Estrogen receptors, PPARs, and liver X receptors are members of the nuclear receptor superfamily of ligand-dependent transcription factors that regulate diverse aspects of development and homeostasis. Recent studies of the biologic roles of these receptors and their mechanisms of action have significantly advanced our understanding of transcriptional programs that control lipid and carbohydrate metabolism, immunity and inflammation, and wound repair. These findings provide insights into the therapeutic actions of existing drugs that target nuclear receptors and raise new possibilities for development of safer, more effective drugs for the prevention and treatment of metabolic and cardiovascular diseases. In this introduction to this Review series, underlying mechanisms that enable nuclear receptors to positively and negatively regulate gene expression are presented as background to the focused reviews on estrogen receptors, PPARs, liver X receptors, and the PPARγ coactivator-1 (PGC-1) family of coactivators.
Christopher K. Glass
Title and authors | Publication | Year |
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Regulation of Epigenetic Modifications in the Placenta during Preeclampsia: PPARγ Influences H3K4me3 and H3K9ac in Extravillous Trophoblast Cells
S Meister, L Hahn, S Beyer, C Paul, S Mitter, C Kuhn, V von Schönfeldt, S Corradini, K Sudan, C Schulz, TM Kolben, S Mahner, U Jeschke, T Kolben |
International journal of molecular sciences | 2021 |
Myeloid-specific deficiency of pregnane X receptor decreases atherosclerosis in LDL receptor-deficient mice
Y Sui, Z Meng, SH Park, W Lu, C Livelo, Q Chen, T Zhou, C Zhou |
Journal of lipid research | 2020 |
Angiotensin II type 2 receptor stimulation with compound 21 improves neurological function after stroke in female rats: a pilot study
W Eldahshan, T Ishrat, B Pillai, MA Sayed, A Alwhaibi, AY Fouda, A Ergul, SC Fagan |
American journal of physiology. Heart and circulatory physiology | 2019 |
Brain activity of anandamide: a rewarding bliss?
M Scherma, P Masia, V Satta, W Fratta, P Fadda, G Tanda |
Acta Pharmacologica Sinica | 2018 |
Statins Attenuate Activation of the NLRP3 Inflammasome by Oxidized LDL or TNF α in Vascular Endothelial Cells through a PXR-Dependent Mechanism
S Wang, X Xie, T Lei, K Zhang, B Lai, Z Zhang, Y Guan, G Mao, L Xiao, N Wang |
Molecular pharmacology | 2017 |
PPARβ/δ and lipid metabolism in the heart
X Palomer, E Barroso, M Zarei, G Botteri, M Vázquez-Carrera |
Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids | 2016 |
Nuclear Receptors in Vascular Biology
D Bishop-Bailey |
Current Atherosclerosis Reports | 2015 |
Bioactive quinone derivatives from the marine brown alga Sargassum thunbergii induce anti-adipogenic and pro-osteoblastogenic activities: Bioactive quinones from Sargassum thunbergii
JA Kim, F Karadeniz, BN Ahn, MS Kwon, OJ Mun, MJ Bae, Y Seo, M Kim, SH Lee, YY Kim, J Mi-Soon, CS Kong |
Journal of the Science of Food and Agriculture | 2015 |
Preventing male infertility by marjoram and sage essential oils through modulating testicular lipid accumulation and androgens biosynthesis disruption in a rat model of dietary obesity
AM El-Wakf, ES Elhabibi, EA El-Ghany |
Egyptian Journal of Basic and Applied Sciences | 2015 |
Prenatal Hypoxia Reduces Mitochondrial Protein Levels and Cytochrome c Oxidase Activity in Offspring Guinea Pig Hearts
YM Al-Hasan, GA Pinkas, LP Thompson |
Reproductive sciences (Thousand Oaks, Calif.) | 2014 |
Role of human pregnane X receptor in high fat diet-induced obesity in pre-menopausal female mice
