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https://www.readbyqxmd.com/read/28088086/design-and-synthesis-of-new-raf-kinase-inhibiting-antiproliferative-quinoline-derivatives-part-2-diarylurea-derivatives
#1
Mohammed I El-Gamal, Mohammad Ashrafuddin Khan, Hamadeh Tarazi, Mohammed S Abdel-Maksoud, Mahmoud M Gamal El-Din, Kyung Ho Yoo, Chang-Hyun Oh
This article describes the design, synthesis, and biological screening of a new series of diarylurea derivatives possessing quinoline nucleus. Nine target compounds were selected by the National Cancer Institute (NCI, Bethesda, Maryland, USA) for in vitro antiproliferative screening against a panel of 58 cancer cell lines of nine cancer types. Following one-dose initial screening, compounds 1d-g and 2b were selected for 5-dose screening in order to calculate their IC50 and total growth inhibition (TGI) values against the cell lines...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28088078/genetically-tailored-magnetosomes-used-as-mri-probe-for-molecular-imaging-of-brain-tumor
#2
M Boucher, F Geffroy, S Prévéral, L Bellanger, E Selingue, G Adryanczyk-Perrier, M Péan, C T Lefèvre, D Pignol, N Ginet, S Mériaux
We investigate here the potential of single step production of genetically engineered magnetosomes, bacterial biogenic iron-oxide nanoparticles embedded in a lipid vesicle, as a new tailorable magnetic resonance molecular imaging probe. We demonstrate in vitro the specific binding and the significant internalization into U87 cells of magnetosomes decorated with RGD peptide. After injection at the tail vein of glioblastoma-bearing mice, we evidence in the first 2 h the rapid accumulation of both unlabeled and functionalized magnetosomes inside the tumor by Enhanced Permeability and Retention effects...
December 19, 2016: Biomaterials
https://www.readbyqxmd.com/read/28088040/listen-up-developmental-differences-in-the-impact-of-ids-on-speech-segmentation
#3
Melanie S Schreiner, Nivedita Mani
While American English infants typically segment words from fluent speech by 7.5-months, studies of infants from other language backgrounds have difficulty replicating this finding. One possible explanation for this cross-linguistic difference is that the input infants from different language backgrounds receive is not as infant-directed as American English infant-directed speech (Floccia et al., 2016). Against this background, the current study investigates whether German 7.5- and 9-month-old infants segment words from fluent speech when the input is prosodically similar to American English IDS...
January 11, 2017: Cognition
https://www.readbyqxmd.com/read/28088024/multi-year-record-of-atmospheric-and-snow-surface-nitrate-in-the-central-antarctic-plateau
#4
R Traversi, S Becagli, M Brogioni, L Caiazzo, V Ciardini, F Giardi, M Legrand, G Macelloni, B Petkov, S Preunkert, C Scarchilli, M Severi, V Vitale, R Udisti
Continuous all year-round samplings of atmospheric aerosol and surface snow at high (daily to 4-day) resolution were carried out at Dome C since 2004-05 to 2013 and nitrate records are here presented. Basing on a larger statistical data set than previous studies, results confirm that nitrate seasonal pattern is characterized by maxima during austral summer for both aerosol and surface snow, occurring in-phase with solar UV irradiance. This temporal pattern is likely due to a combination of nitrate sources and post-depositional processes whose intensity usually enhances during the summer...
December 30, 2016: Chemosphere
https://www.readbyqxmd.com/read/28088018/antibacterial-serine-protease-from-wrightia-tinctoria-purification-and-characterization
#5
Sakthivel Muthu, Venkatesh Babu Gopal, Selvakumar Soundararajan, Karthikeyan Nattarayan, Karthik S Narayan, Mythileeswari Lakshmikanthan, Sathuvan Malairaj, Palani Perumal
A serine protease was purified from the leaves of Wrightia tinctoria by sequential flow through method comprising screening, optimization, ammonium sulfate precipitation, gel filtration and ion exchange column chromatography. The yield and purification fold obtained were 11.58% and 9.56 respectively. A single band of serine protease was visualized on SDS-PAGE and 2-D gel electrophoretic analyses were revealed with the molecular mass of 38.5 kDa. Serine protease had an optimum pH of 8.0 and was stable at 45°C with high relative protease activity...
