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https://www.readbyqxmd.com/read/28549890/-18-f-labeled-indole-based-analogs-as-highly-selective-radioligands-for-imaging-sigma-2-receptors-in-the-brain
#1
Liang Wang, Jiajun Ye, Yingfang He, Winnie Deuther-Conrad, Jinming Zhang, Xiaojun Zhang, Mengchao Cui, Jörg Steinbach, Yiyun Huang, Peter Brust, Hongmei Jia
We have designed and synthesized a series of indole-based σ2 receptor ligands containing 5,6-dimethoxyisoindoline or 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline as pharmacophore. In vitro competition binding assays showed that all ten ligands possessed low nanomolar affinity (Ki=1.79-5.23nM) for σ2 receptors and high subtype selectivity (Ki (σ2)/Ki (σ1)=56-708). Moreover, they showed high selectivity for σ2 receptor over the vesicular acetylcholine transporter (>1000-fold). The corresponding radiotracers [(18)F]16 and [(18)F]21 were prepared by an efficient one-pot, two-step reaction sequence with a home-made automated synthesis module, with 10-15% radiochemical yield and radiochemical purity of >99%...
May 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28549090/sigma-1-receptor-regulates-mitochondrial-function-in-glucose-and-oxygen-deprived-retinal-ganglion-cells
#2
Dorette Z Ellis, Linya Li, Yong Park, Shaoqing He, Brett Mueller, Thomas Yorio
Purpose: Understanding the role of mitochondria in retinal ganglion cells (RGCs) is relevant to human disease as studies have shown mitochondrial abnormalities in primary open-angle glaucoma patients. This study seeks to determine the effects of the sigma-1 receptor (σ-1r) and its agonists on mitochondrial function in oxygen- and glucose- deprived (OGD) purified neonatal RGCs. Methods: Retinal ganglion cells were isolated from rat pups and subjected to OGD in varying conditions in the presence or absence of σ-1r agonist and antagonist and following addition of an AAV2-σ-1r vector that was used to increase σ-1r expression...
May 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28548604/quorum-sensing-systems-in-the-plant-growth-promoting-bacterium-paraburkholderia-phytofirmans-psjn-exhibit-cross-regulation-and-are-involved-in-biofilm-formation
#3
Ana Zúñiga, Raúl A Donoso, Daniela Ruiz, Gonzalo A Ruz, Bernardo González
Quorum-sensing systems play important roles in host colonization and host establishment of Burkholderiales species. Beneficial Paraburkholderia species share a conserved quorum-sensing (QS) system, designated BraI/R, that controls different phenotypes. In this context, the plant growth-promoting bacterium Paraburkholderia phytofirmans PsJN possesses two different homoserine lactone QS systems BpI.1/R.1 and BpI.2/R.2 (BraI/R-like QS system). The BpI.1/R.1 QS system was previously reported to be important to colonize and produce beneficial effects in Arabidopsis thaliana plants...
May 26, 2017: Molecular Plant-microbe Interactions: MPMI
https://www.readbyqxmd.com/read/28548042/new-insights-into-reovirus-evolution-implications-from-a-newly-characterized-mycoreovirus
#4
Lijiang Liu, Jiasen Cheng, Yanping Fu, Huiquan Liu, Daohong Jiang, Jiatao Xie
We performed molecular cloning and complete genome sequencing of a novel mycoreovirus, Sclerotinia sclerotiorumreovirus 1 (SsReV1), isolated from an isolate of the phytopathogenic fungus Sclerotinia sclerotiorum. SsReV1 has a genome of 28 055 bp and is composed of 11 double-stranded RNA segments. With a combination of unique molecular features, virion shape and composition, and phylogenetic analysis, SsReV1 is significantly distinct from all known reoviruses and defines a novel genus in the family Reoviridae...
May 26, 2017: Journal of General Virology
https://www.readbyqxmd.com/read/28545064/transcriptomic-analysis-of-the-response-of-pseudomonas-fluorescens-to-epigallocatechin-gallate-by-rna-seq
#5
Xiaoxiang Liu, Bimiao Shen, Peng Du, Nan Wang, Jiaxue Wang, Jianrong Li, Aihua Sun
Epigallocatechin gallate (EGCG) is a main constituent of green tea polyphenols that are widely used as food preservatives and are considered to be safe for consumption. However, the underlying antimicrobial mechanism of EGCG and the bacterial response to EGCG are not clearly understood. In the present study, a genome-wide transcriptional analysis of a typical spoilage bacterium, Pseudomonas fluorescens that responded to EGCG was performed using RNA-seq technology. A total of 26,365,414 and 23,287,092 clean reads were generated from P...
