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We have previously reported DAPK inhibitors
2020-11-19
We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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Several evidences showed that seizures increase brain extrac
2020-11-19
Several evidences showed that seizures increase brain extracellular glutamate, which binds to N-methyl-d-aspartate (NMDA) receptor, then up-regulated cyclooxygenase-2 (COX-2) expression in brain capillaries to increase BBB P-gp expression [11,13,29,30]. A recent study demonstrated a different signal
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br Author contributions br Conflicts of
2020-11-19
Author contributions Conflicts of interest Introduction Current the 5-year survival rates for lung and pancreatic cancers are 18% and 8%, respectively. These low survival rates are partially because of the late diagnosis of one-half of cases, in which 5-year survival decrease to 4% and 3%,
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dna ligase Another option is to use the thiol groups of
2020-11-19
Another option is to use the thiol groups of cysteine residues, which can be modified by use of PEG-maleimide and vinyl sulfone. However, changes in PEGylation interactions or reaction conditions can result in changes in the functional properties of the therapeutic proteins [[50], [51], [52]]. A st
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Pahlavanzadeh and Fakouri Baygi employed PC
2020-11-19
Pahlavanzadeh and Fakouri-Baygi [6] employed PC-SAFT EoS to predict the Caspase-8, human recombinant protein australia of carbon dioxide by aqueous MEA solutions. They used the ideal form of Smith–Missen algorithm to calculate liquid phase concentrations. The results illustrate acceptable accuracie
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Previously we have shown that complexes of protein PKs with
2020-11-19
Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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Replacement of the saturated propoxy group
2020-11-19
Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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LY3009120 br Funding This work was supported by the National
2020-11-19
Funding This work was supported by the National Natural Science Foundation of China (grant number 81671411); Beijing Natural Science Foundation (grant number 7162062); Beijing Nova Program Interdisciplinary Cooperation Projects (grant number Z161100004916045); Beijing Municipality Health Technolo
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Enhanced oxidative stress has been suggested as the
2020-11-18
Enhanced oxidative stress has been suggested as the critical mechanisms of IS-produced muscle damage [41,42]. NAC as a direct reactive oxygen species ROS scavenger is frequently discussed in the clinical trials of radiocontrast-induced AKI prevention [43]. Despite some supportive epidemiological dat
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The requirement for two distinct signalling pathways for
2020-11-18
The requirement for two distinct signalling pathways for cAMP-induced growth arrest likely represents an important mechanism allowing VSMC to finely modulate their cellular responses to cAMP-elevating stimuli. Our data demonstrates for the first time that activation of both pathways in VSMC results
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br Activatable optical imaging probes
2020-11-18
Activatable optical imaging probes Optical fluorescence imaging, which directly detects photons emitted from fluorescent probes, has become as a powerful analytical method to study biological processes both in vitro and in vivo. It is characterized by high sensitivity, is free of radioactive irra
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annexin v From an industrial perspective the low turnover nu
2020-11-18
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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We should also note that oxygen pressure of Krebs solution
2020-11-18
We should also note that oxygen pressure of Krebs solution bubbled with 95% O2+5% CO2 as we used in our study is reported to around 400 mmHg in several studies [48], [49], which is higher than normal arterial O2 pressure (80–100 mmHg). Although superoxide generation at elevated O2 tensions are noted
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Nicotine mg Elastase belongs to chymotrypsin family of
2020-11-18
Elastase belongs to chymotrypsin family of proteases and it is responsible for the breakdown of elastin and other proteins, such as collagen and fibronectin, which are fundamental for the ECM elastic properties (Imokawa and Ishida, 2015). Misregulations of this enzyme are involved in skin ageing pro
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br Activity based probes br Characterization of
2020-11-18
Activity-based probes Characterization of coronavirus-encoded DUBs with activity-based probes To study the activity of specific DUBs, investigators frequently take advantage of the ~10kDa (monoUb or Ubl ABP) or ~20kDa (DiUb ABP) increase in MW on probe labeling. SDS-PAGE analysis or blotting f
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