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https://www.readbyqxmd.com/read/27932863/non-imidazole-based-histamine-h3-receptor-antagonists-with-anticonvulsant-activity-in-different-seizure-models-in-male-adult-rats
#1
Bassem Sadek, Ali Saad, Gniewomir Latacz, Kamil Kuder, Agnieszka Olejarz, Tadeusz Karcz, Holger Stark, Katarzyna Kieć-Kononowicz
A series of twelve novel non-imidazole-based ligands (3-14) was developed and evaluated for its in vitro binding properties at the human histamine H3 receptor (hH3R). The novel ligands were investigated for their in vivo protective effects in different seizure models in male adult rats. Among the H3R ligands (3-14) tested, ligand 14 showed significant and dose-dependent reduction in the duration of tonic hind limb extension in maximal electroshock (MES)-induced seizure model subsequent to acute systemic administration (5, 10, and 20 mg/kg, intraperitoneally), whereas ligands 4, 6, and 7 without appreciable protection in MES model were most promising in pentylenetetrazole (PTZ) model...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27932644/detection-and-whole-genome-characterization-of-a-g8p-1-group-a-rotavirus-strain-from-deer
#2
Srivishnupriya Anbalagan, Jessica Peterson
Rotavirus A strain 14-02218-2, with genome constellation G8P[1]-I2-R2-C2-M2-A3-N2-T6-E2-H3, was isolated from newborn fawns. The 14-02218-2 rotavirus strain is related to bovine and bovine-like rotavirus strains. To our knowledge, this is the first report on whole-genome-based characterization of a deer rotavirus G8P[1] strain.
December 8, 2016: Genome Announcements
https://www.readbyqxmd.com/read/27931518/vitamin-c-enhances-the-expression-of-il17-in-a-jmjd2-dependent-manner
#3
Mi Hye Song, Varun Sasidharan Nair, Kwon Ik Oh
Previously, we reported that vitamin C facilitates the CpG demethylation of Foxp3 enhancer in CD4+Foxp3+ regulatory T cells (Tregs) by enhancing the activity of a DNA demethylase ten-eleven-translocation (Tet). However, it is not clear whether vitamin C affects other helper T cell lineages like T helper type 17 (Th17) cells which are related with Tregs. Here, we show that the expression of interleukin-17A (IL17) increases with the treatment of vitamin C but not with other antioxidants. Interestingly, the upregulation of IL17 was not accompanied by DNA demethylation in Il17 promoter and was independent of Tet enzymes...
December 9, 2016: BMB Reports
https://www.readbyqxmd.com/read/27930850/elusive-antimony-centered-radical-cations-isolation-characterization-crystal-structures-and-reactivity-studies
#4
Tao Li, Houjia Wei, Yong Fang, Lei Wang, Sheng Chen, Zaichao Zhang, Yue Zhao, Gengwen Tan, Xinping Wang
One-electron oxidation of the stibines Aryl3 Sb (1, Aryl=2,6-(i) Pr2 -4-OMe-C6 H2 ; 2, Aryl=2,4,6-(i) Pr3 -C6 H2 ) with AgSbF6 and NaBAryl(F)4 (Aryl(F) =3,5-(CF3 )2 C6 H3 ) afforded the first structurally characterized examples of antimony-centered radical cations 1(.+) [BAryl(F)4 ](-) and 2(.+) [BAryl(F)4 ](-) . Their molecular and electronic structures were investigated by single-crystal X-ray diffraction, electron paramagnetic resonance spectroscopy (EPR) and UV/Vis absorption spectroscopy, in conjunction with theoretical calculations...
