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QSAR based on the D structures of
2020-06-20
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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Despite the differences in the clustering abilities of DDR
2020-06-19
Despite the differences in the clustering abilities of DDR1b versus DDR2 upon ligand administration, we also noted striking similarities in the spatial distribution and phosphorylation of DDR1b-YFP and DDR2-GFP. We show for the first time that in MC3T3-E1 cells, after 4 h of collagen administration,
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br Four active site residues of KSTD
2020-06-19
Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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We have previously disclosed the
2020-06-19
We have previously disclosed the discovery of a 7-azaindole-3-acetic 961 CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that work, others
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Cancer has been linked to both genetic and epigenetic change
2020-06-19
Cancer has been linked to both genetic and epigenetic changes. Epigenetic modifications, mainly DNA methylation at CpG dinucleotides, affect the regulation of gene transcription without altering the gene\'s sequence. Short sequences rich in CpG dinucleotides (i.e., CpG islands) are often found in th
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Completion of h of education was significant
2020-06-19
Completion of 150 h of education was significant in virtually all prior studies of the 150-h requirement (Allen and Woodland, 2006, Boone et al., 2006 and others). While the 150-h requirement applies to licensure, students are often permitted (as in California) to sit for the CPA exam with fewer tot
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From our array results Supplemental Fig S we found
2020-06-19
From our array results (Supplemental Fig. S2), we found that differential lncRNA profiling exhibited much greater disparity compared to differential gene profiling in CD28nullCD8+ T cells, indicating that differentially expressed lncRNA(s) would serve as ideal hallmarks. Moreover, we were fortunate
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The assessment process is even more difficult when Commercia
2020-06-19
The assessment process is even more difficult when Commercial-Off-The-Shelf (COTS) components – whose internals are partially or totally unknown – come into play. COTS are being increasingly used by the industry to reduce costs and to shorten development (and possibly deployment) time. However, sinc
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An additional difference in ACC between H contortus and C
2020-06-19
An additional difference in ACC-1 between H. contortus and C. elegans is the results from the oocyte expression experiments. Here we found that unlike Cel-ACC-1 that was reported to form a functional homomeric channel (Putrenko et al., 2005), Hco-ACC-1 does not. However, we have observed that in gen
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br Results and discussions In general
2020-06-19
Results and discussions In general, experimental analysis is time consuming and expensive. Thus, In the present study, Taguchi design of experiments (DOE) was adopted to reduce the number of trials. To analyze the data, a High Level Analysis (HLA) is performed by averaging measured data for each
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To overcome problems with the biochemical reconstitution
2020-06-18
To overcome problems with the biochemical reconstitution of these heterodimeric cytokines fusion strategies linking both subunits together have been proposed inspired by the “hyper-IL-6” [28]. Much like fusing a protein to a solubility enhancing protein such as MBP or SUMO, fusing two subunits of a
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Studies also provide evidence that cytokines such
2020-06-18
Studies also provide evidence that cytokines such as TGF-β, a TH3-type cytokine, may also play a role in airway remodeling. Data obtained by Cohen et al suggest that TGF-β1 can induce human BSMC proliferation by increasing the expression of IGFBP-3. Hence, the mitogenic action of TGF-β1 could be rel
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As compared with the broad
2020-06-18
As compared with the broad spectrum of chemicals known to serve as the ligands for PXR and CAR, the ligands of VDR are previously restricted to VD3 as well as its hydroxylated metabolites and the secondary bile amikacin sulfate LCA. Recently, the VDR-binding capacities of more compounds have been d
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Employing distinct genetic and pharmacological
2020-06-18
Employing distinct genetic and pharmacological approaches, Divakaruni et al. now demonstrate that macrophages still acquire their IL-4-elicited phenotype in the absence of CPT1a (considered the main isoform in leukocytes) or CPT2, and highlight that the increased LC-FAO in M(IL-4) cells is less cruc
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br Results and discussion br
2020-06-18
Results and discussion Conclusion Novel and selective aziridine-based inhibitors for the Leishmania mexicana protease LmCBP2.8 were discovered. Compounds 7d (Ki = 0.8 μM), 9d (Ki = 1.36 μM), 12d (Ki = 0.77 μM), 14d (Ki = 0.9 μM) and 18 (Ki = 0.441 μM) showed the highest potency and selectivity
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