K Spruiell, DZ Jones, JM Cullen, EM Awumey, FJ Gonzalez, MA Gyamfi |
Biochemical Pharmacology | 2014 |
Inhibition of FAAH and activation of PPAR: New approaches to the treatment of cognitive dysfunction and drug addiction
LV Panlilio, Z Justinova, SR Goldberg |
Pharmacology & Therapeutics | 2013 |
Soluble soy protein peptic hydrolysate stimulates adipocyte differentiation in 3T3-L1 cells
T Goto, A Mori, S Nagaoka |
Molecular Nutrition & Food Research | 2013 |
The G32E functional variant reduces activity of PPARD by nuclear export and post-translational modification in pigs
Y Duan, B Brenig, X Wu, J Ren, L Huang |
PloS one | 2013 |
The G32E Functional Variant Reduces Activity of PPARD by Nuclear Export and Post-Translational Modification in Pigs
Y Duan, B Brenig, X Wu, J Ren, L Huang, MF Pas |
PloS one | 2013 |
Integrative Biology of Women’s Health
EE Spangenburg |
2013 | |
Sex and Gender Differences in Pharmacology
V Regitz-Zagrosek |
2012 | |
Sex and Gender Differences in Pharmacology
V Regitz-Zagrosek |
2012 | |
Sex and Gender Differences in Pharmacology
V Regitz-Zagrosek |
2012 | |
Sex and Gender Differences in Pharmacology
V Regitz-Zagrosek |
2012 | |
Sex and Gender Differences in Pharmacology
V Regitz-Zagrosek |
2012 | |
Sex and Gender Differences in Pharmacology
V Regitz-Zagrosek |
2012 | |
Sex and Gender Differences in Pharmacology
V Regitz-Zagrosek |
2012 | |
Synthetic oleanane triterpenoids: multifunctional drugs with a broad range of applications for prevention and treatment of chronic disease
KT Liby, MB Sporn |
Pharmacological reviews | 2012 |
Selected Extracts of Chinese Herbal Medicines: Their Effect on NF-κB, PPARα and PPARγ and the Respective Bioactive Compounds
E Rozema, AG Atanasov, N Fakhrudin, J Singhuber, U Namduang, EH Heiss, G Reznicek, CW Huck, GK Bonn, VM Dirsch, B Kopp |
Evidence-based complementary and alternative medicine : eCAM | 2012 |
Natural compounds regulate energy metabolism by the modulating the activity of lipid-sensing nuclear receptors
T Goto, YI Kim, N Takahashi, T Kawada |
Molecular Nutrition & Food Research | 2012 |
Suppression of ERR targets by a PPARα/Sirt1 complex in the failing heart
S Oka, P Zhai, R Alcendor, JY Park, B Tian, J Sadoshima |
Cell cycle (Georgetown, Tex.) | 2012 |
Repeated abortion affects subsequent pregnancy outcomes in BALB/c mice
F Lv, X Xu, S Zhang, L Wang, N Wang, B He, J Wang |
PloS one | 2012 |
Repeated Abortion Affects Subsequent Pregnancy Outcomes in BALB/c Mice
F Lv, X Xu, S Zhang, L Wang, N Wang, B He, J Wang, GE Woloschak |
PloS one | 2012 |
Endocannabinoids and the cardiovascular response to stress
SE OSullivan, PJ Kendall, DA Kendall |
Journal of Psychopharmacology (Oxford, England) | 2012 |
endoCANNABINOIDS
ME Abood, RG Sorensen, N Stella |
2012 | |
Synthetic Oleanane Triterpenoids: Multifunctional Drugs with a Broad Range of Applications for Prevention and Treatment of Chronic Disease
KT Liby, MB Sporn, TA Esbenshade |
Pharmacological reviews | 2012 |
Deficiency of PXR decreases atherosclerosis in apoE-deficient mice[S]
Y Sui, J Xu, J Rios-Pilier, C Zhou |
Journal of lipid research | 2011 |
Farnesyl pyrophosphate regulates adipocyte functions as an endogenous PPARγ agonist
T Goto, H Nagai, K Egawa, YI Kim, S Kato, A Taimatsu, T Sakamoto, S Ebisu, T Hohsaka, H Miyagawa, S Murakami, N Takahashi, T Kawada |
Biochemical Journal | 2011 |
PPARα-Sirt1 Complex Mediates Cardiac Hypertrophy and Failure through Suppression of the ERR Transcriptional Pathway
S Oka, R Alcendor, P Zhai, JY Park, D Shao, J Cho, T Yamamoto, B Tian, J Sadoshima |
