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Several research groups have disclosed potent
2021-08-19
Several research groups have disclosed potent and selective DGAT-1 inhibitors from several chemically-distinct series. Pre-clinical studies with these compounds have confirmed that small molecule DGAT-1 inhibitors can elicit metabolic outcomes comparable to those observed in DGAT-1−/− mice.19, 20, 2
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br Results and discussion To check the hypothesis
2021-08-19
Results and discussion To check the Penciclovir Sodium that the charge of α-synuclein can be altered due to the glycation, we measured zeta potential of native α-synuclein and α-synuclein glycated by two different glycating agents, methylglyoxal (MG) and glyceraldehyde-3-phosphate (GA-3-P). The v
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Previous studies showed that many steroidogenic enzymes act
2021-08-19
Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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Compounds and administered orally to fasted Harlan
2021-08-19
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinica
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Previous studies reported that combined administration of li
2021-08-19
Previous studies reported that combined administration of licorice/GL and TWHF/TP showed reduced toxicity and equal or even potentiated therapeutic efficacy when treating arthritis (YS et al., 2006, YS et al., 2008, Zhang et al., 2007). Our findings that GL reduced exposure to TP in rats confirmed t
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Considering the protumoral functions of TAMs
2021-08-19
Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest in
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Acidic substituents showed moderate biochemical activity but
2021-08-19
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic HBX 41108 mg were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical
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Ezatiostat hydrochloride Our results for imidacloprid were u
2021-08-18
Our results for imidacloprid were unexpected: considering that imidacloprid (Im) is a neonicotinoid insecticide with a different mode of action (agonist of the nicotinic Ezatiostat hydrochloride receptor) than OPs, we expected Es-ChE and T-ChE activity to be largely insensitive to changes in Im conc
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Previous research has suggested that the
2021-08-18
Previous research has suggested that the acetylcholine-gated chloride channels (ACCs) in Caenorhabditis elegans (Putrenko et al., 2005) exhibit the characteristics of promising drug targets. The genes that encode the various subunits of this family are present across the nematode phylum and appear t
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It is not precisely known which of the intramolecular
2021-08-18
It is not precisely known which of the intramolecular interactions created by the SH2 domain, the SH3–SH2 linker and the SH2–kinase linker are essential for the catalytic activity of Csk or how these interactions regulate Csk activity. Thus far it has been shown that site-directed mutagenesis of SH3
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Initially studies of GPCRs predominantly assessed
2021-08-18
Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re
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Thus the understanding of the various mechanisms of action
2021-08-18
Thus, the understanding of the various mechanisms of action of estrogen and SERMs is an important medical challenge and could help to develop an “ideal” SERM, preserving the beneficial effects of estrogen in the bone and urogenital system, and reducing the unwanted side effects, mainly increased ris
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br Materials and methods br Results br Discussion The nitric
2021-08-18
Materials and methods Results Discussion The nitric oxide generating enzymes of the NOS family comprise three isoforms: nNOS, iNOS and eNOS [31]. Expression of eNOS is mainly found in endothelial Exendin-4 where it physically promotes vasodilation [32]. Conversely, evidence also indicates
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Although CCR expression clearly identifies MBC precursors wi
2021-08-18
Although CCR6 expression clearly identifies MBC precursors within the GC, we found that the expression of this chemokine receptor by responding Penciclovir Sodium was not required for MBC differentiation and had no detectable impact on the GC subsets analyzed in this study. Although this is in agre
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br Cytokine impact on ILC
2021-08-18
Cytokine impact on ILC fate Increasing evidence shows that ILC2 and ILC3 may convert into ILC1-like diacylglycerol kinase by downregulating either GATA3 or RORγt, respectively, upregulating T-bet and gaining the capacity for IFN-γ production [60,61]. This process, often referred to as ‘ILC plast
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