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https://www.readbyqxmd.com/read/29061011/-the-role-of-estrogen-related-receptor-%C3%AE-and-atp-dependent-k-channel-kcnj1-in-renal-ischemia-reperfusion-injury
#1
Z M Wu, Q Yang, Z Y Li, D Chen, L J Jiang, X D Li, S L Chen, Z W Liu
Objective: To investigate the correlation between estrogen related-receptorγ (ERRγ) and ATP-dependent K(+) channel Kcnj1 in renal ischemia-reperfusion injury and its possible role in regulating ischemic preconditioning. Methods: The expression of ERRγ in kidney tissues was detected by immunohistochemistry. The expressions of ERRγ and Kcnj1 in human renal tubular epithelial cells (HK-2) under hypoxia (1% O(2)) were detected by RT-PCR. The ERRγ-deficient heterozygous mice model and the ERRγ-deficient completely mice model were established...
October 17, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
https://www.readbyqxmd.com/read/28993941/il-8-is-involved-in-estrogen-related-receptor-%C3%AE-regulated-proliferation-and-migration-of-colorectal-cancer-cells
#2
Sijuan Ding, Zhaohui Tang, Yongjun Jiang, Honglin Huang, Pengfei Luo, Bohua Qing, Siyuan Zhang, Ruoting Tang
BACKGROUND AND AIMS: Studies revealed that estrogenic signals were involved in the development of colorectal cancer (CRC), while the roles of estrogen related receptor (ERR) on the progression of CRC have not been well illustrated. Its roles on the development of CRC were investigated. METHODS: The expression of ERRα/β/γ in CRC cells were measured. The effects of ERRα on cell proliferation, migration and expression of cytokines were investigated accordingly...
December 2017: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/28882502/design-and-synthesis-of-benzoacridines-as-estrogenic-and-anti-estrogenic-agents
#3
Kohei Torikai, Rintaro Koga, Xiaohui Liu, Kaoru Umehara, Tatsuya Kitano, Kenji Watanabe, Tohru Oishi, Hiroshi Noguchi, Yasuyuki Shimohigashi
Estrogens play undisputedly important physiological roles, but lifetime exposure to estrogens has also been linked to the development of breast cancer. Moreover, imbalanced estrogen levels have been associated with various symptoms such as osteoporosis and menopausal disorders. For the improvement of such estrogen imbalances, estrogenic reagents with regulatory properties have shown promising potential. Herein, we report the construction of a 12-arylbenzoacridine library via a diversity-oriented strategy that furnished non-toxic estrogenic and anti-estrogenic agents...
October 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28820402/does-signaling-of-estrogen-related-receptors-affect-structure-and-function-of-bank-vole-leydig-cells
#4
P Pawlicki, A Milon, M Zarzycka, J Galas, W Tworzydlo, A Kaminska, L Pardyak, K Lesniak, A Pacwa, B Bilinska, E Gorowska-Wojtowicz, M Kotula-Balak
To get a deeper insight into the function of estrogen-related receptors (ERRs) and dissect underlying mechanism in Leydig cells, ERRs (type α, β and γ) were blocked or activated in testes of adult bank voles (Myodes glareolus) which show seasonal changes in the intratesticular sex hormones level. Both actively reproducing animals (long day conditions; LD) and those with regression of the reproductive system (short day conditions; SD) received intraperitoneal injections of selective ERRα antagonist 3-[4-(2,4-Bis-trifluoromethylbenzyloxy)-3-methoxyphenyl]-2-cyano-N-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)acrylamide (XCT 790) or selective ERRβ/ERRγ agonist N-(4-(Diethylaminobenzylidenyl)-N'-(4-hydroxybenzoyl)-hydrazine (DY131) (50 μ/kg bw; six doses every other day)...