January 3, 2017: Plant Physiology and Biochemistry: PPB
https://www.readbyqxmd.com/read/28087972/lack-of-effect-of-oral-cabotegravir-on-the-pharmacokinetics-of-a-levonorgestrel-ethinyl-estradiol-containing-oral-contraceptive-in-healthy-adult-females
#6
C Trezza, S L Ford, E Gould, Y Lou, C Huang, J M Ritter, A M Buchanan, W Spreen, P Patel
AIM(S): This study aimed to investigate whether cabotegravir (CAB), an integrase inhibitor in development for treatment and prevention of HIV-1, influences the pharmacokinetics (PK) of a levonorgestrel (LNG) and ethinyl estradiol (EE)-containing oral contraceptive (OC) in healthy women. METHODS: In this open-label, fixed-sequence crossover study, healthy female subjects received LNG 0.15 mg/EE 0.03 mg tablet once daily Days 1-10 alone and with oral CAB 30 mg once daily Days 11-21...
January 14, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28087930/fungal-ecology-principles-and-mechanisms-of-colonization-and-competition-by-saprotrophic-fungi
#7
Lynne Boddy, Jennifer Hiscox
Decomposer fungi continually deplete the organic resources they inhabit, so successful colonization of new resources is a crucial part of their ecology. Colonization success can be split into (i) the ability to arrive at, gain entry into, and establish within a resource and (ii) the ability to persist within the resource until reproduction and dissemination. Fungi vary in their life history strategies, the three main drivers of which are stress (S-selected), disturbance (ruderal, or R-selected), and incidence of competitors (C-selected); however, fungi often have combinations of characteristics from different strategies...
December 2016: Microbiology Spectrum
https://www.readbyqxmd.com/read/28087928/factors-associated-with-non-completion-of-follow-up-33-month-latent-tuberculous-infection-treatment-trial
#8
R N Moro, T R Sterling, J Saukkonen, A Vernon, C R Horsburgh, R E Chaisson, C D Hamilton, M E Villarino, S Goldberg
<h2>SETTING:</h2><p>A post-hoc exploratory analysis of a randomized, open-label clinical trial thatenrolled 8053 participants from the United States, Canada, Brazil, and Spain.</p><h2>OBJECTIVE:</h2><p>To assess factors associated with non-completion of study follow-up (NCF) in a 33-month latent tuberculous infection treatment trial, PREVENT TB.</p><h2>DESIGN:</h2><p>Participants were randomized to receive 3 months of weekly directly observed therapy vs...
January 13, 2017: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/28087823/prognosis-of-carotid-dissecting-aneurysms-results-from-cadiss-and-a-systematic-review
#9
Susanna C Larsson, Alice King, Jeremy Madigan, Christopher Levi, John W Norris, Hugh S Markus
OBJECTIVE: To determine the natural history of dissecting aneurysm (DA) and whether DA is associated with an increased recurrent stroke risk and whether type of antithrombotic drugs (antiplatelets vs anticoagulants) modifies the persistence or development of DA. METHODS: We included 264 patients with extracranial cervical artery dissection (CAD) from the Cervical Artery Dissection in Stroke Study (CADISS), a multicenter prospective study that compared antiplatelet with anticoagulation therapy...
January 13, 2017: Neurology
https://www.readbyqxmd.com/read/28087810/akt1-lkb1-and-yap1-revealed-as-myc-interactors-with-nanoluc-based-protein-fragment-complementation-assay
#10
Xiu-Lei Mo, Qi Qi, Andrei A Ivanov, Qiankun Niu, Yin Luo, Jonathan Havel, Russell Goetze, Sydney Bell, Carlos S Moreno, Lee A D Cooper, Margaret A Johns, Fadlo R Khuri, Yuhong Du, Haian Fu
The c-Myc (MYC) transcription factor is a major cancer driver and a well-validated therapeutic target. However, directly targeting MYC has been challenging. Thus, identifying proteins that interact with and regulate MYC may provide alternative strategies to inhibit its oncogenic activity. Here we report the development of a NanoLuc®-based protein-fragment complementation assay (NanoPCA) and mapping of the MYC protein interaction hub in live mammalian cells. The NanoPCA system was configured to enable detection of protein-protein interactions (PPI) at the endogenous level, as shown with PRAS40 dimerization, and detection of weak interactions, such as PINCH1-NCK2...
