Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis

Diabetes

Volumn 62, Issue 9, 2013, Pages 3093-3102

  Kim, Don Kyu ^a   Gang, Gil Tae ^b   Ryu, Dongryeol ^c   Koh, Minseob ^d   Kim, Yo Na ^e   Kim, Su Sung ^e   Park, Jinyoung ^c   Kim, Yong Hoon ^b   Sim, Taebo ^f   Lee, In Kyu ^g   Choi, Cheol Soo ^e   Park, Seung Bum ^d   Lee, Chul Ho ^b   Koo, Seung Hoi ^c   Choi, Hueng Sik ^a,h  

^a Chonnam National University   (South Korea)

^b Korea Research Institute of Bioscience and Biotechnology (KRIBB)   (South Korea)

^c Korea University   (South Korea)

^d Seoul National University   (South Korea)

^e Gachon University   (South Korea)

^f Korea Institute of Science and Technology   (South Korea)

^g Kyungpook National University School of Medicine   (South Korea)

^h Chonnam National University Medical School   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; CELL NUCLEUS RECEPTOR; ESTROGEN-RELATED RECEPTOR GAMMA; GLUCOSE; GSK 5182; METFORMIN; UNCLASSIFIED DRUG; DRUG DERIVATIVE; ESRRG PROTEIN, MOUSE; ESTROGEN RECEPTOR; GSK5182; TAMOXIFEN;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DIET RESTRICTION; DRUG INHIBITION; EMBRYO; GENE EXPRESSION; GLUCONEOGENESIS; GLUCOSE BLOOD LEVEL; HUMAN; HUMAN CELL; HYPERGLYCEMIA; INVERSE AGONISM; LIVER CELL; MALE; MOUSE; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; WILD TYPE; ANIMAL; C57BL MOUSE; CELL LINE; DRUG EFFECT; DRUG POTENTIATION; LIVER; METABOLISM; POLYMERASE CHAIN REACTION; RAT; SPRAGUE DAWLEY RAT; WESTERN BLOTTING;

ANIMALS; BLOTTING, WESTERN; CELL LINE; GLUCONEOGENESIS; HEPATOCYTES; HUMANS; HYPOGLYCEMIC AGENTS; LIVER; MALE; MICE; MICE, INBRED C57BL; POLYMERASE CHAIN REACTION; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ESTROGEN; TAMOXIFEN;

EID: 84887397982     PISSN: 00121797     EISSN: 1939327X     Source Type: Journal    
DOI: 10.2337/db12-0946     Document Type: Article

References (26)

