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https://www.readbyqxmd.com/read/29240675/improvement-of-gaofen-3-absolute-positioning-accuracy-based-on-cross-calibration
#1
Mingjun Deng, Guo Zhang, Ruishan Zhao, Shaoning Li, Jiansong Li
The Chinese Gaofen-3 (GF-3) mission was launched in August 2016, equipped with a full polarimetric synthetic aperture radar (SAR) sensor in the C-band, with a resolution of up to 1 m. The absolute positioning accuracy of GF-3 is of great importance, and in-orbit geometric calibration is a key technology for improving absolute positioning accuracy. Conventional geometric calibration is used to accurately calibrate the geometric calibration parameters of the image (internal delay and azimuth shifts) using high-precision ground control data, which are highly dependent on the control data of the calibration field, but it remains costly and labor-intensive to monitor changes in GF-3's geometric calibration parameters...
December 14, 2017: Sensors
https://www.readbyqxmd.com/read/29239853/averaged-head-phantoms-from-magnetic-resonance-images-of-korean-children-and-young-adults
#2
Miran Han, Ae-Kyoung Lee, Hyung-Do Choi, Yong Wook Jung, Jin Seo Park
Increased use of mobile phones raises concerns about the health risks of electromagnetic radiation. Phantom heads are routinely used for radiofrequency dosimetry simulations, and the purpose of this study was to construct averaged phantom heads for children and young adults. Using magnetic resonance images (MRI), sectioned cadaver images, and a hybrid approach, we initially built template phantoms representing 6-, 9-, 12-, 15-year-old children and adult. Our subsequent approach revised the template phantoms using 29 averaged items that were identified by averaging the MRI data from 500 children and young adults...
December 14, 2017: Physics in Medicine and Biology
https://www.readbyqxmd.com/read/29238987/modeling-the-effect-of-platelet-concentrate-supernatants-on-endothelial-cells-focus-on-endocan-esm-1
#3
Sofiane Tariket, Caroline Sut, Charles-Antoine Arthaud, Marie-Ange Eyraud, Astrid Meneveaux, Sandrine Laradi, Hind Hamzeh-Cognasse, Olivier Garraud, Fabrice Cognasse
BACKGROUND: Platelets (PLTs) are prone to activation and the release of biologic response modifiers (BRMs) under storage conditions. The transfusion inflammatory reaction in the vascular compartment involves endothelial cell activation due to cell-cell interactions and BRMs infused with the blood products. Endocan/ESM-1 is a proteoglycan secreted by endothelial cells under the control of proinflammatory cytokines. We aimed to measure endocan activity in supernatants of PLT components (PCs), implicated in serious adverse reactions (SARs) or not (no...
December 13, 2017: Transfusion
https://www.readbyqxmd.com/read/29238524/functional-redundancy-modifies-species-area-relationship-for-freshwater-phytoplankton
#4
Gábor Várbíró, Judit Görgényi, Béla Tóthmérész, Judit Padisák, Éva Hajnal, Gábor Borics
Although species-area relationship (SAR) is among the most extensively studied patterns in ecology, studies on aquatic and/or microbial systems are seriously underrepresented in the literature. We tested the algal SAR in lakes, pools and ponds of various sizes (10-2-108 m2) and similar hydromorphological and trophic characteristics using species-specific data and functional groups. Besides the expectation that species richness increases monotonously with area, we found a right-skewed hump-shaped relationship between the area and phytoplankton species richness...
December 2017: Ecology and Evolution
https://www.readbyqxmd.com/read/29237834/structural-basis-for-the-inhibition-of-host-gene-expression-by-porcine-epidemic-diarrhea-virus-nsp1
#5
Zhou Shen, Gang Ye, Feng Deng, Gang Wang, Min Cui, Liurong Fang, Shaobo Xiao, Zhen F Fu, Guiqing Peng
Porcine epidemic diarrhea virus (PEDV), an enteropathogenic Alphacoronavirus, has caused enormous economic losses in the pork industry. The non-structural protein 1 (nsp1) is a characteristic feature of Alpha- and Beltacoronaviruses, which exhibits both functional conservation and mechanistic diversity in inhibiting host gene expression and antiviral responses. However, the detailed structure and molecular mechanisms underlying the Alphacoronavirus nsp1 inhibition of host gene expression remain unclear. Here, we report the first full-length crystal structure of Alphacoronavirus nsp1 from PEDV...