2017: PloS One
https://www.readbyqxmd.com/read/28544475/thiazole-based-sigma-1-receptor-ligands-diversity-by-late-stage-c-h-arylation-of-thiazoles-structure-affinity-and-selectivity-relationships-and-molecular-interactions
#6
Bernhard Wünsch, Artur Kokornaczyk, Dirk Schepmann, Junichiro Yamaguchi, Kenichiro Itami, Erik Laurini, Maurizio Fermeglia, Sabrina Pricl
Spirocyclic thiophene derivatives represent promising sigma-1 ligands with high sigma-1 affinity and selectivity over the sigma-2 subtype. In order to increase ligand efficiency, the thiophene ring was replaced bioisosterically by a thiazole ring and the pyran ring was opened. Late-stage diversification by regioselective C-H arylation of thiazoles 9a-c resulted in a set of 53 compounds with high diversity. This set of compounds was analyzed with respect to sigma-1 affinity, sigma-1/sigma-2 selectivity, lipophilicity (logD7...
May 24, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28538055/high-reliability-principles-must-be-tied-to-value-based-outcomes
#7
Mitchell L Wasden
WellStar Health System and the Medical University of South Carolina (MUSC), highlighted in this issue's feature articles, are two organizations seeking to drive high reliability by educating leaders and incorporating high-reliability principles into their quality improvement (QI) efforts. The organizations have taken slightly different approaches to executing on high reliability, yet both are encouraged by the apparent success of high-reliability principles in other industries.The high-reliability framework is often applied to healthcare despite the limitations of comparing healthcare organizations to nuclear reactors, commercial airlines, and aircraft carriers...
July 2017: Frontiers of Health Services Management
https://www.readbyqxmd.com/read/28537605/factors-affecting-bubble-size-in-ionic-liquids
#8
Sarah F R Taylor, Stuart A Brittle, Pratik Desai, Johan Jacquemin, Christopher Hardacre, William A Zimmerman
This study reports on understanding the formation of bubbles in ionic liquids (ILs), with a view to utilising ILs more efficiently in gas capture processes. In particular, the impact of the IL structure on the bubble sizes obtained has been determined in order to obtain design principles for the ionic liquids utilised. 11 ILs were used in this study with a range of physico-chemical properties in order to determine parametrically the impact on bubble size due to the liquid properties and chemical moieties present...
May 24, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28531088/influence-of-patient-mispositioning-on-sar-distribution-and-simulated-temperature-in-regional-deep-hyperthermia
#9
Bassim Aklan, Pia Gierse, Josefin Hartmann, Oliver J Ott, Rainer Fietkau, Christoph Bert
Patient positioning plays an important role in regional deep hyperthermia to obtain a successful hyperthermia treatment. In this study, the influence of possible patient mispositioning was systematically assessed on specific absorption rate (SAR) and temperature distribution. With a finite difference time domain approach, the SAR and temperature distributions were predicted for six patients at 312 positions. Patient displacements and rotations as well as the combination of both were considered inside the Sigma-Eye applicator...
May 22, 2017: Physics in Medicine and Biology
https://www.readbyqxmd.com/read/28526785/effects-of-arginine-on-growth-virulence-gene-expression-and-stress-tolerance-by-streptococcus-mutans
#10
Brinta Chakraborty, Robert A Burne
Streptococcus mutans is a common constituent of oral biofilms and a primary etiologic agent of human dental caries. The bacteria associated with dental caries have a potent ability to produce organic acids from dietary carbohydrates and to grow and metabolize in acidic conditions. In contrast, many commensal bacteria produce ammonia through the arginine deiminase system (ADS), which moderates the pH of oral biofilms. Arginine metabolism by the ADS is a significant deterrent to the initiation and progression of dental caries...
May 19, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28525360/role-of-sigma-1-receptor-in-high-fat-diet-induced-peripheral-neuropathy
#11
Tieying Song, Jianhui Zhao, Xiaojing Ma, Zaiwang Zhang, Bo Jiang, Yunliang Yang
The neurobiological mechanisms of obesity-induced peripheral neuropathy are poorly understood. We evaluated the role of Sigma-1 receptor (Sig-1R) and NMDA receptor (NMDARs) in the spinal cord in peripheral neuropathy using an animal model of high fat diet-induced diabetes. We examined the expression of Sig-1R and NMDAR subunits GluN2A and GluN2B along with postsynaptic density protein 95 (PSD-95) in the spinal cord after 24- week HFD treatment in both wild-type and Sig-1R-/- mice. Finally, we examined the effects of repeated intrathecal administrations of selective Sig-1R antagonists BD1047 in HFD-fed wild-type mice on peripheral neuropathy...