1. King H, Aubert RE, Herman WH. Global burden of diabetes, 1995-2025: prevalence, numerical estimates, and projections. Diabetes Care 1998;21: 1414-1431
2. Rotella CM, Monami M, Mannucci E. Metformin beyond diabetes: new life for an old drug. Curr Diabetes Rev 2006;2:307-315
3. Hong H, Yang L, Stallcup MR. Hormone-independent transcriptional activation and coactivator binding by novel orphan nuclear receptor ERR3. J Biol Chem 1999;274:22618-22626
4. Razzaque MA, Masuda N, Maeda Y, Endo Y, Tsukamoto T, Osumi T. Estrogen receptor-related receptor gamma has an exceptionally broad specificity of DNA sequence recognition. Gene 2004;340:275-282
5. Lui K, Huang Y, Choi HL, et al. Molecular cloning and functional study of rat estrogen receptor-related receptor gamma in rat prostatic cells. Prostate 2006;66:1600-1619
6. Zhang Z, Teng CT. Interplay between estrogen-related receptor alpha (ERRalpha) and gamma (ERRgamma) on the regulation of ERRalpha gene expression. Mol Cell Endocrinol 2007;264:128-141
7. Giguère V. Transcriptional control of energy homeostasis by the estrogen-related receptors. Endocr Rev 2008;29:677-696
8. Yoon JC, Puigserver P, Chen G, et al. Control of hepatic gluconeogen-esis through the transcriptional coactivator PGC-1. Nature 2001;413: 131-138
9. Kim YD, Park KG, Lee YS, et al. Metformin inhibits hepatic gluconeogen-esis through AMP-activated protein kinase-dependent regulation of the orphan nuclear receptor SHP. Diabetes 2008;57:306-314
10. Chopra AR, Louet JF, Saha P, et al. Absence of the SRC-2 coactivator results in a glycogenopathy resembling Von Gierke's disease. Science 2008; 322:1395-1399
11. Xie YB, Park JH, Kim DK, et al. Transcriptional corepressor SMILE recruits SIRT1 to inhibit nuclear receptor estrogen receptor-related receptor gamma transactivation. J Biol Chem 2009;284:28762-28774
12. Zhang Y, Ma K, Sadana P, et al. Estrogen-related receptors stimulate py-ruvate dehydrogenase kinase isoform 4 gene expression. J Biol Chem 2006;281:39897-39906
13. Kim DK, Ryu D, Koh M, et al. Orphan nuclear receptor estrogen-related receptor g (ERRg) is key regulator of hepatic gluconeogenesis. J Biol Chem 2012;287:21628-21639
14. Kim DK, Kim JR, Koh M, et al. Estrogen-related receptor g (ERRg) is a novel transcriptional regulator of phosphatidic acid phosphatase, LIPIN1, and inhibits hepatic insulin signaling. J Biol Chem 2011;286:38035-38042
15. Coward P, Lee D, Hull MV, Lehmann JM. 4-Hydroxytamoxifen binds to and deactivates the estrogen-related receptor gamma. Proc Natl Acad Sci USA 2001;98:8880-8884
16. Chao EY, Collins JL, Gaillard S, et al. Structure-guided synthesis of ta-moxifen analogs with improved selectivity for the orphan ERRgamma. Bioorg Med Chem Lett 2006;16:821-824
17. Kim D-K, Kim Y-H, Jang H-H, et al. Estrogen-related receptor g controls hepatic CB1 receptor-mediated CYP2E1 expression and oxidative liver injury by alcohol. Gut 2013;62:1044-1054
18. Koo SH, Satoh H, Herzig S, et al. PGC-1 promotes insulin resistance in liver through PPAR-alpha-dependent induction of TRB-3. Nat Med 2004;10:530-534
19. Lee MW, Chanda D, Yang J, et al. Regulation of hepatic gluconeogenesis by an ER-bound transcription factor, CREBH. Cell Metab 2010;11:331-339
20. Ryu D, Oh KJ, Jo HY, et al. TORC2 regulates hepatic insulin signaling via a mammalian phosphatidic acid phosphatase, LIPIN1. Cell Metab 2009;9: 240-251
21. Choi CS, Fillmore JJ, Kim JK, et al. Overexpression of uncoupling protein 3 in skeletal muscle protects against fat-induced insulin resistance. J Clin Invest 2007;117:1995-2003
22. Winzell MS, Ahrén B. The high-fat diet-fed mouse: a model for studying mechanisms and treatment of impaired glucose tolerance and type 2 diabetes. Diabetes 2004;53(Suppl. 3):S215-S219
23. Foretz M, Hébrard S, Leclerc J, et al. Metformin inhibits hepatic gluco-neogenesis in mice independently of the LKB1/AMPK pathway via a decrease in hepatic energy state. J Clin Invest 2010;120:2355-2369
24. Kubo M, Ijichi N, Ikeda K, Horie-Inoue K, Takeda S, Inoue S. Modulation of adipogenesis-related gene expression by estrogen-related receptor gamma during adipocytic differentiation. Biochim Biophys Acta 2009;1789:71-77
25. Herzog B, Cardenas J, Hall RK, et al. Estrogen-related receptor alpha is a repressor of phosphoenolpyruvate carboxykinase gene transcription. J Biol Chem 2006;281:99-106
26. Liu D, Zhang Z, Teng CT. Estrogen-related receptor-gamma and peroxi-some proliferator-activated receptor-gamma coactivator-1alpha regulate estrogen-related receptor-alpha gene expression via a conserved multi-hormone response element. J Mol Endocrinol 2005;34:473-487