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Nuclear Receptors

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https://www.readbyqxmd.com/read/29656307/alveolar-bone-protective-effect-of-hiziki-extracts-on-the-progression-of-periodontitis
#1
Don-Gil Lee, Yu-Kyong Shin, Jae-Hee Park, Sang-Yong Park, Eunson Hwang, Jung-Eun Yang, Hae Jo, Ki-Young Kim, Gafurjon T Mavlonov, Tae-Hoo Yi
The purpose of this study was to evaluate the effects of hiziki extract on alveolar bone loss, inflammation, and osteo-biomarker expression in hPDL cells (10, 50, 100 μg/ml final concentrations in culture medium) and on a ligature-induced periodontitis rat model (50, 100, 200 mg/kg with oral administration). Hiziki extract increased alkaline phosphatase activity and mineralized nodule formation in hPDL cell. In western blot analysis, hiziki extract resulted in increased expression of osteoblast markers, including transforming growth factor beta (TGF-β), SMAD anchor for receptor activation (SARA) and runt-related transcription factor 2 (RUNX2) in hDPL cells...
April 14, 2018: Marine Biotechnology
https://www.readbyqxmd.com/read/29656235/effective-cancer-immunotherapy-in-mice-by-polyic-imiquimod-complexes-and-engineered-magnetic-nanoparticles
#2
Ana Isabel Bocanegra Gondan, Ane Ruiz-de-Angulo, Aintzane Zabaleta, Nina Gómez Blanco, Beatriz Macarena Cobaleda-Siles, María Jesús García-Granda, Daniel Padro, Jordi Llop, Blanca Arnaiz, María Gato, David Escors, Juan C Mareque-Rivas
Encouraging results are emerging from systems that exploit Toll like receptor (TLR) signaling, nanotechnology, checkpoint inhibition and molecular imaging for cancer immunotherapy. A major remaining challenge is developing effective, durable and tumour-specific immune responses without systemic toxicity. Here, we report a simple and versatile system based on synergistic activation of immune responses and direct cancer cell killing by combined TLR ligation using polyIC as TLR3 and imiquimod (R837) as TLR7 agonist, in combination with the model antigen ovalbumin (OVA) and phospholipid micelles loaded with zinc-doped iron oxide magnetic nanoparticles (MNPs)...
April 3, 2018: Biomaterials
https://www.readbyqxmd.com/read/29656212/myeloid-related-proteins-are-up-regulated-in-autoimmune-thyroid-diseases-and-activate-toll-like-receptor-4-and-pro-inflammatory-cytokines-in-vitro
#3
Shiqiao Peng, Xuren Sun, Xinyi Wang, Haoyu Wang, Zhongyan Shan, Weiping Teng, Chenyan Li
PURPOSE: Myeloid-related protein (MRP) family plays an important role in the promotion of cell proliferation and the production of inflammatory cytokines. We investigated the expression of MRP6, MRP8 and MRP14 in thyroid tissues, serum, and peripheral blood monocular cells (PBMCs) in patients with autoimmune thyroid diseases (AITD). METHOD: The expression of MRP6, MRP8, and MRP14 was investigated using immunohistochemical staining and quantitative real-time polymerase chain reaction in the thyroid glands of 7 patients with Graves' disease (GD), 8 with Hashimoto's thyroiditis (HT), and 7 healthy controls (HC)...