Cell Metabolism | 2011 |
17β-Estradiol inhibition of PPARγ-induced adipogenesis and adipocyte-specific gene expression
S Jeong, M Yoon |
Acta Pharmacologica Sinica | 2011 |
Effect of tocopherol supplementation on serum 8-epi-prostaglandin F2 alpha and adiponectin concentrations, and mRNA expression of PPARγ and related genes in ovine placenta and uterus
RK Kasimanickam, VR Kasimanickam |
Theriogenology | 2011 |
Transcriptional control of metabolic and inflammatory pathways by nuclear receptor SUMOylation
E Treuter, N Venteclef |
Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease | 2011 |
Structural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor α/δ Agonist*
L Jin, S Lin, H Rong, S Zheng, S Jin, R Wang, Y Li |
The Journal of biological chemistry | 2011 |
Altered mitochondrial apoptotic pathway in placentas from undernourished rat gestations
L Belkacemi, M Desai, DM Nelson, MG Ross |
American Journal of Physiology - Regulatory, Integrative and Comparative Physiology | 2011 |
Deficiency of PXR decreases atherosclerosis in apoE-deficient mice
Y Sui, J Xu, J Rios-Pilier, C Zhou |
Journal of lipid research | 2011 |
Structural Basis for Iloprost as a Dual Peroxisome Proliferator-activated Receptor α/δ Agonist
L Jin, S Lin, H Rong, S Zheng, S Jin, R Wang, Y Li |
The Journal of biological chemistry | 2011 |
Farnesol, an isoprenoid, improves metabolic abnormalities in mice via both PPARα-dependent and -independent pathways
T Goto, YI Kim, K Funakoshi, A Teraminami, T Uemura, S Hirai, JY Lee, M Makishima, R Nakata, H Inoue, H Senju, M Matsunaga, F Horio, N Takahashi, T Kawada |
American journal of physiology. Endocrinology and metabolism | 2011 |
Altered mitochondrial apoptotic pathway in placentas from undernourished rat gestations
L Belkacemi, M Desai, DM Nelson, MG Ross |
American Journal of Physiology - Regulatory, Integrative and Comparative Physiology | 2011 |
Bioinformatic Analysis of Gene Sets Regulated by Ligand-Activated and Dominant-Negative Peroxisome Proliferator–Activated Receptor γ in Mouse Aorta
HL Keen, CM Halabi, AM Beyer, WJ de Lange, X Liu, N Maeda, FM Faraci, TL Casavant, CD Sigmund |
Arteriosclerosis, thrombosis, and vascular biology | 2010 |
17β-Estradiol inhibits oleic acid-induced rat VSMC Proliferation and migration by restoring PGC-1α expression
X Jiang, Y Zhang, D Hou, L Zhu, W Xu, L Ding, X Qi, G Sun, C Liu, J Zhang, K Zen, Y Xiang, CY Zhang |
Molecular and Cellular Endocrinology | 2010 |
PPARα in Obesity: Sex Difference and Estrogen Involvement
M Yoon |
PPAR Research | 2010 |
Various Terpenoids Derived from Herbal and Dietary Plants Function as PPAR Modulators and Regulate Carbohydrate and Lipid Metabolism
T Goto, N Takahashi, S Hirai, T Kawada |
PPAR Research | 2010 |
Estrogen modulates transactivations of SXR-mediated liver X receptor response element and CAR-mediated phenobarbital response element in HepG2 cells
G Min |
Experimental & molecular medicine | 2010 |
Proton pump inhibitor lansoprazole is a nuclear liver X receptor agonist
AA Cronican, NF Fitz, T Pham, A Fogg, B Kifer, R Koldamova, I Lefterov |
Biochemical Pharmacology | 2010 |
Cannabinoid activation of peroxisome proliferator-activated receptors: Potential for modulation of inflammatory disease
SE O'Sullivan, DA Kendall |
Immunobiology | 2010 |
Mediator subunits: Gene expression pattern, a novel transcript identification and nuclear localization in human endothelial progenitor cells
M Rienzo, J Nagel, A Casamassimi, A Giovane, S Dietzel, C Napoli |
Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms | 2010 |
The effect of Telmisartan on collagen biosynthesis depends on the status of estrogen activation in breast cancer cells
B Kociecka, A Surazynski, W Miltyk, J Palka |
European Journal of Pharmacology | 2010 |
Resolvins, protectins and other lipid mediators in obesity-associated inflammatory disorders
J Clària, E Titos, C López-Vicario, A González-Périz |
Drug Discovery Today: Disease Mechanisms | 2010 |
Casein-kinase-II-dependent phosphorylation of PPARγ provokes CRM1-mediated shuttling of PPARγ from the nucleus to the cytosol
A von Knethen, N Tzieply, C Jennewein, B Brüne |
Journal of cell science | 2010 |
Activation of PXR induces hypercholesterolemia in wild-type and accelerates atherosclerosis in apoE deficient mice
C Zhou, N King, KY Chen, JL Breslow |
Journal of lipid research | 2009 |
Obesity-induced insulin resistance and hepatic steatosis are alleviated by ω-3 fatty acids: a role for resolvins and protectins
A González-Périz, R Horrillo, N Ferré, K Gronert, B Dong, E Morán-Salvador, E Titos, M Martínez-Clemente, M López-Parra, V Arroyo, J Clària |
The FASEB Journal | 2009 |
PPARgamma regulates trophoblast proliferation and promotes labyrinthine trilineage differentiation
MM Parast, H Yu, A Ciric, MW Salata, V Davis, DS Milstone |
PloS one | 2009 |
Negative feedback maintenance of heme homeostasis by its receptor, Rev-erbalpha
N Wu, L Yin, EA Hanniman, S Joshi, MA Lazar |
Genes & development | 2009 |
HO-1 Activation Can Attenuate Cardiomyocytic Apoptosis via Inhibition of NF-κB and AP-1 Translocation Following Cardiac Global Ischemia and Reperfusion
CH Yeh, TP Chen, YC Wang, YM Lin, PJ Lin |
Journal of Surgical Research | 2009 |
Activation of PXR induces hypercholesterolemia in wild-type and accelerates atherosclerosis in apoE deficient mice
C Zhou, N King, KY Chen, JL Breslow |
Journal of lipid research | 2009 |
The Peroxisome Proliferator-Activated Receptor γ Agonist Pioglitazone Improves Cardiometabolic Risk and Renal Inflammation in Murine Lupus
W Zhao, SG Thacker, JB Hodgin, H Zhang, JH Wang, JL Park, A Randolph, EC Somers, S Pennathur, M Kretzler, FC Brosius, MJ Kaplan |
Journal of immunology (Baltimore, Md. : 1950) | 2009 |
The Tangle of Nuclear Receptors that Controls Xenobiotic Metabolism and Transport: Crosstalk and Consequences
JM Pascussi, S Gerbal-Chaloin, C Duret, M Daujat-Chavanieu, MJ Vilarem, P Maurel |
Annual Review of Pharmacology and Toxicology | 2008 |
The PPARα/p16 INK4a Pathway Inhibits Vascular Smooth Muscle Cell Proliferation by Repressing Cell Cycle–Dependent Telomerase Activation
F Gizard, T Nomiyama, Y Zhao, HM Findeisen, EB Heywood, KL Jones, B Staels, D Bruemmer |
Circulation research | 2008 |
PPARgamma agonists as therapeutics for the treatment of Alzheimer's disease
G Landreth, Q Jiang, S Mandrekar, M Heneka |
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics | 2008 |
Statins Activate Human PPARalpha Promoter and Increase PPARalpha mRNA Expression and Activation in HepG2 Cells
M Seo, I Inoue, M Ikeda, T Nakano, S Takahashi, S Katayama, T Komoda |
PPAR Research | 2008 |
Metabolic actions of estrogen receptor beta (ERbeta) are mediated by a negative cross-talk with PPARgamma
A Foryst-Ludwig, M Clemenz, S Hohmann, M Hartge, C Sprang, N Frost, M Krikov, S Bhanot, R Barros, A Morani, JA Gustafsson, T Unger, U Kintscher |
PLoS genetics | 2008 |
A Role for the PPARgamma in Cancer Therapy
MJ Campbell, C Carlberg, HP Koeffler |
PPAR Research | 2008 |
Pharmacological Differences of Glitazones
U Kintscher |