January 13, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28087807/field-validation-of-the-los-angeles-motor-scale-as-a-tool-for-paramedic-assessment-of-stroke-severity
#11
Joon-Tae Kim, Pil-Wook Chung, Sidney Starkman, Nerses Sanossian, Samuel J Stratton, Marc Eckstein, Frank D Pratt, Robin Conwit, David S Liebeskind, Latisha Sharma, Lucas Restrepo, May-Kim Tenser, Miguel Valdes-Sueiras, Jeffrey Gornbein, Scott Hamilton, Jeffrey L Saver
BACKGROUND AND PURPOSE: The Los Angeles Motor Scale (LAMS) is a 3-item, 0- to 10-point motor stroke-deficit scale developed for prehospital use. We assessed the convergent, divergent, and predictive validity of the LAMS when performed by paramedics in the field at multiple sites in a large and diverse geographic region. METHODS: We analyzed early assessment and outcome data prospectively gathered in the FAST-MAG trial (Field Administration of Stroke Therapy-Magnesium phase 3) among patients with acute cerebrovascular disease (cerebral ischemia and intracranial hemorrhage) within 2 hours of onset, transported by 315 ambulances to 60 receiving hospitals...
January 13, 2017: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/28087784/interactions-between-zinc-and-allosteric-modulators-of-the-glycine-receptor
#12
Garrett L Cornelison, Anna W Daszkowski, Natasha C Pflanz, S John Mihic
The glycine receptor is a pentameric ligand-gated ion channel involved in fast inhibitory neurotransmission in the central nervous system. Zinc is an allosteric modulator of glycine receptor function, enhancing the effects of glycine at nM to low μM concentrations, and inhibiting its effects at higher concentrations. Low nM concentrations of contaminating zinc in electrophysiological buffers are capable of synergistically enhancing receptor modulation by other compounds such as ethanol. This suggests that, unless accounted for, previous studies of glycine receptor modulation were measuring the effects of modulator plus co-modulation by zinc on receptor function...
January 13, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28087780/oncogenes-without-a-neighboring-tumor-suppressor-gene-are-more-prone-to-amplification
#13
William K K Wu, Xiangchun Li, Xiansong Wang, Rudin Z W Dai, Alfred S L Cheng, Maggie H T Wang, Thomas Kwong, Tai C Chow, Jun Yu, Matthew T V Chan, Sunny H Wong
Focal copy number gains or losses are important genomic hallmarks of cancer. The genomic distribution of oncogenes and tumor-suppressor genes (TSG) in relation to focal copy number aberrations is unclear. Our analysis revealed that the mean distance of TSGs from oncogenes was significantly shorter than that of non-cancer genes, suggesting that oncogenes and TSGs tend to be in close physical proximity in the human genome. Such relationship was conserved in mouse and drosophila. Pan-cancer analysis using data from The Cancer Genome Atlas indicated that oncogenes without a nearby TSG are more prone to amplification...
January 12, 2017: Molecular Biology and Evolution
https://www.readbyqxmd.com/read/28087758/method-for-the-determination-of-carbonyl-compounds-in-e-cigarette-aerosols
#14
Jason W Flora, Celeste T Wilkinson, James W Wilkinson, Peter J Lipowicz, James A Skapars, Adam Anderson, John H Miller
Low levels of thermal degradation products such as carbonyls (formaldehyde, acetaldehyde, acrolein, crotonaldehyde) have been reported in e-cigarette aerosols. The collection and analysis of e-cigarette aerosol carbonyls are often adapted from methods developed for tobacco cigarette smoke. These methodologies are often not sensitive enough to detect low carbonyl levels in e-cigarette aerosols. One objective of this work was to develop and validate a rapid, selective and sensitive ultra-performance liquid chromatography with mass spectrometry method optimized for analysis of carbonyls in e-cigarette aerosols...
February 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28087661/disturbance-by-an-endemic-rodent-in-an-arid-shrubland-is-a-habitat-filter-effects-on-plant-invasion-and-taxonomical-functional-and-phylogenetic-community-structure
#15
Víctor M Escobedo, Rodrigo S Rios, Cristian Salgado-Luarte, Gisela C Stotz, Ernesto Gianoli
BACKGROUND AND AIMS: Disturbance often drives plant invasion and may modify community assembly. However, little is known about how these modifications of community patterns occur in terms of taxonomic, functional and phylogenetic structure. This study evaluated in an arid shrubland the influence of disturbance by an endemic rodent on community functional divergence and phylogenetic structure as well as on plant invasion. It was expected that disturbance would operate as a habitat filter favouring exotic species with short life cycles...
