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https://www.readbyqxmd.com/read/28342850/structural-basis-for-differential-activities-of-enantiomeric-ppar%C3%AE-agonists-binding-of-s35-to-the-alternate-site
#1
Jun Young Jang, Minseob Koh, Hwan Bae, Doo Ri An, Ha Na Im, Hyoun Sook Kim, Ji Young Yoon, Hye-Jin Yoon, Byung Woo Han, Seung Bum Park, Se Won Suh
Peroxisome proliferator-activated receptor γ (PPARγ) is a member of the nuclear receptor superfamily. It functions as a ligand-activated transcription factor and plays important roles in the regulation of adipocyte differentiation, type 2 diabetes mellitus, and inflammation. Many PPARγ agonists bind to the canonical ligand-binding pocket near the activation function-2 (AF-2) helix (i.e., helix H12) of the ligand-binding domain (LBD). More recently, an alternate ligand-binding site was identified in PPARγ LBD; it is located beside the Ω loop between the helices H2' and H3...
March 22, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28340355/the-human-immunodeficiency-virus-1-asp-rna-promotes-viral-latency-by-recruiting-the-polycomb-repressor-complex-2-and-promoting-nucleosome-assembly
#2
Juan C Zapata, Federica Campilongo, Robert A Barclay, Catherine DeMarino, Maria D Iglesias-Ussel, Fatah Kashanchi, Fabio Romerio
Various epigenetic marks at the HIV-1 5'LTR suppress proviral expression and promote latency. Cellular antisense transcripts known as long noncoding RNAs (lncRNAs) recruit the polycomb repressor complex 2 (PRC2) to gene promoters, which catalyzes trimethylation of lysine 27 on histone H3 (H3K27me3), thus promoting nucleosome assembly and suppressing gene expression. We found that an HIV-1 antisense transcript expressed from the 3'LTR and encoding the antisense protein ASP promotes proviral latency. Expression of ASP RNA reduced HIV-1 replication in Jurkat cells...
March 21, 2017: Virology
https://www.readbyqxmd.com/read/28338656/focal-adhesion-kinase-depletion-reduces-human-hepatocellular-carcinoma-growth-by-repressing-enhancer-of-zeste-homolog-2
#3
Daniela Gnani, Ilaria Romito, Simona Artuso, Marco Chierici, Cristiano De Stefanis, Nadia Panera, Annalisa Crudele, Sara Ceccarelli, Elena Carcarino, Valentina D'Oria, Manuela Porru, Ezio Giorda, Karin Ferrari, Luca Miele, Erica Villa, Clara Balsano, Diego Pasini, Cesare Furlanello, Franco Locatelli, Valerio Nobili, Rossella Rota, Carlo Leonetti, Anna Alisi
Hepatocellular carcinoma (HCC) is the most common type of liver cancer in humans. The focal adhesion tyrosine kinase (FAK) is often over-expressed in human HCC and FAK inhibition may reduce HCC cell invasiveness. However, the anti-oncogenic effect of FAK knockdown in HCC cells remains to be clarified. We found that FAK depletion in HCC cells reduced in vitro and in vivo tumorigenicity, by inducing G2/M arrest and apoptosis, decreasing anchorage-independent growth, and modulating the expression of several cancer-related genes...
March 24, 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/28337379/long-intergenic-non-coding-rna-00152-promotes-renal-cell-carcinoma-progression-by-epigenetically-suppressing-p16-and-negatively-regulates-mir-205
#4
Yongjun Wang, Jianzhen Liu, Hongzhong Bai, Yi Dang, Pei Lv, Shucai Wu
Long non-coding RNAs (lncRNAs) have been reported to play important roles in the tumorigenesis and development of several human cancers. Long intergenic non-coding RNA 152 (LINC00152) is significantly up-regulated in some solid tumors. However, the role of LINC00152 in the pathogenesis and development of renal cell carcinoma (RCC) remains largely unclear. In the study, we showed that LINC00152 expression was up-regulated in RCC tissues compared with adjacent normal tissues and revealed that LINC00152 expression was positively correlated with lymph node metastasis, higher TNM stage, and poor over survival (OS) time in RCC patients...