April 12, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29656209/phosphorylation-of-low-density-lipoprotein-receptor-related-protein-6-is-involved-in-receptor-for-advanced-glycation-end-product-mediated-%C3%AE-catenin-stabilization-in-a-toluene-diisocyanate-induced-asthma-model
#4
Jing Xiong, Wenqu Zhao, Yun Lin, Lihong Yao, Guohua Huang, Changhui Yu, Hangming Dong, Guanhua Xiao, Haijin Zhao, Shaoxi Cai
BACKGROUND: We have previously demonstrated that the receptor for advanced glycation end products (RAGE)/β-catenin axis plays a vital role in regulating airway inflammation and airway remodeling in a toluene diisocyanate (TDI)-induced murine asthma model. However, the exact mechanism of β-catenin activation remains unclear. Given that phosphorylation of the low-density lipoprotein receptor-related protein 6 (Lrp6) is a key step in mediating β-catenin stabilization in canonical wnt/β-catenin signaling, we explored the possible relationship between RAGE and Lrp6 in regulating β-catenin stabilization in TDI-induced asthma...
April 12, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29656192/in-vitro-bioanalysis-of-drinking-water-from-source-to-tap
#5
Anna Kjerstine Rosenmai, Johan Lundqvist, Théo le Godec, Åsa Ohlsson, Rikard Tröger, Björn Hellman, Agneta Oskarsson
The presence of chemical pollutants in sources of drinking water is a key environmental problem threatening public health. Efficient removal of pollutants in drinking water treatment plants (DWTPs) is needed as well as methods for assessment of the total impact of all present chemicals on water quality. In the present study we have analyzed the bioactivity of water samples from source to tap, including effects of various water treatments in a DWTP, using a battery of cell-based bioassays, covering health-relevant endpoints...
April 6, 2018: Water Research
https://www.readbyqxmd.com/read/29656074/protein-phosphatase-2a-as-a-new-target-for-downregulating-osteoclastogenesis-and-alleviating-titanium-particle-induced-bone-resorption
#6
Liangliang Wang, Xiaobin Guo, Wei Zhou, Yayun Ding, Jiawei Shi, Xiexing Wu, Yu Liu, Yaozeng Xu, Huilin Yang, Dechun Geng
Receptor activator of nuclear factor-кB ligand (RANKL)-induced osteoclastogenesis is believed to play a critical role in osteolytic diseases including peri-prosthetic osteolysis (PPO), the primary reason for implant failure and revision surgery. In this study, we observed that protein phosphatase 2A (PP2A), a major serine-threonine phosphatase, was highly expressed in human periprosthetic interface membranes with aseptic loosening and in a murine osteolysis model induced by titanium particle irritation. PP2A inhibition effectively alleviated titanium particle-induced bone destruction at osteolytic sites...
April 12, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29655793/inhibition-of-nlrp9b-attenuates-acute-lung-injury-through-suppressing-inflammation-apoptosis-and-oxidative-stress-in-murine-and-cell-models
#7
Qiu Yanling, Cheng Xiaoning, Bai Fei, Fang Liyun, Hu Huizhong, Sun Daqing
Acute lung injury (ALI), known a severe disease along with high morbidity and mortality, is lacking of specific therapies. Inflammation, apoptosis and oxidative stress are critical pathologies that contribute to ALI. Recently, there is study indicated that NLRP9b, a NOD-like receptor (NLR) member, is critical in modulation of inflammatory response. However, the effects of NLRP9b on sepsis-associated ALI, and the underlying molecular mechanism have not been understood. In the present study, the wild type (WT) and NLRP9b-knockout (NLRP9b-/- ) mice with C57B/L6 background were subjected to a cecal ligation and puncture (CLP) for ALI murine model establishment...
April 12, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29655696/syringin-prevents-bone-loss-in-ovariectomized-mice-via-traf6-mediated-inhibition-of-nf-%C3%AE%C2%BAb-and-stimulation-of-pi3k-akt
#8
Jingjing Liu, Zhuanzhuan Zhang, Qi Guo, Yanhong Dong, Qipeng Zhao, Xueqin Ma
BACKGROUND: Syringin, also called eleutheroside B, is a main bioactive phenolic glycoside in Acanthopanax senticosus (Rupr. et Maxim.) Harms. Based on the "kidney dominates bone" theory of TCM, A. senticosus can strengthen bone and Syringin may be one of the responsibilities. PURPOSE: The objectives of this study were to estimate the osteoporotic activity of Syringin and reveal the possible molecular mechanisms in vivo. METHODS: Sixty female ICR mice were randomly assigned into sham operated group (SHAM, treated with vehicle) and five ovariectomized subgroups (n = 10 each), treated with vehicle as OVX group, estradiol valerate (EV, 1 mg/kg/day) as positive group, and Syringin (10, 20 and 40 mg/kg/day) as low, moderate and high dosage groups...
