001. 2005....
Differential gene regulation in human versus rodent hepatocytes by peroxisome proliferator-activated receptor (PPAR) alpha. PPAR alpha fails to induce peroxisome proliferation-associated genes in human cells independently of the level of receptor expressoJ W Lawrence
Department of Safety Assessment, Merck Research Laboratories, Merck and Co, Inc, West Point, Pennsylvania 19486, USA
J Biol Chem 276:31521-7. 2001..These results suggest that other factors besides PPAR alpha levels determine the species-specific response of human and rat hepatocytes to the induction of PP...
Regulation of PPAR gamma gene expression by nutrition and obesity in rodentsA Vidal-Puig
Department of Medicine, Beth Israel Hospital, Boston, Massachusetts 02215, USA
J Clin Invest 97:2553-61. 1996..These findings demonstrate in vivo modulation of PPAR gamma mRNA levels over a fourfold range and provide an additional level of regulation for the control of adipocyte development and function...
Peroxisome proliferator-activated receptors gamma and alpha mediate in vivo regulation of uncoupling protein (UCP-1, UCP-2, UCP-3) gene expressionL J Kelly
Department of Molecular Endocrinology, Merck Research Laboratories, Rahway, New Jersey 07065, USA
Endocrinology 139:4920-7. 1998..PPAR alpha activation in mice is sufficient to induce liver UCP-2 expression...
Research Grants
- Limiting Inflammation in the CF LungPamela Davis; Fiscal Year: 2007..The name of the principal investigator/program director must be provided at the top of each printed page and each continuation page. RESEARCH GRANT TABLE OF CONTENTS PageNumbers Face Page ' Description, ..
- Beta-cell Compensation in Partial Pancreatectomy MiceJOHN L LEAHY; Fiscal Year: 2010....
- Molecular targeting of PPAR-delta in colon cancerImad Shureiqi; Fiscal Year: 2010..This improved understanding is expected to help determine whether PPAR-d would be a suitable molecular target for development of new drugs to treat colon cancer. ..
- 15-LOX-1 effects on colitis and colon cancerImad Shureiqi; Fiscal Year: 2009..This improved understanding is expected to facilitate the identification of molecular targets for new strategies for colon cancer prevention. ..
- 15-LOX-1 effects on colitis and colon cancerImad Shureiqi; Fiscal Year: 2010..This improved understanding is expected to facilitate the identification of molecular targets for new strategies for colon cancer prevention. ..
- MOLECULAR BASIS OF HIV LIPODYSTROPHY: ROLE OF VPRAshok Balasubramanyam; Fiscal Year: 2003....
- ROLE OF PPAR GAMMA IN LUPUS NEPHRITISGary Gilkeson; Fiscal Year: 2005..As agonists of PPAR gamma (the thiazolidinediones) are already approved for human use, insight gained from these studies can be quickly translated into human trials. ..
- PPAR-gamma Signaling in Normal Pilosebaceous Units and in Scarring AlopeciaPratima Karnik; Fiscal Year: 2010..PHS 398/2590 (Rev. 11/07) Page Continuation Format Page ..
- Transcriptional Control of Macrophage in AtherogenesisAjay Chawla; Fiscal Year: 2010..activated macrophages in tissues is absolutely dependent on the transcriptional activity of Peroxisome Proliferator Activated Receptors gamma and delta (PPAR gamma and delta), providing a mechanistic basis for the protective ..
- Action of Anabolic Factors on Bone Formation in MiceMARJA MARIE HURLEY; Fiscal Year: 2010....
- Action of Anabolic Factors on Bone Formation in MiceMarja Hurley; Fiscal Year: 2009....
- Role of PPARbeta in colon carcinogenesisJeffrey Peters; Fiscal Year: 2007..abstract_text> ..
- Cardiac metabolism and heart failureRong Tian; Fiscal Year: 2009..Results from the study will provide a basis for optimizing cardiac metabolism as part of the treatment strategy for heart failure. This is particularly important for patients with metabolic disorders such as obesity or diabetes. ..
- Pathophysiology of PPARgamma in the lungHong Du; Fiscal Year: 2009..These studies will provide new approaches to design strategies and discover drugs to combat emphysema and COPD. ..
- Pathophysiology of PPARgamma in the lungHong Du; Fiscal Year: 2010..These studies will provide new approaches to design strategies and discover drugs to combat emphysema and COPD. ..
- Pathophysiology of PPARgamma in the lungHong Du; Fiscal Year: 2010..These studies will provide new approaches to design strategies and discover drugs to combat emphysema and COPD. ..
- The function(s) and regulation of PPARs in the ovaryCarolyn Komar; Fiscal Year: 2003....
