ERRα: a metabolic function for the oldest orphan

Mangelsdorf, 1995, The nuclear receptor superfamily: the second decade, Cell, 83, 835, 10.1016/0092-8674(95)90199-X O’Malley, 1990, The steroid receptor superfamily: more excitement predicted for the future, Mol. Endocrinol., 4, 363, 10.1210/mend-4-3-363 Giguere, 1988, Identification of a new class of steroid hormone receptors, Nature, 331, 91, 10.1038/331091a0 Kliewer, 1999, Orphan nuclear receptors: shifting endocrinology into reverse, Science, 284, 757, 10.1126/science.284.5415.757 Chawla, 2001, Nuclear receptors and lipid physiology: opening the X-files, Science, 294, 1866, 10.1126/science.294.5548.1866 Giguere, 2002, To ERR in the estrogen pathway, Trends Endocrinol. Metab., 13, 220, 10.1016/S1043-2760(02)00592-1 Bonnelye, 2005, Estrogen receptor-related receptor alpha: a mediator of estrogen response in bone, J. Clin. Endocrinol. Metab., 90, 3115, 10.1210/jc.2004-2168 Bardet, 2006, Studying non-mammalian models? Not a fool's ERRand!, Trends Endocrinol. Metab., 17, 166, 10.1016/j.tem.2006.03.005 Ariazi, 2006, Estrogen-related receptors as emerging targets in cancer and metabolic disorders, Curr. Top. Med. Chem., 6, 203, 10.2174/156802606776173483 Stein, 2006, Estrogen-related receptor alpha as a therapeutic target in cancer, Endocr. Relat. Cancer, 13, S25, 10.1677/erc.1.01292 Greschik, 2002, Structural and functional evidence for ligand-independent transcriptional activation by the estrogen-related receptor 3, Mol. Cell, 9, 303, 10.1016/S1097-2765(02)00444-6 Horard, 2003, Estrogen receptor-related receptors: orphan receptors desperately seeking a ligand, J. Mol. Endocrinol., 31, 349, 10.1677/jme.0.0310349 Kallen, 2004, Evidence for ligand-independent transcriptional activation of the human estrogen-related receptor alpha (ERRalpha): crystal structure of ERRalpha ligand binding domain in complex with peroxisome proliferator-activated receptor coactivator-1alpha, J. Biol. Chem., 279, 49330, 10.1074/jbc.M407999200 Busch, 2004, Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha, J. Med. Chem., 47, 5593, 10.1021/jm049334f Willy, 2004, Regulation of PPARgamma coactivator 1alpha (PGC-1alpha) signaling by an estrogen-related receptor alpha (ERRalpha) ligand, Proc. Natl. Acad. Sci. U. S. A., 101, 8912, 10.1073/pnas.0401420101 Hyatt, 2007, On the intractability of estrogen-related receptor alpha as a target for activation by small molecules, J. Med. Chem., 50, 6722, 10.1021/jm7012387 Kallen, 2007, Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism, J. Biol. Chem., 282, 23231, 10.1074/jbc.M703337200 Finck, 2006, PGC-1 coactivators: inducible regulators of energy metabolism in health and disease, J. Clin. Invest., 116, 615, 10.1172/JCI27794 Handschin, 2006, Peroxisome proliferator-activated receptor gamma coactivator 1 coactivators, energy homeostasis, and metabolism, Endocr. Rev., 27, 728, 10.1210/er.2006-0037 Vega, 2000, The coactivator PGC-1 cooperates with peroxisome proliferator-activated receptor alpha in transcriptional control of nuclear genes encoding mitochondrial fatty acid oxidation enzymes, Mol. Cell. Biol., 20, 1868, 10.1128/MCB.20.5.1868-1876.2000 Tcherepanova, 2000, Modulation of estrogen receptor-alpha transcriptional activity by the coactivator PGC-1, J. Biol. Chem., 275, 16302, 10.1074/jbc.M001364200 Knutti, 2001, Regulation of the transcriptional coactivator PGC-1 via MAPK-sensitive interaction with a repressor, Proc. Natl. Acad. Sci. U. S. A., 98, 9713, 10.1073/pnas.171184698 Huss, 2002, Peroxisome proliferator-activated receptor coactivator-1alpha (PGC-1alpha) coactivates the cardiac-enriched nuclear receptors estrogen-related receptor-alpha and -gamma. Identification of novel leucine-rich interaction motif within PGC-1alpha, J. Biol. Chem., 277, 40265, 10.1074/jbc.M206324200 Schreiber, 2003, The transcriptional coactivator PGC-1 regulates the expression and activity of the orphan nuclear receptor estrogen-related receptor alpha (ERRalpha), J. Biol. Chem., 278, 9013, 