March 15, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29655569/activation-of-the-porcine-alveolar-macrophages-via-toll-like-receptor-4-nf-%C3%AE%C2%BAb-mediated-pathway-provides-a-mechanism-of-resistin-leading-to-inflammation
#9
Bi Li, Jing Fang, Zhicai Zuo, Sirui Yin, Tingting He, Mingxian Yang, Junliang Deng, Liuhong Shen, Xiaoping Ma, Shumin Yu, Ya Wang, Zhihua Ren, Hengmin Cui
Resistin, a previously discovered cysteine-rich adipokine known to regulate glucose metabolism, has been emerged as a mediator in inflammation and immunity. Its level was supposed to be related to the expression of indicators, such as interleukin-1β (IL-1β), IL-6 and tumor necrosis factor-α (TNF-α) in inflammation. Toll-like receptor 4 (TLR4) was reported to be a receptor for resistin in cells, like leukocytes and peripheral blood mononuclear cells (PBMC). However, the pro-inflammatory role of resistin and its intracellular mechanisms in alveolar macrophages have not been thoroughly validated...
April 11, 2018: Cytokine
https://www.readbyqxmd.com/read/29653294/sclerostin-vaccination-mitigates-estrogen-deficiency-induction-of-bone-mass-loss-and-microstructure-deterioration
#10
Feng-Sheng Wang, Re-Wen Wu, Wei-Shiung Lain, Tsai-Chen Tsai, Yu-Shan Chen, Yi-Chih Sun, Huei-Jing Ke, Jui-Chen Li, Jau-Lang Hwang, Jih-Yang Ko
Sclerostin (SOST) is a Wnt signaling inhibitor detrimental to osteogenic differentiation and bone mineral acquisition. While control of SOST action delays the pathogenesis of skeletal disorders, the effects of SOST vaccination on the estrogen deficiency-induced bone deterioration remain elusive. In this study, we generated a SOST-Fc fusion protein which was composed of a SOST peptide Pro-Asn-Ala-Ile-Gly along with an IgG Fc fragment. SOST-Fc vaccination increased serum anti-SOST antibody levels and reduced serum SOST concentrations in mice...
April 10, 2018: Bone
https://www.readbyqxmd.com/read/29653110/sirna-mediated-lrp-lr-knock-down-reduces-cellular-viability-of-malignant-melanoma-cells-through-the-activation-of-apoptotic-caspases
#11
Thalia M Rebelo, Leila Vania, Eloise Ferreira, Stefan F T Weiss
The 37kDa/67kDa laminin receptor (LRP/LR) is over-expressed in tumour cells and has been implicated in several tumourigenic processes such as metastasis and telomerase activation, however, more importantly the focus of the present study is on the maintenance of cellular viability and the evasion of apoptosis. The aim of the study was to investigate the role of LRP/LR on the cellular viability of early (A375) and late stage (A375SM) malignant melanoma cells. Flow cytometry and western blot analysis revealed that A375SM cells contain more cell-surface and total LRP/LR levels in comparison to the A375 cells, respectively...