2017: American Journal of Cancer Research
https://www.readbyqxmd.com/read/28337120/antidyskinetic-effects-of-mek-inhibitor-are-associated-with-multiple-neurochemical-alterations-in-the-striatum-of-hemiparkinsonian-rats
#5
Guiqin Chen, Shuke Nie, Chao Han, Kai Ma, Yan Xu, Zhentao Zhang, Stella M Papa, Xuebing Cao
L-DOPA-induced dyskinesia (LID) represents one of the major problems of the long-term therapy of patients with Parkinson's disease (PD). Although, the pathophysiologic mechanisms underlying LID are not completely understood, activation of the extracellular signal regulated kinase (ERK) is recognized to play a key role. ERK is phosphorylated by mitogen-activated protein kinase kinase (MEK), and thus MEK inhibitor can prevent ERK activation. Here the effect of the MEK inhibitor PD98059 on LID and the associated molecular changes were examined...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/28336400/mechanistic-characterization-of-s-38093-a-novel-inverse-agonist-at-histamine-h3-receptors
#6
Aurore Sors, Fany Panayi, Lionel Bert, Dominique Favale, Olivier Nosjean, Valérie Audinot, Jean-Michel Arrang, Bruno Buisson, Esther Steidl, Jean-Marie Delbos, Tuulia Huhtala, Outi Kontkanen, Anne-Marie Chollet, Patrick Casara, Pierre Lestage
Histaminergic H3 inverse agonists, by stimulating central histamine release, represent attractive drug candidates to treat cognitive disorders. The present studies aimed to describe the mechanistic profile of S 38093 a novel H3 receptors inverse agonist. S 38093 displays a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2µM, respectively) with no affinity for other histaminergic receptors. In cellular models, the compound was able to antagonize mice H3 receptors (KB = 0.65µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB = 0...
March 20, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28334966/structural-and-mechanistic-insights-into-regulation-of-hbo1-histone-acetyltransferase-activity-by-brpf2
#7
Ye Tao, Chen Zhong, Junjun Zhu, Shutong Xu, Jianping Ding
HBO1, a member of the MYST family of histone acetyltransferases (HATs), is required for global acetylation of histone H3K14 and embryonic development. It functions as a catalytic subunit in multisubunit complexes comprising a BRPF1/2/3 or JADE1/2/3 scaffold protein, and two accessory proteins. BRPF2 has been shown to be important for the HAT activity of HBO1 toward H3K14. Here we demonstrated that BRPF2 can regulate the HAT activity of HBO1 toward free H3 and H4, and nucleosomal H3. Particularly, a short N-terminal region of BRPF2 is sufficient for binding to HBO1 and can potentiate its activity toward H3K14...
February 24, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/28328154/a-symmetric-co-n5-2-h2-o-4-%C3%A2-4%C3%A2-h2-o-high-nitrogen-compound-formed-by-cobalt-ii-cation-trapping-of-a-cyclo-n5-anion
#8
Chong Zhang, Chen Yang, Bingcheng Hu, Chuanming Yu, Zhansheng Zheng, Chengguo Sun
The reactions of (N5 )6 (H3 O)3 (NH4 )4 Cl with Co(NO3 )2 ⋅6 H2 O at room temperature yielded Co(N5 )2 (H2 O)4 ⋅4 H2 O as an air-stable orange metal complex. The structure, as determined by single-crystal X-ray diffraction, has two planar cyclo-N5(-) rings and four bound water molecules symmetrically positioned around the central metal ion. Thermal analysis demonstrated the explosive properties of the material.
March 22, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28326943/analgesia-induced-by-the-epigenetic-drug-l-acetylcarnitine-outlasts-the-end-of-treatment-in-mouse-models-of-chronic-inflammatory-and-neuropathic-pain
#9
Serena Notartomaso, Giada Mascio, Matteo Bernabucci, Cristina Zappulla, Pamela Scarselli, Milena Cannella, Tiziana Imbriglio, Roberto Gradini, Giuseppe Battaglia, Valeria Bruno, Ferdinando Nicoletti
Background L-acetylcarnitine, a drug marketed for the treatment of chronic pain, causes analgesia by epigenetically up-regulating type-2 metabotropic glutamate (mGlu2) receptors in the spinal cord. Because the epigenetic mechanisms are typically long-lasting, we hypothesized that analgesia could outlast the duration of L-acetylcarnitine treatment in models of inflammatory and neuropathic pain. Results A seven-day treatment with L-acetylcarnitine (100 mg/kg, once a day, i.p.) produced an antiallodynic effect in the complete Freund adjuvant mouse model of chronic inflammatory pain...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28325625/-serological-detection-of-brucella-suis-influenza-virus-and-aujeszky-s-disease-virus-in-backyard-and-small-swine-holders-in-argentina
#10
Marina Dibarbora, Javier A Cappuccio, María N Aznar, Fernando A Bessone, Hernán Piscitelli, Ariel J Pereda, Daniel R Pérez
Farmers raising less than 100 sows represent more than 99% of swine producers in Argentina, although little is known about their sanitary status and productive characteristics in the country. Sanitary and productive information was obtained. Furthermore, samples for serological studies were taken to detect antibodies against Brucella suis (Bs), Aujeszky's disease virus (AV) and influenza virus (IV) in 68 backyard and small producers with less than 100 sows located in the north, central and south regions of Argentina...