June 2017: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28780078/atp-maintenance-via-two-types-of-atp-regulators-mitigates-pathological-phenotypes-in-mouse-models-of-parkinson-s-disease
#5
Masaki Nakano, Hiromi Imamura, Norio Sasaoka, Masamichi Yamamoto, Norihito Uemura, Toshiyuki Shudo, Tomohiro Fuchigami, Ryosuke Takahashi, Akira Kakizuka
Parkinson's disease is assumed to be caused by mitochondrial dysfunction in the affected dopaminergic neurons in the brain. We have recently created small chemicals, KUSs (Kyoto University Substances), which can reduce cellular ATP consumption. By contrast, agonistic ligands of ERRs (estrogen receptor-related receptors) are expected to raise cellular ATP levels via enhancing ATP production. Here, we show that esculetin functions as an ERR agonist, and its addition to culture media enhances glycolysis and mitochondrial respiration, leading to elevated cellular ATP levels...
August 2017: EBioMedicine
https://www.readbyqxmd.com/read/28750085/orphan-nuclear-receptor-err%C3%AE-is-a-key-regulator-of-human-fibrinogen-gene-expression
#6
Yaochen Zhang, Don-Kyu Kim, Yan Lu, Yoon Seok Jung, Ji-Min Lee, Young-Hoon Kim, Yong Soo Lee, Jina Kim, Bedair Dewidar, Won-Il Jeong, In-Kyu Lee, Sung Jin Cho, Steven Dooley, Chul-Ho Lee, Xiaoying Li, Hueng-Sik Choi
Fibrinogen, 1 of 13 coagulation factors responsible for normal blood clotting, is synthesized by hepatocytes. Detailed roles of the orphan nuclear receptors regulating fibrinogen gene expression have not yet been fully elucidated. Here, we identified estrogen-related receptor gamma (ERRγ) as a novel transcriptional regulator of human fibrinogen gene expression. Overexpression of ERRγ specially increased fibrinogen expression in human hepatoma cell line. Cannabinoid receptor types 1(CB1R) agonist arachidonyl-2'-chloroethylamide (ACEA) up-regulated transcription of fibrinogen via induction of ERRγ, whereas knockdown of ERRγ attenuated fibrinogen expression...
2017: PloS One
https://www.readbyqxmd.com/read/28479375/estrogen-receptor-related-receptor-%C3%AE-regulates-testicular-steroidogenesis-through-direct-and-indirect-regulation-of-steroidogenic-gene-expression
#7
Eunsook Park, Sudeep Kumar, Bobae Lee, Kyung-Jin Kim, Jeong-Eun Seo, Hueng-Sik Choi, Keesook Lee
Biosynthesis of testosterone, which mainly occurs in testicular Leydig cells, is controlled by steroidogenic proteins, such as StAR and P450c17. Although estrogen-related receptor gamma (ERRγ), an orphan nuclear receptor, is expressed in the testis, its role is not well understood. In this study, we investigated the expression of ERRγ in Leydig cells and its molecular action on testicular steroidogenesis. ERRγ is expressed in mouse Leydig cells from pre-pubertal stages. ERRγ overexpression in primary Leydig cells elevated the production of testosterone with a marked increase of P450c17 expression at both mRNA and protein levels, albeit decreased expression of StAR...
May 4, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28389667/female-rats-with-severe-left-ventricle-volume-overload-exhibit-more-cardiac-hypertrophy-but-fewer-myocardial-transcriptional-changes-than-males
#8
Catherine Beaumont, Élisabeth Walsh-Wilkinson, Marie-Claude Drolet, Élise Roussel, Marie Arsenault, Jacques Couet
Aortic valve regurgitation (AR) imposes a volume overload (VO) to the left ventricle (LV). Male rats with a pathological heart overload usually progress more quickly towards heart failure than females. We examined whether a sexual dimorphism exists in the myocardial transcriptional adaptations to AR. Adult Wistar male and female rats either underwent a sham operation or were induced with AR and then followed for 26 weeks. Female AR rats gained relatively more LV mass than males (75 vs. 42%). They had a similar increase in LV chamber dimensions compared to males but more wall thickening...