December 13, 2017: Journal of Virology
https://www.readbyqxmd.com/read/29232885/design-synthesis-and-fungicidal-activity-of-novel-thiosemicarbazide-derivatives-containing-piperidine-fragments
#6
Xuebo Zhang, Peng Lei, Tengda Sun, Xiaoyu Jin, Xinling Yang, Yun Ling
In order to discover novel eco-friendly lead compounds for plant pathogenic fungi control, a series of benzaldehyde thiosemicarbazide derivatives with a piperidine moiety have been designed and synthesized. Fungicidal activities of all the synthesized compounds were evaluated in vitro. The results indicated that all the title compounds exhibited moderate to good fungicidal activities. Compound 3b displayed excellent activities against Pythium aphanidermatum, Rhizoctonia solani, Valsa mali, and Gaeu-mannomyces graminsis, with EC50 values lower than 10 μg/mL...
December 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29232514/discovery-of-novel-selective-acetyl-coa-carboxylase-acc-1-inhibitors
#7
Ryo Mizojiri, Moriteru Asano, Daisuke Tomita, Hiroshi Banno, Noriyuki Nii, Masako Sasaki, Hiroyuki Sumi, Yoshihiko Satoh, Yukiko Yamamoto, Takeo Moriya, Yoshinori Satomi, Hironobu Maezaki
We initiated our structure-activity relationship (SAR) studies for selective ACC1 inhibitors from 1a as a lead compound. SAR studies of bicyclic scaffolds revealed many potent and selective ACC1 inhibitors represented by 1f, however most of them had physicochemical issues, particularly low aqueous solubility and potent CYP inhibition. To address these two issues and improve the drug-likeness of this chemical series, we converted the bicyclic scaffold into a monocyclic framework. Ultimately, this lead us to discover a novel monocyclic derivative 1q as a selective ACC1 inhibitor, which showed highly potent and selective ACC1 inhibition as well as acceptable solubility and CYP inhibition profiles...
December 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29232162/efficacy-and-safety-of-biosimilar-sar342434-insulin-lispro-in-adults-with-type-2-diabetes-also-using-insulin-glargine-sorella-2-study
#8
Karl-Michael Derwahl, Timothy S Bailey, Karin Wernicke-Panten, Lin Ping, Suzanne Pierre
BACKGROUND: SAR342434 (SAR-Lis) is a biosimilar (follow-on) of insulin lispro (U100; Humalog®; Ly-Lis). This study aimed to show similar efficacy, safety, and immunogenicity of SAR-Lis versus Ly-Lis in adult patients with type 2 diabetes mellitus (T2DM) treated with multiple daily injections, while using insulin glargine (GLA-100; Lantus®) as basal insulin. METHODS: SORELLA 2 was a 6-month, randomized, open-label, Phase 3 study (NCT02294474). Insulin doses were adjusted to achieve fasting and 2-h postprandial glucose targets according to American Diabetes Association guidelines...
December 12, 2017: Diabetes Technology & Therapeutics
https://www.readbyqxmd.com/read/29229225/design-synthesis-and-pharmacological-evaluation-of-new-acyl-sulfonamides-as-potent-and-selective-bcl-2-inhibitors
#9
Xiaohua Liu, Yu Zhang, Wenjing Huang, Wenfu Tan, Ao Zhang
The antiapoptotic protein Bcl-2, overexpressed in many tumor cells, is an attractive target for potential small molecule anticancer drug discovery. Herein, we report a different structural modification approach on ABT-263 by merging the piperazinyl-phenyl fragment into a bicyclic framework leading to a series of novel analogues, among which tetrahydroisoquinoline 13 was nearly equally potent against Bcl-2 as ABT-263. Further SAR in the P4-interaction pocket affored the difluoroazetidine substituted analogue 55, which retained good Bcl-2 activity with improved Bcl-2/Bcl-xL selectivity...
December 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29229009/the-unwelcome-houseguest-secondary-household-transmission-of-norovirus
#10
Z A Marsh, S P Grytdal, J C Beggs, E Leshem, P A Gastañaduy, B Rha, M Nyaku, B A Lopman, A J Hall
Norovirus is the leading cause of acute gastroenteritis in the USA. Although secondary household transmission of norovirus is frequently reported in outbreaks, little is known about specific risk factors for susceptibility and infectiousness in the household. Three norovirus outbreaks were investigated and data were collected on individuals exposed in the primary outbreak setting and their household members. Potential individual- and household-level risk factors for susceptibility and infectiousness were assessed using univariate and multivariate generalised linear mixed models...