March 18, 2017: Revista Argentina de Microbiología
https://www.readbyqxmd.com/read/28318771/cross-protection-to-new-drifted-influenza-a-h3-viruses-and-prevalence-of-protective-antibodies-to-seasonal-influenza-during-2014-in-portugal
#11
Raquel Guiomar, Susana Pereira da Silva, Patrícia Conde, Paula Cristóvão, Ana Carina Maia, Pedro Pechirra, Ana Paula Rodrigues, Baltazar Nunes, Luís Milho, Ana Paula Coelho, Aida Fernandes, Paula Caseiro, Fernando Rodrigues, Lurdes Correia, João Pereira-Vaz, Sofia Almeida, Paula Branquinho, Rita Côrte-Real, Regina Viseu, Maria João Peres, Raquel Sanches, Filipa Dantas, Ludovina Freitas, Graça Andrade, Manuel Maurílio, Filomena Caldeira, Rita Cabral Veloso, Luisa Mota-Vieira, Marta Soares, Ana Rita Couto, Jácome Bruges-Armas, Rita Mouro Pinto, Joana Sobrinho Simões, Maria do Rosário Costa, João Tiago Guimarães, Luís Martins, Mário Cunha
INTRODUCTION: Immune profile for influenza viruses is highly changeable over time. Serological studies can assess the prevalence of influenza, estimate the risk of infection, highlight asymptomatic infection rate and can also provide data on vaccine coverage. The aims of the study were to evaluate pre-existing cross-protection against influenza A(H3) drift viruses and to assess influenza immunity in the Portuguese population. MATERIALS AND METHODS: We developed a cross-sectional study based on a convenience sample of 626 sera collected during June 2014, covering all age groups, both gender and all administrative health regions of Portugal...
March 15, 2017: Vaccine
https://www.readbyqxmd.com/read/28315523/dna-mediated-association-of-two-histone-bound-caf-1-complexes-drives-tetrasome-assembly-in-the-wake-of-dna-replication
#12
Francesca Mattiroli, Yajie Gu, Tejas Yadav, Jeremy L Balsbaugh, Michael R Harris, Eileen S Findlay, Yang Liu, Catherine A Radebaugh, Laurie A Stargell, Natalie G Ahn, Iestyn Whitehouse, Karolin Luger
Nucleosome assembly in the wake of DNA replication is a key process that regulates cell identity and survival. Chromatin assembly factor 1 (CAF-1) is a H3-H4 histone chaperone that associates with the replisome and orchestrates chromatin assembly following DNA synthesis. Little is known about the mechanism and structure of this key complex. Here we investigate the CAF-1•H3-H4 binding mode and the mechanism of nucleosome assembly. We show that CAF-1 binding to a H3-H4 dimer activates the Cac1 winged helix domain interaction with DNA...
March 18, 2017: ELife
https://www.readbyqxmd.com/read/28302719/a-repressive-role-of-enhancer-of-zeste-homolog-2-in-11%C3%AE-hydroxysteroid-dehydrogenase-type-2-expression-in-human-placenta
#13
Rujuan Zuo, Xiaohui Liu, Wangsheng Wang, Wenjiao Li, Hao Ying, Kang Sun
The expression of 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), which acts as a placental glucocorticoid barrier, is silenced in the cytotrophoblasts but substantially up-regulated during syncytialization. However, the repressive mechanism of 11β-HSD2 expression before syncytialization and how this repression is lifted during syncytialization remain mostly unresolved. Here we found that enhancer of zeste homolog 2 (EZH2) accounts for the silence of 11β-HSD2 expression via trimethylation of histone H3 lysine 27 (H3K27me3) at the promoter of 11β-HSD2 gene...
March 16, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28294989/a-flavone-constituent-from-myoporum-bontioides-induces-m-phase-cell-cycle-arrest-of-mcf-7-breast-cancer-cells
#14
Jing-Ru Weng, Li-Yuan Bai, Wei-Yu Lin, Chang-Fang Chiu, Yu-Chang Chen, Shi-Wei Chao, Chia-Hsien Feng
Myoporum bontioides is a traditional medicinal plant in Asia with various biological activities, including anti-inflammatory and anti-bacterial characteristics. To identify the bioactive constituents from M. bontioides, a newly-identified flavone, 3,4'-dimethoxy-3',5,7-trihydroxyflavone (compound 1), along with eight known compounds, were investigated in human MCF-7 breast cancer, SCC4 oral cancer, and THP-1 monocytic leukemia cells. Among these compounds, compound 1 exhibited the strongest antiproliferative activity with half-maximal inhibitory concentration (IC50) values ranging from 3...