April 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28382164/visualization-of-macrophage-recruitment-to-inflammation-lesions-using-highly-sensitive-and-stable-radionuclide-embedded-gold-nanoparticles-as-a-nuclear-bio-imaging-platform
#9
Sang Bong Lee, Ho Won Lee, Thoudam Debraj Singh, Yinghua Li, Sang Kyoon Kim, Sung Jin Cho, Sang-Woo Lee, Shin Young Jeong, Byeong-Cheol Ahn, Sangil Choi, In-Kyu Lee, Dong-Kwon Lim, Jaetae Lee, Yong Hyun Jeon
Reliable and sensitive imaging tools are required to track macrophage migration and provide a better understating of their biological roles in various diseases. Here, we demonstrate the possibility of radioactive iodide-embedded gold nanoparticles (RIe-AuNPs) as a cell tracker for nuclear medicine imaging. To demonstrate this utility, we monitored macrophage migration to carrageenan-induced sites of acute inflammation in living subjects and visualized the effects of anti-inflammatory agents on this process...
2017: Theranostics
https://www.readbyqxmd.com/read/28209382/err%C3%AE-a-junior-orphan-with-a-senior-role-in-metabolism
#10
REVIEW
Jagannath Misra, Don-Kyu Kim, Hueng-Sik Choi
Estrogen-related receptor (ERR)γ is an orphan nuclear hormone receptor that belongs to the ERR subfamily of transcription factors. No endogenous ligand has been identified to date. ERRγ possesses ligand-independent transcriptional activity that is regulated by co-regulator interactions, and post-translational modifications (PTMs). Recent data from animal models have established ERRγ as a crucial mediator of multiple endocrine and metabolic signals. ERRγ plays important roles in pathological conditions such as insulin resistance, alcoholic liver injury, and cardiac hypertrophy, and controls energy metabolism in the heart, skeletal muscle, and pancreatic β cells...
April 2017: Trends in Endocrinology and Metabolism: TEM
https://www.readbyqxmd.com/read/28119057/immunohistochemical-profiling-of-estrogen-related-receptor-gamma-in-rat-brain-and-colocalization-with-estrogen-receptor-alpha-in-the-preoptic-area
#11
Takashi Tanida, Ken Ichi Matsuda, Shunji Yamada, Mitsuhiro Kawata, Masaki Tanaka
Estrogen-related receptor (ERR) is a member of the nuclear receptor superfamily that has strong homology with estrogen receptor (ER) α. Despite the lack of endogenous ligands, ERR serves as transcription factors through their constitutively active structure with or without interaction with ERα. Among the three subtypes of ERR (α, β, and γ), ERRγ is highly expressed in brain, but the distribution of ERRγ is poorly characterized. Therefore, we investigated ERRγ immunoreactivity throughout the rostro-caudal axis in rat brain...
March 15, 2017: Brain Research
https://www.readbyqxmd.com/read/27853434/expression-of-steroid-receptors-in-ameloblasts-during-amelogenesis-in-rat-incisors
#12
Sophia Houari, Sophia Loiodice, Katia Jedeon, Ariane Berdal, Sylvie Babajko
Endocrine disrupting chemicals (EDCs) play a part in the modern burst of diseases and interfere with the steroid hormone axis. Bisphenol A (BPA), one of the most active and widely used EDCs, affects ameloblast functions, leading to an enamel hypomineralization pattern similar to that of Molar Incisor Hypomineralization (MIH). In order to explore the molecular pathways stimulated by BPA during amelogenesis, we thoroughly investigated the receptors known to directly or indirectly mediate the effects of BPA. The expression patterns of high affinity BPA receptors (ERRγ, GPR30), of ketosteroid receptors (ERs, AR, PGR, GR, MR), of the retinoid receptor RXRα, and PPARγ were established using RT-qPCR analysis of RNAs extracted from microdissected enamel organ of adult rats...