January 12, 2017: Annals of Botany
https://www.readbyqxmd.com/read/28087646/wheat-genotypes-with-combined-resistance-to-wheat-curl-mite-wheat-streak-mosaic-virus-wheat-mosaic-virus-and-triticum-mosaic-virus
#16
Wen-Po Chuang, Lina Maria Aguirre Rojas, Luaay Kahtan Khalaf, Guorong Zhang, Allan K Fritz, Anna E Whitfield, C Michael Smith
The wheat curl mite, Aceria tosichella Keifer, (WCM) is a global pest of bread wheat that reduces yields significantly. In addition, WCM carries Wheat streak mosaic virus (WSMV, family Potyviridae, genus Tritimovirus), the most significant wheat virus in North America; High Plains wheat mosaic virus (HPWMoV, genus Emaravirus, formerly High plains virus); and Triticum mosaic virus (TriMV, family Potyviridae, genus Poacevirus). Viruses carried by WCM have reduced wheat yields throughout the U.S. Great Plains for >50 yr, with average yield losses of 2-3% and occasional yield losses of 7-10%...
January 13, 2017: Journal of Economic Entomology
https://www.readbyqxmd.com/read/28087622/calmodulin-limits-pathogenic-na-channel-persistent-current
#17
Haidun Yan, Chaojian Wang, Steven O Marx, Geoffrey S Pitt
Increased "persistent" current, caused by delayed inactivation, through voltage-gated Na(+) (NaV) channels leads to cardiac arrhythmias or epilepsy. The underlying molecular contributors to these inactivation defects are poorly understood. Here, we show that calmodulin (CaM) binding to multiple sites within NaV channel intracellular C-terminal domains (CTDs) limits persistent Na(+) current and accelerates inactivation across the NaV family. Arrhythmia or epilepsy mutations located in NaV1.5 or NaV1.2 channel CTDs, respectively, reduce CaM binding either directly or by interfering with CTD-CTD interchannel interactions...
January 13, 2017: Journal of General Physiology
https://www.readbyqxmd.com/read/28087614/usefulness-of-ftir-spectroscopy-to-distinguish-rough-and-smooth-variants-of-lactobacillus-farciminis-cncm-i-3699
#18
R Tareb, M Bernardeau, C Amiel, J P Vernoux
In this study, the potential of FTIR spectroscopy for assessing putative biochemical and structural differences between the two variants Rough (R) and Smooth (S) of Lactobacillus farciminis CNCM-I-3699, a pleomorphic strain, was investigated. The main differences observed were localized in the polysaccharide (1200-900 cm(-1)) and protein (1700-1500 cm(-1)) regions. Based on spectral information in these two spectral ranges, clustering resulted in a dendrogram that showed a clear discrimination between both morphotypes...
January 12, 2017: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/28087600/sunitinib-stimulates-expression-of-vegfc-by-tumor-cells-and-promotes-lymphangiogenesis-in-clear-cell-renal-cell-carcinomas
#19
Maeva Dufies, Sandy Giuliano, Damien Ambrosetti, Audrey Claren, Papa Diogop Ndiaye, Michalis Mastri, Walid Moghrabi, Lindsay S Cooley, Marc Ettaiche, Emmanuel Chamorey, Julien Parola, Valerie Vial, Marilena Lupu-Plesu, Jean-Christophe Bernhard, Alain Ravaud, Delphine Borchiellini, Jean Marc Ferrero, Andreas Bikfalvi, John M L Ebos, Khalid S A Khabar, Renaud Grepin, Gilles Pagès
Sunitinib is an antiangiogenic therapy given as a first-line treatment for renal cell carcinoma (RCC). While treatment improves progression-free survival, most patients relapse. We hypothesized that patient relapse can stem from the development of a lymphatic network driven by the production of the main growth factor for lymphatic endothelial cells, vascular endothelial growth factor C (VEGFC). In this study, we found that sunitinib can stimulate VEGFC gene transcription and increase VEGFC mRNA half-life. Additionally, sunitinib activated p38 MAP kinase, which resulted in the upregulation/activity of HuR and inactivation of tristetraprolin, two AU-rich-element binding proteins...
January 13, 2017: Cancer Research
https://www.readbyqxmd.com/read/28087587/association-between-dietary-intake-and-school-valued-outcomes-a-scoping-review
#20
H S K Chan, C Knight, M Nicholson
Approximately one in four Australian children aged 5-17 years are overweight or obese. Most of the health effects of overweight and obesity in childhood do not eventuate until into adulthood; therefore, motivation for children to have a healthy diet may be low. This scoping review examined the literature for associations between diet quality in 5-18 year olds and 'school-valued' outcomes including student attendance, academic performance, behaviour at school and mental health. A literature search for studies that assessed dietary intake and at least one 'school-valued' outcome in schoolchildren, in highly developed countries was conducted...
January 13, 2017: Health Education Research
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