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Nimodipine administration also inhibited the eIF
2019-12-17
Nimodipine administration also inhibited the eIF2α/ATF4 singnaling which is a crucial evolutionarily conserved adaptive pathway during cellular stresses including hypoxia and ischemia (Evans et al., 2016; Manwani and McCullough, 2013). While, the eIF2a/ATF4 pathway, activated by different forms of s
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wst-1 assay synthesis In an effort to discover additional GP
2019-12-17
In an effort to discover additional GPCRs directing the migratory events of responding B cells, we identified Epstein-Barr virus (EBV)-induced gene 2 (EBI2) as a promising candidate. The gene encoding EBI2 (Ebi2, also known as Gpr183) was originally identified together with Ebi1 (Ccr7) as the most h
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The preferences for source of FAs for DGAT and
2019-12-17
The preferences for source of FAs for DGAT1 and DGAT2 are related to their membrane topologies, subcellular locations, interactions with other proteins or organelles (discussed in the former section), and their differential expression, substrate specificities, and enzyme kinetics. According to UniPr
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Kumar et al studied Umbelliferone D galactopyranoside UFG be
2019-12-17
Kumar et al. studied Umbelliferone β-D-galactopyranoside (UFG) (benzopyrone), found in many plants exhibiting numerous pharmacological actions. The results of the study showed that UFG in a dose of 10, 20 or 40mgkg-1 per day, helps to prevent paw edema and arthritic score development for arthritis i
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br Experimental br Declaration of interest br Introduction b
2019-12-17
Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR MK-0752 library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound was modified and
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This structure guided the variation of the compounds
2019-12-17
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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br Conclusion br Declaration of interest br Introduction Gly
2019-12-17
Conclusion Declaration of interest Introduction Glyphosate [N-(phosphonomethyl)glycine] is the main active ingredient in one of the most widely used herbicides in the world. The commercially used concentrations of glyphosate range from 1% for domestic use to 41% for conventional agricultura
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We can think of two ways in which collagen
2019-12-17
We can think of two ways in which collagen binding could activate DDR (Figure 8). A single collagen triple helix could interact with both DS domains in the DDR dimer (“composite binding site”) and thereby activate the receptor, similar to the situation exemplified by the growth hormone-growth hormon
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BRD-K4477 br Results and discussion br
2019-12-17
Results and discussion Conclusion Recent studies showed that EGFR signaling is involved in inflammatory response in several inflammatory conditions. The normal inflammatory macrophage BRD-K4477 show EGFR-dependent production of inflammatory mediators. Nevertheless, the development of EGFR inh
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In mice our EBI EGFP reporter
2019-12-16
In mice, our EBI2EGFP reporter showed that EBI2 is expressed consistently in naive T helper cells. Already single positive CD4+ thymocytes express EBI2 (not shown). In effector and regulatory T cells in naive mice, the percentage of EBI2 expression was lower (∼40%). Like others (Liu et al., 2011), w
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PR-171 br Acknowledgments Studies in the
2019-12-16
Acknowledgments Studies in the Tomkinson laboratory on DNA ligase III are supported by research grants from the National Institutes of Health (P01 CA92584 and ES12512 to AET), a grant from the V Foundation and the University of New Mexico Cancer Center. Introduction Ionizing radiation (IR) as
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br Fragment based drug discovery FBDD is a powerful
2019-12-16
Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical levosimendan space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It
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Cysteinyl leukotrienes CysLTs are potent
2019-12-16
Cysteinyl leukotrienes (CysLTs) are potent inflammatory mediators closely associated with cerebral ischemic injury. CysLTs induce inflammatory responses mediated by at least two different CysLT receptors (CysLT1R and CysLT2R) (Bäck et al., 2011, Singh et al., 2010). It has been reported that the Cys
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As described above when EGCG was orally administered CYP
2019-12-16
As described above, when EGCG was orally administered, CYP3A expression in the liver decreased; however, the CYP3A expression level in the intestine was unchanged (Fig. 3). Although we remain speculative, one reason for this may be that because the level of intestinal bacteria in the upper part of t
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Previously published results on this topic are inconsistent
2019-12-16
Previously published results on this topic are inconsistent. Stressin1-A, a novel CRF1 receptor agonist, increased anxiety-like behavior in the social interaction and shock-probe tests [51]. Pharmacological blockade of CRF1 (NBI-30775) reversed both CRF-induced increases in startle and CRF-induced d
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