December 12, 2017: Epidemiology and Infection
https://www.readbyqxmd.com/read/29227648/quinazolinone-based-anticancer-agents-synthesis-anti-proliferative-sar-anti-tubulin-activity-and-tubulin-co-crystal-structure
#11
Wolfgang Dohle, Fabrice L Jourdan, Gregory Menchon, Andrea E Prota, Paul A Foster, Pascoe Mannion, Ernest Hamel, Mark P Thomas, Philip G Kasprzyk, Eric Ferrandis, Michel O Steinmetz, Mathew P Leese, Barry V L Potter
Quinazolinone-based anti-cancer agents were designed, decorated with functional groups from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl sulfamate motif of steroid sulfatase (STS) inhibitors. The steroidal AB-ring system was mimicked, favoring conformations with an N-2 substituent occupying D-ring space. Evaluation against breast and prostate tumor cell lines identified 7b with DU-145 anti-proliferative activity (GI50 300 nM). A preliminary structure-activity relationship afforded compounds (e...
December 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29226088/a-chimeric-hs4-insulator-scaffold-attachment-region-enhances-transgene-expression-in-transfected-chinese-hamster-ovary-cells
#12
Si-Jia Chen, Wen Wang, Feng-Yi Zhang, Yan-Long Jia, Xiao-Yin Wang, Xiao Guo, Shao-Nan Chen, Jian-Hui Gao, Tian-Yun Wang
Chinese hamster ovary (CHO) cells are one of the most commonly used expression systems for the production of recombinant proteins but low levels of transgene expression and transgene silencing are frequently encountered. Epigenetic regulatory elements such as the chicken β-globin locus control region hypersensitive site 4 (HS4) and scaffold/matrix attachment regions (S/MARs) have positive effects on transgene expression. In this study, a chimeric HS4-SAR was cloned upstream or downstream of an enhanced green fluorescent protein (eGFP) expression cassette in a eukaryotic vector, and the resulting vectors were transfected into CHO cells...
December 2017: FEBS Open Bio
https://www.readbyqxmd.com/read/29225629/synthesis-sar-and-docking-studies-disclose-2-arylfuran-1-4-naphthoquinones-as-in-vitro-antiplasmodial-hits
#13
Tatiane Freitas Borgati, Maria Fernanda Alves do Nascimento, Juma Fortunato Bernardino, Lunamaura Claudia Oliveira Martins, Alex Gutterres Taranto, Alaíde Braga de Oliveira
A total of 28 lapachol-related naphthoquinones with four different scaffolds were synthesized and spectroscopically characterized. In vitro antiplasmodial activity was assayed against the chloroquine-resistant Plasmodium falciparum W2 strain by the parasite lactate dehydrogenase (pLDH) method. Cytotoxicity against Hep G2A16 cell was determined by the MTT assay. All compounds disclosed higher in vitro antiplasmodial activity than lapachol. Ortho- and para-naphthoquinones with a furan ring fused to the quinonoid moiety were more potent than 2-hydroxy-3-(1'-alkenyl)-1,4-naphthoquinones, while ortho-furanonaphthoquinones were more cytotoxic...
2017: Journal of Tropical Medicine
https://www.readbyqxmd.com/read/29224335/structure-activity-relationship-sar-of-phenolics-for-2-amino-1-methyl-6-phenylimidazo-4-5-b-pyridine-phip-formation-in-phenylalanine-creatinine-reaction-mixtures-including-or-not-oxygen-and-lipid-hydroperoxides
#14
Francisco J Hidalgo, José L Navarro, Rosario Zamora
Phenolics can act as either promoters or inhibitors in 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) formation. In an attempt to clarify the structure-activity relationship (SAR) of phenolics for this reaction, the formation of PhIP in mixtures of phenylalanine, creatinine, 13-hydroperoxide of linoleic acid (LOOH) or 4-oxo-2-nonenal, and a wide array of phenolics was studied in the presence and in the absence of oxygen. The obtained results suggested that those phenolics having a high carbonyl scavenging ability inhibited the formation of PhIP...