December 8, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27923618/novel-3-methylindoline-inhibitors-of-ezh2-design-synthesis-and-sar
#5
Amantullah Ansari, Sharad Satalkar, Varshavekumar Patil, Amit S Shete, Simranjeet Kaur, Ashu Gupta, Siddhartha Singh, Mohd Raja, Daniel L Severance, Sebastián Bernales, Sarvajit Chakravarty, David T Hung, Son M Pham, Francisco J Herrera, Roopa Rai
EZH2 (enhancer of zeste homologue 2) is the catalytic subunit of the polycomb repressive complex 2 (PRC2) that catalyzes the methylation of lysine 27 of histone H3 (H3K27). Dysregulation of EZH2 activity is associated with several human cancers and therefore EZH2 inhibition has emerged as a promising therapeutic target. Several small molecule EZH2 inhibitors with different chemotypes have been reported in the literature, many of which use a bicyclic heteroaryl core. Herein, we report the design and synthesis of EZH2 inhibitors containing an indoline core...
November 25, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27922185/relaxin-family-peptides-structure-activity-relationship-studies
#6
REVIEW
Nitin A Patil, K Johan Rosengren, Frances Separovic, John D Wade, Ross A D Bathgate, Mohammed Akhter Hossain
The human relaxin peptide family consists of seven cystine-rich peptides, four of which are known to signal through relaxin family peptide receptors, RXFP1-4. Considering the vital roles these peptides play in physiology and various diseases, they are of considerable importance for drug discovery and development. Detailed structure-activity relationship (SAR) studies towards understanding the role of important residues in each of these peptides have been reported over the years and utilised for design of antagonists and minimised agonist variants...
December 6, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27918982/traffic-derived-particulate-matter-exposure-and-histone-h3-modification-a-repeated-measures-study
#7
Yinan Zheng, Marco Sanchez-Guerra, Zhou Zhang, Brian T Joyce, Jia Zhong, Jacob K Kresovich, Lei Liu, Wei Zhang, Tao Gao, Dou Chang, Citlalli Osorio-Yanez, Juan Jose Carmona, Sheng Wang, John P McCracken, Xiao Zhang, Yana Chervona, Anaite Díaz, Pier A Bertazzi, Petros Koutrakis, Choong-Min Kang, Joel Schwartz, Andrea A Baccarelli, Lifang Hou
BACKGROUND: Airborne particulate matter (PM) may induce epigenetic changes that potentially lead to chronic diseases. Histone modifications regulate gene expression by influencing chromatin structure that can change gene expression status. We evaluated whether traffic-derived PM exposure is associated with four types of environmentally inducible global histone H3 modifications. METHODS: The Beijing Truck Driver Air Pollution Study included 60 truck drivers and 60 office workers examined twice, 1-2 weeks apart, for ambient PM10 (both day-of and 14-day average exposures), personal PM2...
December 2, 2016: Environmental Research
https://www.readbyqxmd.com/read/27916793/histone-h3-methyltransferase-suv39h1-prevents-myogenic-terminal-differentiation-by-repressing-mef2-activity-in-muscle-cells
#8
Wei Jin, Yangyang Shang, Jian Peng, Siwen Jiang
The myogenic regulatory factors (MRFs) and myocyte enhancer factor 2 (MEF2) transcription factors have been extensively studied as key transcription factors that regulate myogenic gene expression. However, few reports on the molecular mechanism that modulates chromatin remodeling during skeletal muscle differentiation are available. We reported here that the expression of the H3-K9 methyltransferase Suv39h1 was decreased during myoblast differentiation. Ectopic expression of Suv39h1 could inhibit myoblast differentiation, increasing H3-K9 methylation levels, whereas knockdown of Suv39h1 stimulated myoblast differentiation...
