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#32272481 2020/04/09 To Up
Structure of M from COVID-19 virus and discovery of its inhibitors.A new coronavirus (CoV) identified as COVID-19 virus is the etiological agent responsible for the 2019-2020 viral pneumonia outbreak that commenced in Wuhan. Currently there are no targeted therapeutics and effective treatment options remain very limited. In order to rapidly discover lead compounds for clinical use, we initiated a program of combined structure-assisted drug design, virtual drug screening and high-throughput screening to identify new drug leads that target the COVID-19 virus main protease (M). M is a key CoV enzyme, which plays a pivotal role in mediating viral replication and transcription, making it an attractive drug target for this virus. Here, we identified a mechanism-based inhibitor, N3, by computer-aided drug design and subsequently determined the crystal structure of COVID-19 virus M in complex with this compound. Next, through a combination of structure-based virtual and high-throughput screening, we assayed over 10,000 compounds including approved drugs, drug candidates in clinical trials, and other pharmacologically active compounds as inhibitors of M. Six of these compounds inhibited M with IC values ranging from 0.67 to 21.4 μM. Ebselen also exhibited promising antiviral activity in cell-based assays. Our results demonstrate the efficacy of this screening strategy, which can lead to the rapid discovery of drug leads with clinical potential in response to new infectious diseases for which no specific drugs or vaccines are available.
Zhenming Jin, Xiaoyu Du, Yechun Xu, Yongqiang Deng, Meiqin Liu, Yao Zhao, Bing Zhang, Xiaofeng Li, Leike Zhang, Chao Peng, Yinkai Duan, Jing Yu, Lin Wang, Kailin Yang, Fengjiang Liu, Rendi Jiang, Xinglou Yang, Tian You, Xiaoce Liu, Xiuna Yang, Fang Bai, Hong Liu, Xiang Liu, Luke W Guddat, Wenqing Xu, Gengfu Xiao, Chengfeng Qin, Zhengli Shi, Hualiang Jiang, Zihe Rao, Haitao Yang 50 UG100 ug100 ug1 mg11 mg0.25 mg200 100ul 96 Tests 1 ml1 mg
#32272479 2020/04/09 To Up
Cardiorespiratory Fitness and Physical Activity following Lung Transplantation: A National Cohort Study.Low cardiorespiratory fitness and inactivity are common after lung transplantation (LTx). The causes of exercise intolerance are incompletely understood.
Mariann Ulvestad, Michael Thomas Durheim, Johny Steinar Kongerud, Bjørge Herman Hansen, May Brit Lund, Elisabeth Edvardsen
2089 related Products with: Cardiorespiratory Fitness and Physical Activity following Lung Transplantation: A National Cohort Study.100ug100 assays0.1 mg 25 MG 96 Tests 100 assays100ug2 x 96 well plate
#32272478 2020/04/09 To Up
Effectiveness of Energy Conservation Techniques in Patients with COPD.Patients with chronic obstructive pulmonary disease (COPD) might suffer from severe dyspnea, which importantly impacts on the performance of activities of daily living (ADL). Patient training of energy conservation techniques (ECTs) might be useful to improve the tolerance and execution of these ADL, but objective studies evaluating the effect of teaching ECTs on the metabolic equivalent of task (MET) in patients with COPD are sparse.
Ann Sylvia Louise Wingårdh, Carina Göransson, Sven Larsson, Frode Slinde, Lowie E G W Vanfleteren96 tests1 Set100 1 Set2.5 mg1 Set1 Set100 μg5 500 ml
#32272470 2020/04/10 To Up
Transposable DNA Elements in Amazonian Fish: From Genome Enlargement to Genetic Adaptation to Stressful Environments.Transposable elements have driven genome evolution and plasticity in many ways across a range of organisms. Different types of biotic and abiotic stresses can stimulate the expression or transposition of these mobile elements. Here, we cytogenetically analyzed natural fish populations of the same species living under different environmental conditions to test the influence and organization of transposable elements in their genome. Differential behavior was observed for the markers Rex 1, Rex 3, and Rex 6 in the chromosomes of individuals of the same species but coming from different environments (polluted and unpolluted). An increase in the number of Rex transposable elements in the chromosomes and their influence on the genome of populations living in a polluted environment indicates that they must be under constant adaptive evolution.
Francijara A da Silva, Erika M Corrêa Guimarães, Natália D M Carvalho, Alex M V Ferreira, Carlos H Schneider, Gislene A Carvalho-Zilse, Eliana Feldberg, Maria C Gross
2547 related Products with: Transposable DNA Elements in Amazonian Fish: From Genome Enlargement to Genetic Adaptation to Stressful Environments.1 mg96 wells (1 kit)1 kit 1 G1mg10 100 μg1 kit
#32272458 2020/04/09 To Up
Refinement of a protocol to induce reliable muscle cramps in the abductor hallucis.To test the reliability of immediate replication of muscle cramp characteristics induced with different electrical stimulation protocols.
Ashley P Akerman, Robert J Walker, John B W Schollum, Tracey L Putt, Luke C Wilson
2660 related Products with: Refinement of a protocol to induce reliable muscle cramps in the abductor hallucis.100 100 100ug100 ul1 kit1 mg100 ul
#32272456 2020/04/09 To Up
Single-channel oximetry monitor versus in-lab polysomnography oximetry analysis: does it make a difference?Portable oximetry has been shown to be a promising candidate for large-scale obstructive sleep apnea screening. In polysomnography (PSG), the gold standard OSA diagnosis test, the oxygen desaturation index (ODI) is usually computed from desaturation events occurring during sleep periods only, i.e., overnight desaturations occurring during or overlapping with a wake state are excluded. However, for unattended home oximetry, all desaturations are taken into account since no reference electroencephalogram is available for sleep staging. We aim to evaluate the hypothesis that the predictive power of oximetry for OSA screening is not impaired when reference sleep stages are not available.
Joachim Behar, Niclas Palmius, Sroussi Zacharie, Armand Chocron, Thomas Penzel, Lia Bittencourt, Sergio Tufik
2706 related Products with: Single-channel oximetry monitor versus in-lab polysomnography oximetry analysis: does it make a difference?1,000 tests100 25 100 1mg3 modules100 Tests25 Tests
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