March 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28293664/the-expression-of-b7-h3-molecule-in-periodontal-disease
#15
Saumya John, Arun Kurumathur, Avaneendra Talwar, Keerthana Kumar, Teenu Abraham, Ananthi Alagiri, Gnanasagar Walaja, Jasmine Clements
STATEMENT OF THE PROBLEM: T cells have been shown to play a role in the etiopathogenesis of periodontal disease. B7-H3, a costimulatory molecule, is found to be associated with regulation of T cell function in some tumoral tissues, as well as autoimmune and inflammatory diseases. PURPOSE: The aim of this study was to investigate the expression of B7-H3 molecule in healthy and diseased gingival tissue samples. MATERIALS AND METHOD: Gingival samples were taken from 2 groups (A and B) representing periodontal health and periodontal disease, respectively...
March 2017: Journal of Dentistry
https://www.readbyqxmd.com/read/28292308/surveillance-of-avian-influenza-viruses-in-south-korea-between-2012-and-2014
#16
Eun-Kyoung Lee, Hyun-Mi Kang, Byung-Min Song, Yu-Na Lee, Gyeong-Beum Heo, Hee-Soo Lee, Youn-Jeong Lee, Jae-Hong Kim
BACKGROUND: National surveillance of avian influenza virus (AIV) in South Korea has been annually conducted for the early detection of AIV and responses to the introduction of highly pathogenic avian influenza (HPAI) virus. In this study, we report on a nationwide surveillance study of AIV in domestic poultry and wild birds in South Korea between 2012 and 2014. METHODS: During the surveillance programs between 2012 and 2014, 141,560 samples were collected. Of these, 102,199 were from poultry farms, 8215 were from LBMs, and 31,146 were from wild bird habitats...
March 14, 2017: Virology Journal
https://www.readbyqxmd.com/read/28291648/combining-stable-insect-cell-lines-with-baculovirus-mediated-expression-for-multi-ha-influenza-vlp-production
#17
Daniela P Sequeira, Ricardo Correia, Manuel J T Carrondo, António Roldão, Ana P Teixeira, Paula M Alves
Safer and broadly protective vaccines are needed to cope with the continuous evolution of circulating influenza virus strains and promising approaches based on the expression of multiple hemagglutinins (HA) in a virus-like particle (VLP) have been proposed. However, expression of multiple genes in the same vector can lead to its instability due to tandem repetition of similar sequences. By combining stable with transient expression systems we can rationally distribute the number of genes to be expressed per platform and thus mitigate this risk...
March 10, 2017: Vaccine
https://www.readbyqxmd.com/read/28288770/experimental-toxoplasma-gondii-infections-in-pigs-humoral-immune-response-estimation-of-specific-igg-avidity-and-the-challenges-of-reproducing-vertical-transmission-in-sows
#18
Walter Basso, Felix Grimm, Maja Ruetten, Vitomir Djokic, Radu Blaga, Xaver Sidler, Peter Deplazes
Ten pregnant sows were experimentally inoculated per os with T. gondii in order to investigate vertical and galactogenic transmission of the parasite and the evolution and maturation of the specific IgG humoral response in the sows and piglets. Five seronegative sows received 10(4)T. gondii (CZ isolate clone H3) sporulated oocysts during late-pregnancy (Exp. 1), three sows received 10(4) oocysts during mid-pregnancy (Exp. 2) and three sows from Exp. 1 (and two seronegative sows) were re-inoculated with 10(5) oocysts during a further pregnancy (late-pregnancy) (Exp...
March 15, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28284625/putative-vaccine-breakthrough-event-associated-with-heterotypic-rotavirus-infection-in-newborn-calves-turkey-2015
#19
Ilke Karayel, Enikő Fehér, Szilvia Marton, Nüvit Coskun, Krisztián Bányai, Feray Alkan
Group A rotaviruses (RVA) are regarded as major enteric pathogens of large ruminants, including cattle. Rotavirus vaccines administered to pregnant cows are commonly used to provide passive immunity that protects newborn calves from the clinical disease. In this study we report the detection of RVA from calves with severe diarrhea in a herd regularly vaccinated to prevent enteric infections including RVA. Diarrheic disease was observed in newborn calves aged 4-15days, with high morbidity and mortality rates, but no diarrhea was seen in adult animals...
March 2017: Veterinary Microbiology
https://www.readbyqxmd.com/read/28284043/the-histone-variant-h3-3-claims-its-place-in-the-crowded-scene-of-epigenetics
#20
Daniele Bano, Antonia Piazzesi, Paolo Salomoni, Pierluigi Nicotera
Histones are evolutionarily conserved DNA-binding proteins. As scaffolding molecules, they significantly regulate the DNA packaging into the nucleus of all eukaryotic cells. As docking units, they influence the recruitment of the transcriptional machinery, thus establishing unique gene expression patterns that ultimately promote different biological outcomes. While canonical histones H3.1 and H3.2 are synthetized and loaded during DNA replication, the histone variant H3.3 is expressed and deposited into the chromatin throughout the cell cycle...
March 10, 2017: Aging
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