May 19, 2017: Biological Chemistry
https://www.readbyqxmd.com/read/28524089/green-synthesized-zinc-oxide-zno-nanoparticles-induce-oxidative-stress-and-dna-damage-in-lathyrus-sativus-l-root-bioassay-system
#12
Kamal K Panda, Dambaru Golari, A Venugopal, V Mohan M Achary, Ganngam Phaomei, Narasimham L Parinandi, Hrushi K Sahu, Brahma B Panda
Zinc oxide nanoparticles (ZnONP-GS) were synthesised from the precursor zinc acetate (Zn(CH₃COO)₂) through the green route using the milky latex from milk weed (Calotropis gigantea L. R. Br) by alkaline precipitation. Formation of the ZnONP-GS was monitored by UV-visible spectroscopy followed by characterization and confirmation by energy-dispersive X-ray spectroscopy (EDX), transmission electron microscopy (TEM), and X-ray diffraction (XRD). Both the ZnONP-GS and the commercially available ZnONP-S (Sigma-Aldrich) and cationic Zn(2+) from Zn(CH₃COO)₂ were tested in a dose range of 0-100 mg·L(-1) for their potency (i) to induce oxidative stress as measured by the generation reactive oxygen species (ROS: O₂(•-), H₂O₂ and (•)OH), cell death, and lipid peroxidation; (ii) to modulate the activities of antioxidant enzymes: catalase (CAT), superoxide dismutase (SOD), guaiacol peroxidase (GPX), and ascorbate peroxidase (APX); and (iii) to cause DNA damage as determined by Comet assay in Lathyrus sativus L...
May 18, 2017: Antioxidants (Basel, Switzerland)
https://www.readbyqxmd.com/read/28522802/proteome-remodelling-by-the-stress-sigma-factor-rpos-%C3%AF-s-in-salmonella-identification-of-small-proteins-and-evidence-for-post-transcriptional-regulation
#13
Magali Lago, Véronique Monteil, Thibaut Douche, Julien Guglielmini, Alexis Criscuolo, Corinne Maufrais, Mariette Matondo, Françoise Norel
The RpoS/σ(S) sigma subunit of RNA polymerase is the master regulator of the general stress response in many Gram-negative bacteria. Extensive studies have been conducted on σ(S)-regulated gene expression at the transcriptional level. In contrast, very limited information regarding the impact of σ(S) on global protein production is available. In this study, we used a mass spectrometry-based proteomics approach to explore the wide σ(S)-dependent proteome of the human pathogen Salmonella enterica serovar Typhimurium...
May 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28507242/an-rpohi-dependent-response-promotes-outgrowth-after-extended-stationary-phase-in-the-alphaproteobacterium-rhodobacter-sphaeroides
#14
B Remes, T Rische-Grahl, K M H Müller, K U Förstner, Y Sung-Huan, L Weber, A Jäger, V Peuser, G Klug
Under unfavorable growth conditions, bacteria enter stationary phase and can maintain cell viability over prolonged periods with no increase in cell number. To get insights into the regulatory mechanisms that allow bacteria to resume growth when conditions become favorable again (outgrowth) we performed global transcriptome analyses at different stages of growth for the alphaproteobacterium Rhodobacter sphaeroides The majority of genes was not differentially expressed across growth phases. After short stationary phase (about 20 h after growth starts to slow down), only 7 % of the genes showed altered expression (fold change of > 1...
May 15, 2017: Journal of Bacteriology
https://www.readbyqxmd.com/read/28495886/the-sigma-1-receptor-modulates-dopamine-transporter-conformation-and-cocaine-binding-and-may-thereby-potentiate-cocaine-self-administration-in-rats
#15
Weimin Conrad Hong, Hideaki Yano, Takato Hiranita, Frederick T Chin, Christopher R McCurdy, Tsung-Ping Su, Susan G Amara, Jonathan L Katz
The dopamine transporter (DAT) regulates dopamine (DA) neurotransmission by recapturing DA into the presynaptic terminals, and is a principal target of the psychostimulant cocaine. The sigma-1 receptor (σ1R) is a molecular chaperone, and its ligands have been shown to modulate dopamine neuronal signaling, although their effects on DAT activity are unclear. Here, we report that the prototypical σ1R agonist (+)-pentazocine potentiated the dose response of cocaine self-administration in rats, consistent with effects of the σR agonists PRE-084 and DTG reported previously...