10.1074/jbc.M212923200 Gaillard, 2007, Definition of the molecular basis for estrogen receptor-related receptor-alpha-cofactor interactions, Mol. Endocrinol., 21, 62, 10.1210/me.2006-0179 Schreiber, 2004, The estrogen-related receptor alpha (ERRalpha) functions in PPARgamma coactivator 1alpha (PGC-1alpha)-induced mitochondrial biogenesis, Proc. Natl. Acad. Sci. U. S. A., 101, 6472, 10.1073/pnas.0308686101 Kamei, 2003, PPARgamma coactivator 1beta/ERR ligand 1 is an ERR protein ligand, whose expression induces a high-energy expenditure and antagonizes obesity, Proc. Natl. Acad. Sci. U. S. A., 100, 12378, 10.1073/pnas.2135217100 Laganiere, 2004, A polymorphic autoregulatory hormone response element in the human estrogen-related receptor alpha (ERRalpha) promoter dictates peroxisome proliferator-activated receptor gamma coactivator-1alpha control of ERRalpha expression, J. Biol. Chem., 279, 18504, 10.1074/jbc.M313543200 Mootha, 2004, Erralpha and Gabpa/b specify PGC-1alpha-dependent oxidative phosphorylation gene expression that is altered in diabetic muscle, Proc. Natl. Acad. Sci. U. S. A., 101, 6570, 10.1073/pnas.0401401101 Liu, 2005, Estrogen-related receptor-gamma and peroxisome proliferator-activated receptor-gamma coactivator-1alpha regulate estrogen-related receptor-alpha gene expression via a conserved multi-hormone response element, J. Mol. Endocrinol., 34, 473, 10.1677/jme.1.01586 Sladek, 1997, The orphan nuclear receptor estrogen-related receptor alpha is a transcriptional regulator of the human medium-chain acyl coenzyme A dehydrogenase gene, Mol. Cell. Biol., 17, 5400, 10.1128/MCB.17.9.5400 Vega, 1997, A role for estrogen-related receptor alpha in the control of mitochondrial fatty acid beta-oxidation during brown adipocyte differentiation, J. Biol. Chem., 272, 31693, 10.1074/jbc.272.50.31693 Kressler, 2002, The PGC-1-related protein PERC is a selective coactivator of estrogen receptor alpha, J. Biol. Chem., 277, 13918, 10.1074/jbc.M201134200 Ichida, 2002, Identification of a specific molecular repressor of the peroxisome proliferator-activated receptor gamma Coactivator-1 alpha (PGC-1alpha), J. Biol. Chem., 277, 50991, 10.1074/jbc.M210262200 Cartoni, 2005, Mitofusins 1/2 and ERRalpha expression are increased in human skeletal muscle after physical exercise, J. Physiol., 567, 349, 10.1113/jphysiol.2005.092031 Barry, 2005, Epidermal growth factor-induced signaling in breast cancer cells results in selective target gene activation by orphan nuclear receptor estrogen-related receptor alpha, Cancer Res., 65, 6120, 10.1158/0008-5472.CAN-05-0922 Ariazi, 2007, Estrogen-related receptor alpha1 transcriptional activities are regulated in part via the ErbB2/HER2 signaling pathway, Mol. Cancer Res., 5, 71, 10.1158/1541-7786.MCR-06-0227 Vu, 2007, Phosphorylation-dependent sumoylation of estrogen-related receptor alpha1, Biochemistry, 46, 9795, 10.1021/bi700316g Tremblay, 2008, Phosphorylation-Dependent Sumoylation Regulates Estrogen-Related Receptor-{alpha} and -{gamma} Transcriptional Activity through a Synergy Control Motif, Mol. Endocrinol., 22, 570, 10.1210/me.2007-0357 Castet, 2006, Receptor-interacting protein 140 differentially regulates estrogen receptor-related receptor transactivation depending on target genes, Mol. Endocrinol., 20, 1035, 10.1210/me.2005-0227 Gaillard, 2006, Receptor-selective coactivators as tools to define the biology of specific receptor-coactivator pairs, Mol. Cell, 24, 797, 10.1016/j.molcel.2006.10.012 Huss, 2004, Estrogen-related receptor alpha directs peroxisome proliferator-activated receptor alpha signaling in the transcriptional control of energy metabolism in cardiac and skeletal muscle, Mol. Cell. Biol., 24, 9079, 10.1128/MCB.24.20.9079-9091.2004 Carrier, 2004, Estrogen-related receptor alpha (ERRalpha) is a transcriptional regulator of apolipoprotein A-IV and controls lipid handling in the intestine, J. Biol. Chem., 279, 52052, 10.1074/jbc.M410337200 Villena, 2007, Orphan nuclear receptor estrogen-related receptor