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nitric oxide inhibitor br Activation of soluble guanylate cy
2021-10-19
Activation of soluble guanylate cyclase The molecular steps involved in sGC activation have evolved significantly over the last several years. The key studies are outlined below, but here we provide an overall summary. The activation mechanism of sGC was initially proposed to be relatively simple
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Third we performed correlation analysis between the
2021-10-19
Third, we performed correlation analysis between the results obtained using DMR agonist assay in HT-29 and Tango assay in the engineered U2OS cells. First, we compared their relative efficacy, the maximal responses after normalized to the maximal responses of zaprinast obtained using both DMR and Ta
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Our inhibitor studies revealed the
2021-10-19
Our inhibitor studies revealed the presence of a signaling network triggered by dicarbonyl stress. Nevertheless, p38-MAPK activation was clearly necessary for NADPH-oxidase mediated production of ROS. This is consistent with data from other groups using different cell culture systems [37], [38], [39
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Natural products have been always the most
2021-10-19
Natural products have been always the most important and productive sources of lead compounds for the development of drugs [[15], [16], [17]]. A variety of potent α-glucosidase inhibitors have been identified from natural products, such as quercetin, resveratrol, isorhamnetin, calein C and curcumin
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In contrast with the above results in
2021-10-18
In Ursodiol mg with the above results, in our GC model system, FPR1-, but not FPR2-knockout, enhanced tumour formation. However, it should be noted that the prominent role of mFPR2 with respect to mFPR1 in the mouse colon might be due to the significantly higher expression of mFPR2 than mFPR1 in thi
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In addition to the four classical FGFRs there
2021-10-18
In addition to the four classical FGFRs there is an additional receptor, FGFR like-1 (FGFRL1, also known as FGFR5) (Ornitz and Itoh, 2015, Trueb et al., 2003). FGFRL1 gene was discovered in a cartilage specific cDNA library in 2000 (Trueb, 2011, Trueb et al., 2003) and thereafter it has been found i
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One year after the Brose paper was published Littleton
2021-10-18
One year after the Brose . paper was published, Littleton . reported the first measurements of evoked synaptic transmission in syt1 nulls, using the neuromuscular junction as a model system. These experiments revealed that syt1 was essential for rapid, robust evoked neurotransmitter release. Similar
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The biochemical cell culture activities and properties of bi
2021-10-18
The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chlori
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Here we report the kinetics of inhibition of the MYST
2021-10-18
Here, we report the kinetics of inhibition of the MYST HAT family member KAT8 by MG149, and a calculation of the inhibitory constant Ki of MG149 for KAT8. The inhibition of HATs by MG149 could be correlated to inhibition of histone acetylation in murine PCLS upon MG149 treatment, as determined by a
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Concerning the molecular mechanisms underlying transcription
2021-10-18
Concerning the molecular mechanisms underlying transcriptional regulation of the GSTP1-1 gene expression we and others have characterized structural and functional properties of the human GSTP1-1 promoter. GSTP1-1 gene promoter activity is driven by a TATA-box [16] as well as Spl [16], [17], AP-1 [1
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Lipid sensing GPCRs as therapeutic
2021-10-18
Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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br Computational details and modeling All
2021-10-18
Computational details and modeling All calculations were performed using the density functional B3LYP [34] method, implemented in Gaussian03 program [35]. The structures of reactants, transition states, intermediates, and products were optimized using the 6-31+G(d) basis set for the H, C, N, O an
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To further investigate its role in stresses tolerance OsGly
2021-10-18
To further investigate its role in stresses tolerance, OsGly I was overexpressed in transgenic rice. qRT-PCR and zymologic determination showed that prostaglandin synthase level of OsGly I and the glyoxalase I activity were significantly increased to different extent in the transgenic overexpressio
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The mechanisms by which NEIL and NEIL excise
2021-10-18
The mechanisms by which NEIL1 and NEIL3 excise bulky adducts and unhook ICLs are unclear. Structures of NEIL1 are available only in complex with DNA containing small lesions 79., 80., 81., and the single available structure of NEIL3 lacks DNA (Figure 5D,E) [73]. Nonetheless, comparison of the two st
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To synthesize the azaindole based compound Suzuki coupling o
2021-10-18
To synthesize the 7-azaindole based compound , Suzuki coupling of 6-chloro-7-azaindole with 4-CFO-phenylboronic Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) mg was carried out in the presence of Pd(dppf)Cl·CHCl to supply biaryl in quantitative yield (). Iodination at the C-3 position res
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