December 9, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29223717/synthesis-and-biological-evaluation-of-novel-synthetic-chalcone-derivatives-as-anti-tumor-agents-targeting-cat-l-and-cat-k
#15
Yali Wang, Situ Xue, Ruolan Li, Zhihui Zheng, Hong Yi, Zhuorong Li
A series of chalcone derivatives bearing benzamide or benzenesulfonamide moieties were synthesized and evaluated for their anti-tumor effect on HCT116, MCF7 and 143B cell lines in vitro. SAR analysis showed that compounds bearing a benzenesulfonamide group had greater potency than those bearing a benzamide group. It was also shown that compounds with a mono-methyl or mono-halogen group at the 3-position on the terminal phenyl ring were more effective than those with trifluoromethyl or methoxy groups. Compound 8e exhibited the most potent anti-tumor activities against HCT116, MCF7 and 143B cell lines, with IC50 values of 0...
September 18, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29223097/recent-advances-in-microtubule-stabilizing-agents
#16
REVIEW
Ya-Nan Cao, Ling-Li Zheng, Dan Wang, Xiao-Xia Liang, Feng Gao, Xian-Li Zhou
Highly dynamic mitotic spindle microtubules are superb therapeutic targets for a group of chemically diverse and clinically successful anticancer drugs. Microtubule-targeted drugs disrupt microtubule dynamics in distinct ways, and they are primarily classified into two groups: microtubule destabilizing agents (MDAs), such as vinblastine, colchicine, and combretastatin-A4, and microtubule stabilizing agents (MSAs), such as paclitaxel and epothilones. Systematic discovery and development of new MSAs have been aided by extensive research on paclitaxel, yielding a large number of promising anticancer compounds...
November 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29220792/4-quinolone-derivatives-and-their-activities-against-gram-positive-pathogens
#17
Gui-Fu Zhang, Shu Zhang, Baofeng Pan, Xiaofeng Liu, Lian-Shun Feng
Gram-positive bacteria are responsible for a broad range of infectious diseases, and the emergency and wide spread of drug-resistant Gram-positive pathogens including MRSA and MRSE has caused great concern throughout the world. 4-Quinolones which are exemplified by fluoroquinolones are mainstays of chemotherapy against various bacterial infections including Gram-positive pathogen infections, and their value and role in the treatment of bacterial infections continues to expand. However, the resistance of Gram-positive organisms to 4-quinolones develops rapidly and spreads widely, making them more and more ineffective...
November 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29219990/bat-cave-solves-mystery-of-deadly-sars-virus-and-suggests-new-outbreak-could-occur
#18
David Cyranoski
No abstract text is available yet for this article.
December 7, 2017: Nature
https://www.readbyqxmd.com/read/29218465/long-term-survival-of-recurrent-intrahepatic-cholangiocarcinoma-the-impact-and-selection-of-repeat-surgery
#19
Tomoaki Yoh, Etsuro Hatano, Satoru Seo, Yukihiro Okuda, Hiroaki Fuji, Yoshinobu Ikeno, Kojiro Taura, Kentaro Yasuchika, Hideaki Okajima, Toshimi Kaido, Shinji Uemoto
BACKGROUND: Definitive guidelines for recurrent intrahepatic cholangiocarcinoma (ICC) do not exist. This study has focused on the repeat surgery when analyzing the survival outcomes of recurrent ICC. We evaluated the relationship between clinicopathological features of the primary tumor and implementation of the repeat surgery to identify its potential selection criteria. METHODS: A total of 108 patients with recurrent ICC between 1993 and 2015 were analyzed. Of these, 15 patients underwent repeat surgery and 93 did not...
December 7, 2017: World Journal of Surgery
https://www.readbyqxmd.com/read/29217849/life-time-dosimetric-assessment-for-mice-and-rats-exposed-in-reverberation-chambers-of-the-2-year-ntp-cancer-bioassay-study-on-cell-phone-radiation
#20
Yijian Gong, Myles Capstick, Sven Kuehn, Perry Wilson, John Ladbury, Galen Koepke, David L McCormick, Ronald L Melnick, Niels Kuster
In this paper, we present the detailed life-time dosimetry analysis for rodents exposed in the reverberation exposure system designed for the two-year cancer bioassay study conducted by the National Toxicology Program of the National Institute of Environmental Health Sciences. The study required the well-controlled and characterized exposure of individually housed, unrestrained mice at 1900 MHz and rats at 900 MHz, frequencies chosen to give best uniformity exposure of organs and tissues. The wbSAR, the peak spatial SAR and the organ specific SAR as well as the uncertainty and variation due to the exposure environment, differences in the growth rates, and animal posture were assessed...
December 2017: IEEE Transactions on Electromagnetic Compatibility
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