May 11, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28493522/national-survey-on-turnaround-time-of-clinical-biochemistry-tests-in-738-laboratories-in-china
#16
Xiaoyan Zhang, Yang Fei, Wei Wang, Haijian Zhao, Minqi Wang, Bingquan Chen, Jie Zhou, Zhiguo Wang
BACKGROUND: This survey was initiated to estimate the current status of turnaround time (TAT) monitoring of clinical biochemistry in China, provide baseline data for establishment of quality specifications and analyze the impact factors of TAT. METHODS: 738 laboratories were included. Questionnaires involved general information and data of related indicators of TAT during 1 week were provided to participating laboratories. Nine quality indicators were covered, which were medians, 90th and outlier rates of pre-examination, examination, and post-examination TAT...
May 11, 2017: Journal of Clinical Laboratory Analysis
https://www.readbyqxmd.com/read/28476021/association-of-body-mass-index-with-er-pr-and-14-3-3%C3%AF-expression-in-tumor-and-stroma-of-type-i-and-type-ii-endometrial-carcinoma
#17
Joseph F Peevey, Brandon-Luke L Seagle, Kruti P Maniar, J Julie Kim
Obesity is a prominent risk factor for endometrial cancer (EC) and can impede on surgical and hormonal treatments. Markers of EC, estrogen receptor (ER), progesterone receptor (PR), phospho(Ser473)-AKT (pAKT) and 14-3-3 sigma (14-3-3σ) were measured in EC tissues in both the tumor and stroma and grouped by body mass index (BMI). Immunohistochemical scoring of 82 cases of Type 1 and Type II EC tissues revealed a significantly increased tumor expression of ER, PR and 14-3-3σ in women with Type I (BMI < 40) as compared to Type II (BMI < 30) EC...
April 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28470136/reducing-patients-falls-rate-in-an-academic-medical-center-amc-using-six-sigma-dmaic-approach
#18
Ahmed Al Kuwaiti, Arun Vijay Subbarayalu
Purpose The purpose of this paper is to evaluate the impact of adopting the Six Sigma define, measure, analyze, improve and control (DMAIC) approach in reducing patients fall rate in an Academic Medical Center, Saudi Arabia. Design/methodology/approach A prospective study design was adopted and this study was conducted at King Fahd Hospital of the University (KFHU) during the year 2014. Based on the historical data of the patients' falls reported at KFHU during the year 2013, the goal was fixed to reduce the falls rate from 7...
May 8, 2017: International Journal of Health Care Quality Assurance
https://www.readbyqxmd.com/read/28469104/investigation-and-analysis-of-hemoglobin-a1c-measurement-systems-performance-for-135-laboratories-in-china
#19
Hai-Jian Zhao, Tian-Jiao Zhang, Jie Zeng, Cui-Hua Hu, Rong Ma, Chuan-Bao Zhang
BACKGROUND: Hemoglobin A1c (HbA1c) measurement is of great value for the diagnosis and monitoring of diabetes. Many manufacturers have developed various experiments to determine the HbA1c concentration. However, the longitudinal use of these tests requires strict quality management. This study aimed to analyze the quality of HbA1c measurement systems in China using six sigma techniques to help improve their performances. METHODS: A total of 135 laboratories were involved in this investigation in 2015...
May 5, 2017: Chinese Medical Journal
https://www.readbyqxmd.com/read/28456572/treatment-with-sodium-nitroprusside-improves-the-endothelial-function-in-aortic-rings-with-endothelial-dysfunction
#20
Tereza Cristina Buzinari, Jorge Camargo Oishi, Thiago Francisco De Moraes, Izabela Pereira Vatanabe, Heloisa Sobreiro Selistre-de-Araújo, Cezar Rangel Pestana, Gerson Jhonatan Rodrigues
PURPOSE: Verify if sodium nitroprusside (SNP) is able to improve endothelial function and if this effect is independent of nitric oxide (NO) release of the compound. METHODS: Normotensive (2K) and hypertensive (2K-1C) wistar rats were used. Intact endothelium aortas were placed in a myograph and incubated with SNP: 0.1nM; 1nM or 10nM during 30min. Cumulative concentration-effect curves for acetylcholine (Ach) were realized to measure the relaxing capacity. Intracellular NO were measured (by DAF-2DA probe) in HUVEC treated with SNP 0...
April 27, 2017: European Journal of Pharmaceutical Sciences
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