November 28, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27904655/increased-set1-binding-at-the-promoter-induces-aberrant-epigenetic-alterations-and-up-regulates-cyclic-adenosine-5-monophosphate-response-element-modulator-alpha-in-systemic-lupus-erythematosus
#9
Qing Zhang, Shu Ding, Huilin Zhang, Hai Long, Haijing Wu, Ming Zhao, Vera Chan, Chak-Sing Lau, Qianjin Lu
BACKGROUND: Up-regulated cyclic adenosine 5'-monophosphate response element modulator α (CREMα) which can inhibit IL-2 and induce IL-17A in T cells plays a critical role in the pathogenesis of systemic lupus erythematosus (SLE). This research aimed to investigate the mechanisms regulating CREMα expression in SLE. RESULTS: From the chromatin immunoprecipitation (ChIP) microarray data, we found a sharply increased H3 lysine 4 trimethylation (H3K4me3) amount at the CREMα promoter in SLE CD4+ T cells compared to controls...
2016: Clinical Epigenetics
https://www.readbyqxmd.com/read/27904046/cocl2-decreases-ec-sod-expression-through-histone-deacetylation-in-cos7-cells
#10
Shuhei Hattori, Tetsuro Kamiya, Hirokazu Hara, Masayuki Ninomiya, Mamoru Koketsu, Tetsuo Adachi
Extracellular-superoxide dismutase (EC-SOD), one of the SOD isozymes, is negatively regulated under hypoxic conditions, and decreases in its expression may exacerbate vascular diseases. Moreover, epigenetics, such as DNA methylation and histone modifications, are known to play a critical role in the progression of cancer, type 2 diabetes, and atherosclerosis. We previously investigated the involvement of reactive oxygen species (ROS) and p38 mitogen-activated protein kinase (MAPK) in decreases in EC-SOD expression in hypoxic COS7 cells; however, the role of epigenetics in this process currently remains unknown...
2016: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27903601/performance-evaluation-of-allplex%C3%A2-respiratory-panel-1-2-and-3-for-the-detection-of-respiratory-viruses-and-influenza-a-virus-subtypes
#11
Hee Jae Huh, Ji-Youn Kim, Hyeon Jeong Kwon, Sun Ae Yun, Myoung-Keun Lee, Nam Yong Lee, Jong-Won Kim, Chang-Seok Ki
The Allplex™ Respiratory Panel 1, 2, and 3 (Allplex) is a one-step real-time reverse transcription PCR assay for the detection of respiratory viruses (RVs) and influenza A subtypes based on MuDT™ technology. Performance of the Allplex assay was compared to the AdvanSure™ RV real-time PCR Kit (AdvanSure) and PowerChek™ Pandemic H1N1/H3N2/H5N1 Real-time PCR Kit (PowerChek) using 417 clinical respiratory specimens. Compared to the AdvanSure assay for RV detection by each virus, the ranges of positive percent agreement, negative percent agreement, and kappa value were 82...
November 30, 2016: Journal of Clinical Microbiology
https://www.readbyqxmd.com/read/27899915/novel-h7n2-and-h5n6-avian-influenza-a-viruses-in-sentinel-chickens-a-sentinel-chicken-surveillance-study
#12
Teng Zhao, Yan-Hua Qian, Shan-Hui Chen, Guo-Lin Wang, Meng-Na Wu, Yong Huang, Guang-Yuan Ma, Li-Qun Fang, Gregory C Gray, Bing Lu, Yi-Gang Tong, Mai-Juan Ma, Wu-Chun Cao
In 2014, a sentinel chicken surveillance for avian influenza viruses was conducted in aquatic bird habitat near Wuxi City, Jiangsu Province, China. Two H7N2, one H5N6, and two H9N2 viruses were isolated. Sequence analysis revealed that the H7N2 virus is a novel reassortant of H7N9 and H9N2 viruses and H5N6 virus is a reassortant of H5N1 clade 2.3.4 and H6N6 viruses. Substitutions V186 and L226 (H3 numbering) in the hemagglutinin (HA) gene protein was found in two H7N2 viruses but not in the H5N6 virus. Two A138 and A160 mutations were identified in the HA gene protein of all three viruses but a P128 mutation was only observed in the H5N6 virus...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/27895384/exendin-4-induces-extracellular-superoxide-dismutase-through-histone-h3-acetylation-in-human-retinal-endothelial-cells
#13
Hiroyuki Yasuda, Atsuko Ohashi, Shohei Nishida, Tetsuro Kamiya, Tetsuya Suwa, Hirokazu Hara, Jun Takeda, Yoshinori Itoh, Tetsuo Adachi
Extracellular-superoxide dismutase (genetic name SOD3) is a secreted anti-oxidative enzyme, and its presence in vascular walls may play an important role in protecting the vascular system against oxidative stress. Oxidative stress has been implicated in the pathogenesis of diabetic retinopathy; therefore, increases in extracellular-superoxide dismutase have been suggested to inhibit the progression of diabetic retinopathy. Incretin-based drugs such as glucagon-like peptide-1 receptor agonists are used in the treatment of type 2 diabetes...