alpha is essential for adaptive thermogenesis, Proc. Natl. Acad. Sci. U. S. A., 104, 1418, 10.1073/pnas.0607696104 Rangwala, 2007, Estrogen-related receptor alpha is essential for the expression of antioxidant protection genes and mitochondrial function, Biochem. Biophys. Res. Commun., 357, 231, 10.1016/j.bbrc.2007.03.126 Sonoda, 2007, Nuclear receptor ERR alpha and coactivator PGC-1 beta are effectors of IFN-gamma-induced host defense, Genes Dev., 21, 1909, 10.1101/gad.1553007 Soriano, 2006, Evidence for a mitochondrial regulatory pathway defined by peroxisome proliferator-activated receptor-gamma coactivator-1 alpha, estrogen-related receptor-alpha, and mitofusin 2, Diabetes, 55, 1783, 10.2337/db05-0509 Wende, 2005, PGC-1alpha coactivates PDK4 gene expression via the orphan nuclear receptor ERRalpha: a mechanism for transcriptional control of muscle glucose metabolism, Mol. Cell. Biol., 25, 10684, 10.1128/MCB.25.24.10684-10694.2005 Dufour, 2007, Genome-wide orchestration of cardiac functions by the orphan nuclear receptors ERRalpha and gamma, Cell Metab., 5, 345, 10.1016/j.cmet.2007.03.007 Araki, 2006, Identification of ERRalpha as a specific partner of PGC-1alpha for the activation of PDK4 gene expression in muscle, FEBS J., 273, 1669, 10.1111/j.1742-4658.2006.05183.x Zhang, 2006, Estrogen-related receptors stimulate pyruvate dehydrogenase kinase isoform 4 gene expression, J. Biol. Chem., 281, 39897, 10.1074/jbc.M608657200 Huss, 2007, The nuclear receptor ERRalpha is required for the bioenergetic and functional adaptation to cardiac pressure overload, Cell Metab., 6, 25, 10.1016/j.cmet.2007.06.005 Johnston, 1997, Estrogen-related receptor alpha 1 functionally binds as a monomer to extended half-site sequences including ones contained within estrogen-response elements, Mol. Endocrinol., 11, 342, 10.1210/me.11.3.342 Powelka, 2006, Suppression of oxidative metabolism and mitochondrial biogenesis by the transcriptional corepressor RIP140 in mouse adipocytes, J. Clin. Invest., 116, 125, 10.1172/JCI26040 Christian, 2006, Metabolic regulation by the nuclear receptor corepressor RIP140, Trends Endocrinol. Metab., 17, 243, 10.1016/j.tem.2006.06.008 Herzog, 2006, Estrogen-related receptor alpha is a repressor of phosphoenolpyruvate carboxykinase gene transcription, J. Biol. Chem., 281, 99, 10.1074/jbc.M509276200 Barry, 2006, A single nucleotide in an estrogen-related receptor alpha site can dictate mode of binding and peroxisome proliferator-activated receptor gamma coactivator 1alpha activation of target promoters, Mol. Endocrinol., 20, 302, 10.1210/me.2005-0313 Luo, 2003, Reduced fat mass in mice lacking orphan nuclear receptor estrogen-related receptor alpha, Mol. Cell. Biol., 23, 7947, 10.1128/MCB.23.22.7947-7956.2003 Kelly, 2004, Transcriptional regulatory circuits controlling mitochondrial biogenesis and function, Genes Dev., 18, 357, 10.1101/gad.1177604 Ijichi, 2007, Estrogen-related receptor alpha modulates the expression of adipogenesis-related genes during adipocyte differentiation, Biochem. Biophys. Res. Commun., 358, 813, 10.1016/j.bbrc.2007.04.209 Mootha, 2003, PGC-1alpha-responsive genes involved in oxidative phosphorylation are coordinately downregulated in human diabetes, Nat. Genet., 34, 267, 10.1038/ng1180 Patti, 2003, Coordinated reduction of genes of oxidative metabolism in humans with insulin resistance and diabetes: Potential role of PGC1 and NRF1, Proc. Natl. Acad. Sci. U. S. A., 100, 8466, 10.1073/pnas.1032913100 Chan, 2006, Mitochondria: dynamic organelles in disease, aging, and development, Cell, 125, 1241, 10.1016/j.cell.2006.06.010 Lin, 2006, Mitochondrial dysfunction and oxidative stress in neurodegenerative diseases, Nature, 443, 787, 10.1038/nature05292 McGill, 2006, PGC-1alpha, a new therapeutic target in Huntington's disease?, Cell, 127, 465, 10.1016/j.cell.2006.10.023 Nichol, 2006, RIP140 expression is stimulated by estrogen-related receptor alpha during adipogenesis, J. Biol. Chem., 281, 32140, 10.1074/jbc.M604803200