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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/27930850/elusive-antimony-centered-radical-cations-isolation-characterization-crystal-structures-and-reactivity-studies
#2
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/27926813/perturbation-of-h3k27me3-associated-epigenetic-processes-increases-agrobacterium-mediated-transformation
#3
Hidekazu Iwakawa, Benjamin C Carter, Brett C Bishop, Joe Ogas, Stanton B Gelvin
Agrobacterium-mediated transformation is a core technology for basic plant science and agricultural biotechnology. Improving transformation frequency is a major goal for plant transgenesis. We previously showed that T-DNA insertions in some histone genes decreased transformation susceptibility, whereas overexpression of several Arabidopsis H2A and H4 isoforms increased transformation. Overexpression of several histone H2B and H3 isoforms had little effect on transformation frequency. However, overexpression of histone H3-11 (HTR11) enhanced transformation...
December 7, 2016: Molecular Plant-microbe Interactions: MPMI
https://www.readbyqxmd.com/read/27924151/effect-of-sp600125-on-the-mitotic-spindle-in-hela-cells-leading-to-mitotic-arrest-endoreduplication-and-apoptosis
#4
Donia Mili, Kaouthar Abid, Imed Rjiba, Abderraouf Kenani
BACKGROUND: The JNK inhibitor SP600125 strongly inhibits cell proliferation in many human cancer cells by blocking mitosis progression and inducing cell death. Despite, all this study, the mechanism by which SP600125 inhibits mitosis-related effects in human cervical cells (HeLa cells) remains unclear. In this study, we investigated the effects of SP600125 on the cell viability, cell cycle, and on the spindle assembly during mitosis in HeLa cells. METHODS: To explore this approach, we used a viability test, an immunofluorescence microscopy to detect Histone phosphorylation and mitotic spindle aberrations...
2016: Molecular Cytogenetics
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/27923410/supplementation-with-brazil-nuts-and-green-tea-extract-regulates-targeted-biomarkers-related-to-colorectal-cancer-risk-in-humans
#6
Ying Hu, Graeme H McIntosh, Richard K Le Leu, Roshini Somashekar, Xing Q Meng, Geetha Gopalsamy, Libby Bambaca, Ross A McKinnon, Graeme P Young
Se and green tea have been shown in epidemiological, observational and preclinical studies to be inversely related to the risk of developing colorectal cancer (CRC). However, there are limited studies to evaluate their regulatory effects on genes/proteins that relate to CRC oncogenesis in human subjects, such as selenoproteins, WNT signalling pathway, inflammation and methylation. This study examined the effects of supplementation of Se using Brazil nuts and green tea extract (GTE) capsules, alone and in combination, on targeted biomarkers...
December 7, 2016: British Journal of Nutrition
https://www.readbyqxmd.com/read/27922185/relaxin-family-peptides-structure-activity-relationship-studies
#7
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
#8
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/27908123/spooky-correlations-and-unusual-van-der-waals-forces-between-gapless-and-near-gapless-molecules
#9
John F Dobson, Andreas Savin, János G Ángyán, Ru-Fen Liu
We consider the zero-temperature van der Waals (vdW) interaction between two molecules, each of which has a zero or near-zero electronic gap between a ground state and the first excited state, using a toy model molecule (equilateral H3) as an example. We show that the van der Waals energy between two ground state molecules falls off as D(-3) instead of the usual D(-6) dependence, when the molecules are separated by distance D. We show that this is caused by a perfect "spooky" correlation between the two fluctuating electric dipoles...
November 28, 2016: Journal of Chemical Physics
https://www.readbyqxmd.com/read/27907905/association-of-high-microvessel-%C3%AE-v%C3%AE-3-and-low-pten-with-poor-outcome-in-stage-3-neuroblastoma-rationale-for-using-first-in-class-dual-pi3k-brd4-inhibitor-sf1126
#10
Anat Erdreich-Epstein, Alok R Singh, Shweta Joshi, Francisco M Vega, Pinzheng Guo, Jingying Xu, Susan Groshen, Wei Ye, Melissa Millard, Mihaela Campan, Guillermo Morales, Joseph R Garlich, Peter W Laird, Robert C Seeger, Hiroyuki Shimada, Donald L Durden
Neuroblastoma (NB) is the most common extracranial solid tumor in children. Our previous studies showed that the angiogenic integrin αvβ3 was increased in high-risk metastatic (stage 4) NB compared with localized neuroblastomas. Herein, we show that integrin αvβ3 was expressed on 68% of microvessels in MYCN-amplified stage 3 neuroblastomas, but only on 34% (means) in MYCN-non-amplified tumors (p < 0.001; n = 54). PTEN, a tumor suppressor involved in αvβ3 signaling, was expressed in neuroblastomas either diffusely, focally or not at all (immunohistochemistry)...