November 2016: Journal of Clinical Biochemistry and Nutrition
https://www.readbyqxmd.com/read/27889645/suppression-of-tumor-growth-and-muscle-wasting-in-a-transgenic-mouse-model-of-pancreatic-cancer-by-the-novel-histone-deacetylase-inhibitor-ar-42
#14
Sally E Henderson, Li-Yun Ding, Xiaokui Mo, Tanios Bekaii-Saab, Samuel K Kulp, Ching-Shih Chen, Po-Hsien Huang
PURPOSE: Pancreatic ductal adenocarcinoma (PDAC) is the third leading cause of cancer death in the United States. This study was aimed at evaluating the efficacy of AR-42 (formerly OSU-HDAC42), a novel histone deacetylase (HDAC) inhibitor currently in clinical trials, in suppressing tumor growth and/or cancer-induced muscle wasting in murine models of PDAC. EXPERIMENTAL DESIGN: The in vitro antiproliferative activity of AR-42 was evaluated in six human pancreatic cancer cell lines (AsPC-1, COLO-357, PANC-1, MiaPaCa-2, BxPC-3, SW1990)...
November 24, 2016: Neoplasia: An International Journal for Oncology Research
https://www.readbyqxmd.com/read/27886392/deregulated-expression-of-ezh2-in-congenital-brainstem-disconnection
#15
P G Barth, E Aronica, S Fox, K Fluiter, M A J Weterman, A Poretti, D C Miller, E Boltshauser, B Harding, M Santi, F Baas
Congenital brainstem disconnection (CBSD) is an enigmatic embryo-fetal defect presenting as (sub)total absence of a segment between mesencephalon and lower brainstem. Rostro-caudal limits of the defect vary while the basal pons is always involved and the cerebellum is globally hypoplastic. A recent update and review[1] lists 14 cases, including 3 brain autopsy studies[1-3]. Necrosis and glial- or inflammatory reactions were absent. Inferior olivary nuclei were small or absent, pontine nuclei depleted, and the cerebellar dentate nuclei dysplastic...
November 25, 2016: Neuropathology and Applied Neurobiology
https://www.readbyqxmd.com/read/27884950/neutrophil-extracellular-traps-in-the-amniotic-cavity-of-women-with-intra-amniotic-infection-a-new-mechanism-of-host-defense
#16
Nardhy Gomez-Lopez, Roberto Romero, Yi Xu, Derek Miller, Ronald Unkel, Majid Shaman, Suzanne M Jacques, Bogdan Panaitescu, Valeria Garcia-Flores, Sonia S Hassan
OBJECTIVE: Neutrophil extracellular traps (NETs) control microbial infections through their antimicrobial activities attributed to DNA, histones, granules, and cytoplasmic proteins (eg, elastase). Intra-amniotic infection is characterized by the influx of neutrophils into the amniotic cavity; therefore, the aim of this study was to determine whether amniotic fluid neutrophils form NETs in this inflammatory process. METHODS: Amniotic fluid samples from women with intra-amniotic infection (n = 15) were stained for bacteria detection using fluorescent dyes...
