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Historically covalent drugs have had
2021-01-07
Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form
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It was hypothesized that if modafinil
2021-01-07
It was hypothesized that if modafinil acts primarily via a noradrenergic mechanism, Dbh −/− mice should be non-responsive since they completely lack NE. In contrast, if modafinil acts mainly through DA systems, these mice should be hypersensitive. Modafinil was tested in Dbh −/− mice using both loco
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cGAS has a central role in STING activation after DNA
2021-01-07
cGAS has a central role in STING activation after DNA sensing, but it is unknown if most of the DNA sensors act independently or in cooperation with the cGAS-cGAMP pathway. This was addressed for IFI16 (Almine et al., 2017, Jønsson et al., 2017) and PQBP1 (Yoh et al., 2015) but remains to be tested
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Eeyarestatin I QSAR based on the D structures of ligands pla
2021-01-07
QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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Compound was advanced to a
2021-01-07
Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, Cytarabine 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured daily
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br Results and discussion To check the hypothesis that
2021-01-07
Results and discussion To check the Furosemide that the charge of α-synuclein can be altered due to the glycation, we measured zeta potential of native α-synuclein and α-synuclein glycated by two different glycating agents, methylglyoxal (MG) and glyceraldehyde-3-phosphate (GA-3-P). The value for
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The isolation of a proteinaceous putative
2021-01-07
The isolation of a proteinaceous putative inhibitor of cysteine proteases from the extracts of Y. enterocolitica and E. coli was performed by affinity chromatography on immobilized and inactivated papain (Fig. 7A). Instead of the column variant of this technique (Tsushima et al., 1992), we used a ba
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br Introduction Benzanthrone BNZ is a
2021-01-07
Introduction Benzanthrone (BNZ) is a dye intermediate used in the synthesis of number of polycyclic vat and disperse dyes. It has been detected as an environmental pollutant in urban ambient air particulates, originating from furnace effluents, municipal refuge, wood and coal combustion and autom
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AMD is equally active against a
2021-01-07
AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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By using the C elegans Matrisome Annotator tool
2021-01-06
By using the C. elegans Matrisome Annotator tool, we found substantial enrichment for matrisome Diclofenac Sodium in these data sets. Thus, re-analyzing -omic datasets with the C. elegans Matrisome Annotator tool may be useful to generate novel hypotheses about the role of the C. elegans matrisome
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MSCs are self renewing multipotent
2021-01-06
MSCs are self-renewing, multipotent progenitor cells, with multilineage potential to differentiate into adipocytes, osteocytes, and chondrocytes. In addition, MSCs can migrate to sites of inflammation, supporting hematopoiesis and homeostatic maintenance. Given their unique therapeutic properties, M
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br Results and discussion The effects
2021-01-06
Results and discussion The effects of hypoxia, a combination of shear stress and hyperoxia, and a combination of shear stress and hypoxia in BAECs were assessed at 0, 15, 30, 60, 120, and 180 min. Changes in phosphorylation levels of eNOS at Ser635 were investigated using immunoblotting, and repr
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Glycolysis is important to maintain the vital functions of T
2021-01-06
Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its ZD 9379 metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egress from host cells.
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For these reasons molecules of the ET family
2021-01-06
For these reasons, molecules of the ET family and in particular ET-1 are considered useful factors in the evaluation of malignancy and in consequence, in the prognosis for several forms of neoplasia, such as ovarian (Bagnato et al., 2005), prostate (Nelson et al, 1995, Nelson et al, 1996), colorecta
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Costunolide receptor The lack of robust immunocompetent anim
2021-01-06
The lack of robust immunocompetent animal models permissive for HCV makes it hard to assess if the quantity and quality of vaccine-induced immunity is sufficient to confer protection. Thus, it is difficult to predict to what extent antibody responses induced by current vaccination approaches, includ
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