2016: Frontiers in Physiology
https://www.readbyqxmd.com/read/27821488/androgen-dependent-repression-of-err%C3%AE-reprograms-metabolism-in-prostate-cancer
#13
Étienne Audet-Walsh, Tracey Yee, Shawn McGuirk, Mathieu Vernier, Carlo Ouellet, Julie St-Pierre, Vincent Giguère
How androgen signaling contributes to the oncometabolic state of prostate cancer remains unclear. Here, we show how the estrogen-related receptor γ (ERRγ) negatively controls mitochondrial respiration in prostate cancer cells. Sustained treatment of prostate cancer cells with androgens increased the activity of several metabolic pathways, including aerobic glycolysis, mitochondrial respiration, and lipid synthesis. An analysis of the intersection of gene expression, binding events, and motif analyses after androgen exposure identified a metabolic gene expression signature associated with the action of ERRγ...
January 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/27805390/insights-of-a-lead-optimization-study-and-biological-evaluation-of-novel-4-hydroxytamoxifen-analogs-as-estrogen-related-receptor-%C3%AE-err%C3%AE-inverse-agonists
#14
Jina Kim, Seo Yeon Woo, Chun Young Im, Eun Kyung Yoo, Seungmi Lee, Hyo-Ji Kim, Hee-Jong Hwang, Joong-Heui Cho, Won Seok Lee, Heeseok Yoon, Shinae Kim, Oh-Bin Kwon, Hayoung Hwang, Kyung-Hee Kim, Jae-Han Jeon, Thoudam Debraj Singh, Sang Wook Kim, Sung Yeoun Hwang, Hueng-Sik Choi, In-Kyu Lee, Seong Heon Kim, Yong Hyun Jeon, Jungwook Chin, Sung Jin Cho
We evaluated the in vitro pharmacology as well as the absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of chemical entities that not only were shown to be highly selective agonists for ERRγ but also exhibited enhanced pharmacokinetic profile compared with 3 (GSK5182). 6g and 10b had comparable potency to 3 and were far more selective for ERRγ over the ERRα, -β, and ERα. The in vivo pharmacokinetic profiles of 6g and 10b were further evaluated, as they possessed superior in vitro ADMET profiles compared to the other compounds...
November 23, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27763777/complementary-roles-of-estrogen-related-receptors-in-brown-adipocyte-thermogenic-function
#15
Marin L Gantner, Bethany C Hazen, Elodie Eury, Erin L Brown, Anastasia Kralli
Brown adipose tissue (BAT) thermogenesis relies on a high abundance of mitochondria and the unique expression of the mitochondrial Uncoupling Protein 1 (UCP1), which uncouples substrate oxidation from ATP synthesis. Adrenergic stimulation of brown adipocytes activates UCP1-mediated thermogenesis; it also induces the expression of Ucp1 and other genes important for thermogenesis, thereby endowing adipocytes with higher oxidative and uncoupling capacities. Adipocyte mitochondrial biogenesis and oxidative capacity are controlled by multiple transcription factors, including the estrogen-related receptor (ERR)α...
December 2016: Endocrinology
https://www.readbyqxmd.com/read/27532429/estrogen-related-receptor-%C3%AE-participates-transforming-growth-factor-%C3%AE-tgf-%C3%AE-induced-epithelial-mesenchymal-transition-of-osteosarcoma-cells
#16
Yantao Chen, Kunshui Zhang, Yang Li, Qing He
Osteosarcoma patients often exhibit pulmonary metastasis, which results in high patient mortality. Understanding the mechanisms of advanced metastasis in osteosarcoma cell is important for the targeted treatment and drug development. Our present study revealed that transforming growth factor-β (TGF-β) treatment can significantly promote the in vitro migration and invasion of human osteosarcoma MG-63 and HOS cells. The loss of epithelial characteristics E-cadherin (E-Cad) and up regulation of mesenchymal markers Vimentin (Vim) suggested TGF-β induced epithelial-mesenchymal transition (EMT) of osteosarcoma cells...