November 23, 2016: Reproductive Sciences
https://www.readbyqxmd.com/read/27884697/3-cyano-6-5-methyl-3-pyrazoloamino-pyridines-part-2-a-dual-inhibitor-of-aurora-kinase-and-tubulin-polymerization
#17
Masahiko Morioka
A new class of a dual inhibitor of Aurora kinase and tubulin polymerization was created by introducing various substituted phenoxyethylamino or pyridyloxyethylamino groups to the 2-position of 3-cyano-4-methyl-6-(5-methyl-3-pyrazoloamino)-pyridine. Compound 3g exhibited Aurora kinase inhibition, excellent protein kinase selectivity to Aurora kinase in comparison with 66 other kinases, inhibition of phosphorylation of Ser10 of histone H3 as an Aurora kinase inhibitor, inhibition of tubulin polymerization in vitro, good cell membrane permeability, and a good PK profile...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27884646/microrna-92a-3p-regulates-the-expression-of-cartilage-specific-genes-by-directly-targeting-histone-deacetylase-2-in-chondrogenesis-and-degradation
#18
G Mao, Z Zhang, Z Huang, W Chen, G Huang, F Meng, Z Zhang, Y Kang
OBJECTIVE: Increased activity of histone deacetylase 2 (HDAC2) has been found in patients with osteoarthritis (OA) and cartilage matrix degradation and has been shown to mediate the repression of cartilage-specific gene expression in human chondrocytes. We aimed to determine whether microRNA-92a-3p (miR-92a-3p) regulates cartilage-specific gene expression via targeted HDAC2 in chondrogenesis and degradation. METHODS: miR-92a-3p expression was assessed in vitro in a human mesenchymal stem cells (hMSCs) model of chondrogenesis and in normal and OA primary human chondrocytes (PHCs), and in normal and OA human cartilage by in situ hybridization...
November 21, 2016: Osteoarthritis and Cartilage
https://www.readbyqxmd.com/read/27884075/srm-based-measurements-of-proprotein-convertase-subtilisin-kexin-type-9-and-lipoprotein-a-kinetics-in-nonhuman-primate-serum
#19
Fang Xie, Maurice G Emery, John P Gibbs, Dan A Rock, Brooke M Rock
AIM: PCSK9 and Lp(a) have been identified as potential biomarkers for cardiovascular disease. The ability to measure protein turnover rates will provide insights into the dynamic properties of these proteins and lead to better understanding of their biological roles. We aimed to implement the stable isotope-labeled tracers ([(2)H3]-leucine) and develop a novel LC-selected reaction monitoring (SRM) mass spectrometry (MS) method to study the kinetics of PCSK9 and Lp(a). RESULTS: A sensitive method using immunoaffinity enrichment coupled with LC-SRM MS was developed to measure the production and degradation rates of PCSK9 and Lp(a) in naive nonhuman primate serum...
December 2016: Bioanalysis
https://www.readbyqxmd.com/read/27874088/g9a-participates-in-nerve-injury-induced-kcna2-downregulation-in-primary-sensory-neurons
#20
Lingli Liang, Xiyao Gu, Jian-Yuan Zhao, Shaogen Wu, Xuerong Miao, Jifang Xiao, Kai Mo, Jun Zhang, Brianna Marie Lutz, Alex Bekker, Yuan-Xiang Tao
Nerve injury-induced downregulation of voltage-gated potassium channel subunit Kcna2 in the dorsal root ganglion (DRG) is critical for DRG neuronal excitability and neuropathic pain genesis. However, how nerve injury causes this downregulation is still elusive. Euchromatic histone-lysine N-methyltransferase 2, also known as G9a, methylates histone H3 on lysine residue 9 to predominantly produce a dynamic histone dimethylation, resulting in condensed chromatin and gene transcriptional repression. We showed here that blocking nerve injury-induced increase in G9a rescued Kcna2 mRNA and protein expression in the axotomized DRG and attenuated the development of nerve injury-induced pain hypersensitivity...
November 22, 2016: Scientific Reports
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