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br Activatable bioorthogonal reactions reagents br Cycloprop
2021-03-19
Activatable bioorthogonal reactions/reagents Cyclopropenes as bioorthogonal reagents for IEDDA substrates Cyclopropenes have become popular bioorthogonal reagents due to their small size, inertness to biological nucleophiles, ability to be genetically encoded (Yu et al., 2012), and participati
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Future advances in the in vivo molecular imaging
2021-03-19
Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measur
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The redox sensitive transcription factor NF B is reported
2021-03-19
The redox sensitive transcription factor NF-κB is reported to play a crucial role in the COPD pathogenesis via up regulating the expression of several cytokines, chemokines, growth factors, and adhesion molecules [71]. Incidentally, we and others have shown that PARP-1 modulates the NF-κB activation
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Most remarkably an essentially identical collagen
2021-03-19
Most remarkably, an essentially identical collagen-binding mode to DDR2 is employed by SPARC, an α-helical matricellular protein unrelated to DDR2 that also recognizes the GVMGFO motif in collagen (Giudici et al., 2008, Hohenester et al., 2008). The convergence of binding mechanisms suggests that th
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Studies have focused on a hydrophobic cage at the CULT
2021-03-19
Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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Approximately of the etamicastat dose was recovered
2021-03-19
Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be
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Cephalexin CFSs are recognized as a driver of genome instabi
2021-03-19
CFSs are recognized as a driver of genome instability in human cells and are hotspots for deletions or translocations in cancers (Richards, 2001). The generally accepted model for their expression is that the CFS locus shows a delay in chromatin condensation in early mitosis caused by the persistenc
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We next focused our design building into the
2021-03-19
We next focused our design building into the ribose binding site, which had not been yet utilized in this effort. Compounds bearing a series of five-membered aromatic heterocycles (compound , ) showed reduced inhibition of the Gram-positive isozymes compared with compound , but a 20-fold improved po
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The members in apple are
2021-03-19
The 8 members in apple are similar in number to the 7 in Arabidopsis and the 8 in rice, but fewer than the 10 found in mammalian species. GenBank numbers have also been reported for DGK homologues from tomato (AW035995), maize (AY106320), wheat (BT009326), a Populus cross (BU828590), grape (CB981130
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There was a good alignment profile between compound
2021-03-19
There was a good alignment profile between compound 26 (IC50 0.06μM) and MTX (IC50 0.08μM) explaining its activity pattern (Fig. 5a). Fig. 5b clearly indicates a different alignment profiles where carbonyl groups are not on the same side between 25 (IC50>100.0μM) and MTX which is in consistency with
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Some limitations to our study
2021-03-19
Some limitations to our study should be noted. First, the sample size of our study was limited. As DDR2 mutations are rare in lung SCC, it is possible that the power of our study was insufficient to detect potential associated factors. Second, a significant proportion of the 271 sequenced patients h
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Ponceau S Staining Solution Cys LT have been shown
2021-03-19
Cys-LT have been shown to be critical for stimulation of monocytes to produce various proinflammatory factors [32,67]. Fig. 3 shows results obtained with human peripheral monocyte-derived macrophages differentiated for 6 days with 20 ng/ml macrophage colony-stimulating factor (M-CSF) and challenged
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A cocktail approach can detect the
2021-03-19
A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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Signal transduction through IL c FMS ligand receptor also le
2021-03-19
Signal transduction through IL-34/ c-FMS ligand receptor also leads to the differentiation, survival and, angiogenesis, proliferation, adhesion and migration of cells of the monocyte/macrophage lineage similar to that of CSF-1 through the various pathways-First is through FAK (Focal Adhesion Kinase)
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Besides the regulation of the stress responses CRF and
2021-03-19
Besides the regulation of the stress responses, CRF and the urocortins have been implicated in drug addiction (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). For instance nicotine, the addictive substance of tobacco, can activate the HPA axis, just like any other stressor may do, although its imp
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