April 10, 2018: Experimental Cell Research
https://www.readbyqxmd.com/read/29653076/e4bp4-regulates-carboxylesterase-2-enzymes-through-repression-of-the-nuclear-receptor-rev-erb%C3%AE-in-mice
#12
Mengjing Zhao, Tianpeng Zhang, Fangjun Yu, Lianxia Guo, Baojian Wu
Carboxylesterases (CES) are a family of phase I enzymes that plays an important role in xenobiotic clearance and lipid metabolism. Here, we investigate a potential role of E4 promoter-binding protein 4 (E4bp4) in regulation of Ces and CPT-11 (irinotecan, a first-line drug for treating colorectal cancer) pharmacokinetics in mice. Mouse hepatoma Hepa-1c1c7 cells were transfected with Rev-erbα expression plasmid or siRNA targeting E4bp4. The relative mRNA and protein levels of Ces enzymes in the cells or the livers of wild-type and E4bp4-deficient (E4bp4-/- ) mice were determined by qPCR and Western blotting, respectively...
April 10, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29652619/circulating-cytokine-chemokine-concentrations-respond-to-ionizing-radiation-doses-but-not-radiation-dose-rates-granulocyte-colony-stimulating-factor-and-interleukin-18
#13
Juliann G Kiang, Joan T Smith, Sara R Hegge, Natalia I Ossetrova
Exposure to ionizing radiation is a crucial life-threatening factor in nuclear and radiological incidents. It is known that ionizing radiation affects cytokine/chemokine concentrations in the blood of B6D2F1 mice. It is not clear whether radiation dose rates would vary the physiological response. Therefore, in this study we utilized data from two experiments using B6D2F1 female mice exposed to six different dose rates ranging from low to high rates. In one experiment, mice received a total dose of 8 Gy (LD0/30 ) of 60 Co gamma radiation at four dose rates: 0...
April 13, 2018: Radiation Research
https://www.readbyqxmd.com/read/29652606/development-of-pei-rank-sirna-complex-loaded-plga-nanocapsules-for-the-treatment-of-osteoporosis
#14
Deniz Sezlev Bilecen, Hasan Uludag, Vasif Hasirci
Osteoporosis, which is characterized by low bone mineral density and susceptibility to fracture, is caused by increased osteoclastic activity. Receptor Activator of Nuclear Factor Kappa B Ligand (RANKL)/RANK signaling plays an important role in osteoclast differentiation and activation. The current treatment strategies for osteoporosis do not directly address this underlying cause and generates undesired side effects. This led to emergence of controlled delivery systems to increase drug bioavailability and efficacy specifically at the bone tissue...
March 14, 2018: Tissue Engineering. Part A
https://www.readbyqxmd.com/read/29652575/olive-fruit-blends-modulate-lipid-sensing-nuclear-receptor-ppar%C3%AE-cell-survival-and-oxidative-stress-response-in-human-osteoblast-cells
#15
Sergio Ammendola, Rossana Cocchiola, Mariangela Lopreiato, Laura Politi, Roberto Scandurra, Anna Maria Giusti, Anna Scotto d'Abusco
OBJECTIVE: The aim of the present study was to investigate how different extravirgin olive oils (EVOOs), obtained by blending Olea europea cultivars, could influence the cell growth, the response to inflammatory stimuli, and oxidative stress in a culture of the osteosarcoma cell line Saos-2. METHODS: Three different extravirgin olive oils were physicochemically characterized, determining the free acidity, the oxidation status, the polyphenols content, and the antioxidative activity...
April 13, 2018: Journal of the American College of Nutrition
https://www.readbyqxmd.com/read/29651663/finding-the-molecular-scaffold-of-nuclear-receptor-inhibitors-through-high-throughput-screening-based-on-proteochemometric-modelling
#16
Tianyi Qiu, Dingfeng Wu, Jingxuan Qiu, Zhiwei Cao
Nuclear receptors (NR) are a class of proteins that are responsible for sensing steroid and thyroid hormones and certain other molecules. In that case, NR have the ability to regulate the expression of specific genes and associated with various diseases, which make it essential drug targets. Approaches which can predict the inhibition ability of compounds for different NR target should be particularly helpful for drug development. In this study, proteochemometric modelling was introduced to analysis the bioactivity between chemical compounds and NR targets...
