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Our recent discovery M P H R
2021-01-29
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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Apart from neutrophil mediated inflammation the production o
2021-01-29
Apart from neutrophil-mediated inflammation, the production of pro-inflammatory cytokines and chemokines from PGD2/CRTH2 activated macrophages could further aggravate LPS-induced lung injury (Eguchi et al., 2011; Jandl et al., 2016). Interestingly, genetic ablation of CRTH2 diminishes the TNF-α prod
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Prostaglandins production and some of their possible
2021-01-29
Prostaglandins production and some of their possible biological functions have been reported in protozoa, helminths, and fungi organisms, for example amphizoic amoebas of the genus Acanthamoeba and Entamoeba (E. histolytica) produce PGA2, PGE2 and PGF2α [5,6]. PGA2 is believed to be an intrinsic osm
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SPR was used to measure biomolecular
2021-01-29
SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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Compounds were synthesized as illustrated in tetrazole yl
2021-01-29
Compounds – were synthesized as illustrated in , , , , . 3-(1-tetrazole-5-yl)benzaldehyde was obtained in 95% yield via [2+3] cycloaddition of sodium azide to commercially available 3-cyanobenzaldehyde in presence of triethylamine as reported in the literature. Nitration of 3-hydroxyacetophenone wi
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In this regard http www apexbt com
2021-01-29
In this regard, some attempts have been made to reduce the presence of those radicals. In presence of fluorine source, it seems that the fluorine atoms can substitute the hydrogen atoms linked to silicon atoms, forming Si-F bonds with a higher bonding XL413 hydrochloride (536 kJ mo1−1) than the Si-
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Otherwise ES cells express high
2021-01-29
Otherwise, ES AZD-9291 mesylate receptor express high level of histone lysine specific demethylase 1 (LSD1) expression. In this context, it is proposed that LSD1 inhibition may block the function of EWS-ETS proteins [70]. Furthermore, checkpoint kinase 1 (CHK1), a modulator of cell survival under t
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In conclusion the data suggest
2021-01-29
In conclusion, the data suggest that doses of COX-2 inhibitors and EP1 receptor antagonists which have previously been reported to exert disease modulating or antiepileptic drug potentiating effects do not negatively affect seizure control in temporal lobe epilepsy. The contrasting impact of the EP1
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The reaction of chitosan with
2021-01-29
The reaction of chitosan with DVS should take place primarily through a nucleophilic attack of the vinyl sulfone groups to the amino groups in chitosan [39,50], although its hydroxyl groups can also be involved, as it happens when using agarose [35]. These reactions create very stable secondary amin
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Most xenobiotics undergo biotransformation before being excr
2021-01-29
Most xenobiotics undergo biotransformation before being excreted. Such biotransformation is classified into two phases. In the first phase, the lipophilic substrate is oxidized by the cytochrome P-450 (CYP450) enzyme system, which introduces a single oxygen Phenyl sulfate into the molecule (Moutou
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A-803467 The enantiomeric ratio ER of chiral compounds accum
2021-01-29
The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER o
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The molecular docking data supported the potential
2021-01-29
The molecular docking data supported the potential interaction of lapachol and the synthetic naphthoquinonolyl compounds with the PfDHODH enzyme as the putative mechanism of action and the inhibition of parasite growth in vitro. In general, compounds fit well into the binding pocket of PfDHODH, the
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In this review focusing on biocatalyst formate dehydrogenase
2021-01-29
In this review, focusing on biocatalyst “formate dehydrogenase FDH” catalyzing both of the formic Fluorescein TSA Fluorescence System Kit oxidation to CO2 and the CO2 reduction to formic acid, representative examples of properties, types, structure of active-site of FDH and, reaction mechanism of fo
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The second DDR binding partner identified here Shp
2021-01-29
The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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br Results and discussion A
2021-01-29
Results and discussion A systematic search for genes encoding H+-PPases was carried out by PCR using genomic DNA from a wide range of protozoa as templates and degenerate oligonucleotides, designed from amino colorimetric assay receptor domains conserved in H+-PPases of higher plants and the pro
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