July 4, 2017: Cell Adhesion & Migration
https://www.readbyqxmd.com/read/27507929/estrogen-related-receptor-%C3%AE-err%C3%AE-renaissance-receptor-or-receptor-renaissance
#17
REVIEW
Shailaja D Divekar, Deanna M Tiek, Aileen Fernandez, Rebecca B Riggins
Estrogen-related receptors (ERRs) are founding members of the orphan nuclear receptor (ONR) subgroup of the nuclear receptor superfamily. Twenty-seven years of study have yet to identify cognate ligands for the ERRs, though they have firmly placed ERRα and ERRγ at the intersection of cellular metabolism and oncogenesis. The pace of discovery for novel functions of ERRβ, however, has until recently been somewhat slower than that of its family members. ERRβ has also been largely ignored in summaries and perspectives of the ONR literature...
2016: Nuclear Receptor Signaling
https://www.readbyqxmd.com/read/27498368/characterization-of-a-selective-inverse-agonist-for-estrogen-related-receptor-%C3%AE-as-a-potential-agent-for-breast-cancer
#18
Liudi Zhang, Peihong Liu, Haifei Chen, Qunyi Li, Lu Chen, Huijie Qi, Xiaojin Shi, Yongli Du
The estrogen-related receptor α (ERRα) is an orphan nuclear receptor that plays a primary role in the regulation of cellular energy homeostasis and osteogenesis. It is reported that ERRα is widely expressed in a range of tissues and accumulating evidence has supported that the high expression of ERRα correlates with poor prognosis of various human malignancies, including breast, endometrium, colon, prostate and ovary cancers. Herein is described the discovery of a novel selective inverse agonist (HSP1604) of ERRα, but not of ERRβ and ERRγ, as determined using transient transfection luciferase reporter assay and a time-resolved fluorescence resonance energy transfer (TR-FRET) co-activator assay...
October 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27494364/enhanced-exercise-and-regenerative-capacity-in-a-mouse-model-that-violates-size-constraints-of-oxidative-muscle-fibres
#19
Saleh Omairi, Antonios Matsakas, Hans Degens, Oliver Kretz, Kenth-Arne Hansson, Andreas Våvang Solbrå, Jo C Bruusgaard, Barbara Joch, Roberta Sartori, Natasa Giallourou, Robert Mitchell, Henry Collins-Hooper, Keith Foster, Arja Pasternack, Olli Ritvos, Marco Sandri, Vihang Narkar, Jonathan R Swann, Tobias B Huber, Ketan Patel
A central tenet of skeletal muscle biology is the existence of an inverse relationship between the oxidative fibre capacity and its size. However, robustness of this relationship is unknown. We show that superimposition of Estrogen-related receptor gamma (Errγ) on the myostatin (Mtn) mouse null background (Mtn(-/-)/Errγ(Tg/+)) results in hypertrophic muscle with a high oxidative capacity thus violating the inverse relationship between fibre size and oxidative capacity. We also examined the canonical view that oxidative muscle phenotype positively correlate with Satellite cell number, the resident stem cells of skeletal muscle...
August 5, 2016: ELife
https://www.readbyqxmd.com/read/27486708/screening-of-toxic-effects-of-bisphenol-a-and-products-of-its-degradation-zebrafish-danio-rerio-embryo-test-and-molecular-docking
#20
Katerina Makarova, Pawel Siudem, Katarzyna Zawada, Justyna Kurkowiak
Bisphenol A (BPA) acts as an endocrine-disrupting compound even at a low concentration. Degradation of BPA could lead to the formation of toxic products. In this study, we compare the toxicity of BPA and seven intermediate products of its degradation. The accuracy of three molecular docking programs (Surflex, Autodock, and Autodock Vina) in predicting the binding affinities of selected compounds to human (ERα, ERβ, and ERRγ) and zebrafish (ERα, ERRγA, and ERRγB) estrogen and estrogen-related receptors was evaluated...
October 2016: Zebrafish
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