Journal of the American College of Cardiology | 2008 |
Structural determination of estrogen-related receptor γ in the presence of phenol derivative compounds
MC Abad, H Askari, J O’Neill, AL Klinger, C Milligan, F Lewandowski, B Springer, J Spurlino, D Rentzeperis |
The Journal of Steroid Biochemistry and Molecular Biology | 2008 |
Cooperation of docosahexaenoic acid and vitamin E in the regulation of UDP-glucuronosyltransferase mRNA expression
M Caputo, D Eletto, G Torino, MF Tecce |
Journal of Cellular Physiology | 2008 |
Nuclear receptors and human disease: Resistance to thyroid hormone and lipodystrophic insulin resistance
VK Chatterjee |
Annales d'Endocrinologie | 2008 |
Metabolic Actions of Estrogen Receptor Beta (ERβ) are Mediated by a Negative Cross-Talk with PPARγ
A Foryst-Ludwig, M Clemenz, S Hohmann, M Hartge, C Sprang, N Frost, M Krikov, S Bhanot, R Barros, A Morani, JÅ Gustafsson, T Unger, U Kintscher, J Auwerx |
PLoS genetics | 2008 |
T2384, a Novel Antidiabetic Agent with Unique Peroxisome Proliferator-activated Receptor γ Binding Properties
Y Li, Z Wang, N Furukawa, P Escaron, J Weiszmann, G Lee, M Lindstrom, J Liu, X Liu, H Xu, O Plotnikova, V Prasad, N Walker, RM Learned, JL Chen |
The Journal of biological chemistry | 2008 |
In Vivo Activation of Peroxisome Proliferator-Activated Receptor-δ Protects the Heart from Ischemia/Reperfusion Injury in Zucker Fatty Rats
TL Yue, SS Nerurkar, W Bao, BM Jucker, L Sarov-Blat, K Steplewski, EH Ohlstein, RN Willette |
The Journal of pharmacology and experimental therapeutics | 2008 |
Alzheimer's Disease
LF Lau, MA Brodney |
Alzheimer's Disease | 2008 |
Orphan nuclear receptor estrogen-related receptor alpha is essential for adaptive thermogenesis
JA Villena, MB Hock, WY Chang, JE Barcas, V Giguère, A Kralli |
Proceedings of the National Academy of Sciences | 2007 |
Inflammation in Diabetes Mellitus: Role of Peroxisome Proliferator-Activated Receptor–α and Peroxisome Proliferator-Activated Receptor–γ Agonists
P Libby, J Plutzky |
The American Journal of Cardiology | 2007 |
Cannabinoids go nuclear: evidence for activation of peroxisome proliferator-activated receptors
SE O'Sullivan |
British Journal of Pharmacology | 2007 |
Therapeutic potential of retinoid x receptor modulators for the treatment of the metabolic syndrome
JA Pinaire, A Reifel-Miller |
PPAR Research | 2007 |
Resolving fibrosis in the diseased liver: Translating the scientific promise to the clinic
AK Muddu, IN Guha, AM Elsharkawy, DA Mann |
The International Journal of Biochemistry & Cell Biology | 2007 |
Mediator complexes and eukaryotic transcription regulation: An overview
A Casamassimi, C Napoli |
Biochimie | 2007 |
Role of signalling systems in the effects of dietary factors on the expression of mammalian CYPs
M Murray |
Expert Opinion on Drug Metabolism & Toxicology | 2007 |
Constitutive Coactivator of Peroxisome Proliferator-Activated Receptor (PPARγ), a Novel Coactivator of PPARγ that Promotes Adipogenesis
D Li, Q Kang, DM Wang |
Molecular Endocrinology | 2007 |
PGC-1alpha controls hepatitis B virus through nutritional signals
A Shlomai, N Paran, Y Shaul |
Proceedings of the National Academy of Sciences | 2006 |
Pharmacological Targeting of Adipocytes/Fat Metabolism for Treatment of Obesity and Diabetes
PF Pilch, N Bergenhem |
Molecular pharmacology | 2006 |
Cholesterol metabolism during cell growth: Which role for the plasma membrane?
B Batetta, F Sanna |
European Journal of Lipid Science and Technology | 2006 |
Grundlagen der Molekularen Medizin
D Ganten, K Ruckpaul |
2003 |