November 16, 2016: Oncotarget
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/27901066/greater-efficacy-of-atorvastatin-versus-a-non-statin-lipid-lowering-agent-against-renal-injury-potential-role-as-a-histone-deacetylase-inhibitor
#12
Ravi Shankar Singh, Dharmendra Kumar Chaudhary, Aradhana Mohan, Praveen Kumar, Chandra Prakash Chaturvedi, Carolyn M Ecelbarger, Madan M Godbole, Swasti Tiwari
Statins, 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase inhibitors have been shown to improve diabetic nephropathy. However, whether they provide protection via Histone deacetylases (HDAC) inhibition is not clear. We conducted a comparative evaluation of Atorvastatin (AT) versus the non-statin cholesterol-lowering drug, Ezetimibe (EZT) on severity of diabetic nephropathy. Streptozotocin-treated male Wistar rats were fed a cholesterol-supplemented diet and gavaged daily with vehicle, AT or EZT. Control rats received normal diet and gavaged vehicle (n = 8-9/group)...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27900936/malignant-progression-of-a-histone-h3-3-k27m-mutated-spinal-pilocytic-astrocytoma-in-an-adult
#13
Stefan Reers, David Krug, Walter Stummer, Martin Hasselblatt
No abstract text is available yet for this article.
November 30, 2016: Clinical Neuropathology
https://www.readbyqxmd.com/read/27899915/novel-h7n2-and-h5n6-avian-influenza-a-viruses-in-sentinel-chickens-a-sentinel-chicken-surveillance-study
#14
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/27899151/lung-ultrasound-can-be-used-to-predict-the-potential-of-prone-positioning-and-assess-prognosis-in-patients-with-acute-respiratory-distress-syndrome
#15
Xiao-Ting Wang, Xin Ding, Hong-Min Zhang, Huan Chen, Long-Xiang Su, Da-Wei Liu
BACKGROUND: It is very important to assess the effectiveness of prone positioning (PP) in patients with severe acute respiratory distress syndrome (ARDS). However, it is difficult to identify patients who may benefit from PP. The purpose of this study was to investigate whether prone positioning potential (PPP) can be predicted by lung ultrasound in patients with ARDS. METHODS: In this prospective study, 45 patients with ARDS were included for the assessment of PPP...
November 30, 2016: Critical Care: the Official Journal of the Critical Care Forum
https://www.readbyqxmd.com/read/27894872/synthesis-screening-and-docking-analysis-of-hispolon-analogs-as-potential-antitubercular-agents
#16
Neduri V Balaji, Bollikolla Hari Babu, Gottumukkala V Subbaraju, Kurre Purna Nagasree, Muthyala Murali Krishna Kumar
A series of 20 hispolons/dihydrohispolons were synthesized and characterized by spectral data. These compounds were subjected to in vitro antitubercular activity screening against Mycobacterium tuberculosis (H37Rv) strain. The synthesized compounds showed varied antitubercular activity ranging from 100 to 1.6μg/mL. Among the screened compounds, four compounds (H1, H2, H3 and H15) have shown moderate activity with MIC 25μg/mL. Potent activities were observed for the dihydrohispolon derivative H14 (MIC 1.6μg/mL) followed by H13 (6...
November 18, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27894815/the-histone-variant-h3-3-in-transcriptional-regulation-and-human-disease
#17
REVIEW
Leilei Shi, Hong Wen, Xiaobing Shi
Histone proteins wrap around DNA to form nucleosomes, which further compact into higher order structure of chromatin. In addition to the canonical histones, there are also variant histones that often have pivotal roles in regulating chromatin dynamics and the accessibility of the underlying DNA. H3.3 is the most common non-centromeric variant of histone H3 that differs from the canonical H3 by just 4-5 amino acids. Here we discuss the current knowledge of H3.3 in transcriptional regulation and the recent discoveries and molecular mechanisms of H3...
November 25, 2016: Journal of Molecular Biology
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
#18
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
#19
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
#20
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
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