April 12, 2018: Journal of Cheminformatics
https://www.readbyqxmd.com/read/29651431/hsp90-inhibition-reduces-tlr5-surface-expression-and-nf-%C3%AE%C2%BA-b-activation-in-human-myeloid-leukemia-thp-1-cells
#17
Bon Hyang Na, Thi Xoan Hoang, Jae Young Kim
Tumors highly express active heat shock protein 90 (Hsp90), which is involved in tumor survival and progression. Enhanced Toll-like receptor (TLR) 5 expression and signaling were reported to be associated with acute myeloid leukemia. In the present study, we investigated the possible modulatory effects of Hsp90 inhibitors on TLR5 expression and signaling in the human myeloid leukemia cell line THP-1. Cells were pretreated with various concentrations of the Hsp90 inhibitor geldanamycin (GA) or the Hsp70 inhibitor VER155008, followed by stimulation with bacterial flagellin...
2018: BioMed Research International
https://www.readbyqxmd.com/read/29651293/homeobox-a5-promotes-white-adipose-tissue-browning-through-inhibition-of-the-tenascin-c-toll-like-receptor-4-nuclear-factor-kappa-b-inflammatory-signaling-in-mice
#18
Weina Cao, Hongtao Huang, Tianyu Xia, Chenlong Liu, Saeed Muhammad, Chao Sun
Lipopolysaccharide (LPS) induces rapid increase in systemic inflammatory factors. As adipose tissue is a key contributor to the inflammatory response to numerous metabolic stimuli, it is important to understand the mechanism behind the LPS-induced inflammation in white adipose tissue (WAT). Homeobox a5 (Hoxa5) is an important transcription factor, which is highly expressed in adipose tissue, and its mRNA expression is increased at cold exposure in mice. So far, the function of Hoxa5 in adipose tissue browning has been poorly understood...
2018: Frontiers in Immunology
https://www.readbyqxmd.com/read/29650790/effect-of-endocannabinoid-oleamide-on-rat-and-human-liver-cytochrome-p450-enzymes-in-in-vitro-and-in-vivo-models
#19
Gabriela Dovrtelova, Ondrej Zendulka, Kristyna Noskova, Jan Jurica, Ondrej Pes, Jan Dusek, Alejandro Carazo, Iveta Zapletalova, Natasa Hlavacova, Petr Pavek
The endocannabinoid system is important for many physiological and pathological processes, but its role in the regulation of liver cytochromes P450 (CYPs) is still unknown. We studied the influence of the endocannabinoid oleamide on rat and human liver CYPs. Oleamide was administered i.p. to rats at doses of 0.1, 1 and 10 mg/kg/day for 7 days. The content and activity of key CYPs was evaluated in rat liver microsomes. Moreover, its interactions with nuclear receptors regulating CYP genes and serum levels of their ligands (prolactin, corticosterone, and free triiodothyronine) were tested in vitro CYP inhibition assays...
April 12, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29649907/farnesoid-x-receptor-modulators-2014-present-a-patent-review
#20
Valentina Sepe, Eleonora Distrutti, Stefano Fiorucci, Angela Zampella
The nuclear receptor FXR regulates the expression of genes involved in bile acids, glucose and lipid homeostasis. For its role as guardian of metabolism, FXR has been identified a promising pharmacological target in liver bile acid and lipid accumulation, such as cholestasis and non-alcoholic fatty liver disease (NAFLD). The field of FXR research is extremely competitive with a large number of patents and articles published in the last decades identifying promising hit compounds. Areas covered. The present review summarizes recent patent activity (2014-to date) filing for synthetic and natural FXR ligands, including bile acid derivatives and non-steroidal compounds, alongside their in vitro and in vivo efficacy as well as their therapeutic applications...
April 13, 2018: Expert Opinion on Therapeutic Patents
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