- Pparg In Macrophage Promote Hematoma Absorption After Intracerebral HemorrhageXiurong Zhao; Fiscal Year: 2007..Our long-term goal is to identify the molecular mechanism of PPAR? in phagocytosis/hematoma resolution and neuroprotection after ICH for future evaluation as a potential therapeutic target. ..
- Transcriptional Repression of PPARgamma-2 by Glucocorticoid-Induced Leucine ZippeXing Ming Shi; Fiscal Year: 2010..Thus, understanding how PPAR(2 can be negatively regulated, a focus of this study, may lead to new therapies for treating osteoporosis and obesity. ..
- Transcriptional Repression of PPARgamma-2 by Glucocorticoid-Induced Leucine ZippeXingming Shi; Fiscal Year: 2009..Thus, understanding how PPAR(2 can be negatively regulated, a focus of this study, may lead to new therapies for treating osteoporosis and obesity. ..
- Transcriptional Repression of PPARgamma-2 by Glucocorticoid-Induced Leucine ZippeXing Ming Shi; Fiscal Year: 2010..Thus, understanding how PPAR(2 can be negatively regulated, a focus of this study, may lead to new therapies for treating osteoporosis and obesity. ..
- PEROXISOME PROLIFERATORS AND THE CELL CYCLEJANE ISHMAEL; Fiscal Year: 2002..In general it is hoped that these studies will increase our understanding of the relationship between cell proliferation and hepatocarcinogenesis induced by nongenotoxic carcinogens. ..
- Role of PPAR-gamma Isoforms in Regulation of Macrophage apoE & LPL ExpressionJheem Medh; Fiscal Year: 2006..Information about ligand specificities of individual PPAR-g protein isoforms and their specific gene targets will allow for the selective induction of desirable genes and repression of harmful ones. ..
- Association of PPAR gamma ligands & colonic neoplasiaJames Lewis; Fiscal Year: 2006..Our results will allow us to translate the existing in vitro and in vivo observations to the intact human colon and could lead to further chemoprevention strategies. ..
- GLUCOSE UTILIZATION IN HYPERTROPHIED AND FAILING HEARTSRong Tian; Fiscal Year: 2007..3) increasing glucose transport in failing hearts improves energy supply and contractile performance. 4) increasing glucose transport enhances the efficacy of SERCA2a overexpression in the treatment of heart failure. ..
- The PPAR-delta pathway in neural function and Hungtington's disease neuropathologAlbert R La Spada; Fiscal Year: 2010....
- Cellular Selenium Status and PGJ2 MetabolismKUMBLE SANDEEP PRABHU; Fiscal Year: 2009....
- H.Pylori Relationship to Digestive Diseases and CancerRichard Peek; Fiscal Year: 2007..pylori-induced carcinogenesis and facilitate identification of potential therapeutic targets, but may also provide insights into other malignancies that arise within the context of inflammatory states. ..
- 5-LOX-1 and Clinical Chemoprevention of Colon TumorsImad Shureiqi; Fiscal Year: 2007..If our hypothesis is confirmed, efforts can be directed to develop chemopreventive interventions that specifically target the GATA-6 and 15-LOX-1 signaling pathway. ..
- Chemoprevention of Pituitary Corticotroph TumorsAnthony Heaney; Fiscal Year: 2006..Our ultimate goal is to develop a rationale for clinical application of these PPAR-gamma ligands as a novel medical therapy in Cushing's disease. ..
- Gene expression and anemia of chronic renal failureSaul Nurko; Fiscal Year: 2007..abstract_text> ..
- Structural and functional studies of the nuclear receptor PPARgammaH Eric Xu; Fiscal Year: 2007....
- Elucidation of injury pathways in alcoholic liver disease and development of prevAlbert J Fornace; Fiscal Year: 2010..Results will improve approaches to prevent or treat alcoholic liver disease with a solid mechanistic rationale. ..
- Structural and functional studies of the nuclear receptor PPARgammaH Eric Xu; Fiscal Year: 2009....
- Structural and functional studies of the nuclear receptor PPARgammaH Eric Xu; Fiscal Year: 2010....
- The impact of PPAR-gamma and estrogen receptor crosstalk on insulin actionAndrea Hevener; Fiscal Year: 2007..Additionally our goal is to elucidate the importance of nuclear receptor crosstalk in the regulation of gene transcription and show that aberrant crosstalk is an underlying mechanism of insulin resistance and obesity. ..
- Programmed Adipogenesis and Lipid DysregulationMina Desai; Fiscal Year: 2010..As increased body fat is one of the key features of obesity, the proposed studies will investigate the mechanism in which fat signaling factors are altered. ..
