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The ester moiety is a promising structural
2022-08-22
The ester moiety is a promising structural motif at the C-3 position for the development of drug-like molecules. However, the labile C-3 ester bond impels these derivate to be susceptible to plasmatic degradation by esterases and this is natural steroidal metabolic process [39,40]. Hence, the isoste
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During pain signal transmission glutamate is released into
2022-08-22
During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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br Discussion RBCs possess a much simpler
2022-08-22
Discussion RBCs possess a much simpler composition and structure than other eukaryotic Pirinixic Acid and can therefore serve as a convenient system on which to study how cell functioning relates to the molecular and supramolecular properties of its constituents. The model developed in this work
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br Results and discussion br Conclusion In
2022-08-19
Results and discussion Conclusion In normal and curd coconuts, full-length cDNA and parental genomic DNA sequences encoding endosperm specific AGal were sequenced and characterized. At least, three mutation Bcl Family Set I were identified in CnAGal gene. In vitro expression in K. phaffii show
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We reviewed the results of comprehensive
2022-08-19
We reviewed the results of comprehensive genomic profiling (CGP) in 26,054 cases of NSCLC and examined the frequency and clinical characteristics of patients whose tumors harbor FGFR fusions. To our knowledge, this is the most in-depth evaluation of FGFR fusions exclusively in NSCLC. Here we will de
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Data are expressed as means SE Statistical significance was
2022-08-19
Data are expressed as means±SE. Statistical significance was determined by the Student's -test or ANOVA with post hoc Bonferroni test. A value of Epiberberine expressing human FPPS. Western blot analysis showed a clear band, which indicated the overexpression of FPPS, in U87MG cells (A, insert). Ex
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More specific quantitative assays for DiXaIs are based
2022-08-19
More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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br Anandamide signaling and cardiovascular function
2022-08-19
Anandamide signaling and cardiovascular function The cardiovascular effects of cannabinoid compounds have been known for a long time. Studies in humans indicate that chronic use of marijuana causes long lasting decrease in blood pressure and heart rate, whereas the acute use increases heart rate
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RO5185426 br STAR Methods br Author Contributions br
2022-08-19
STAR★Methods Author Contributions Introduction Hyaluronan, a major constituent of the extracellular matrix (ECM), is produced by hyaluronan synthases (HASs) and degraded by hyaluronidases (HYALs) (Vigetti et al., 2014). Physiologically, hyaluronan exists in a form with a molecular weight of
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br Prostaglandins meet Hippo The prostaglandins lie at the
2022-08-19
Prostaglandins meet Hippo The prostaglandins lie at the crossroads between inflammation, regeneration and tumorigenesis (Figure 3). Prostaglandins are synthesized from archidonic Ruxolitinib by Cox1 and Cox2 enzymes [40, 41] and in the gut, prostaglandin E2 (PGE2) protects against DSS-induced co
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Eribulin mesylate In conclusion while class I HDAC
2022-08-19
In conclusion, while class I HDAC inhibitors, isoform-specific HDAC3 and HDAC6 inhibitors may represent novel therapeutic targets for prevention of clinical AF onset and progression, the specific HDAC3 and HDAC6 inhibitors may be more appropriate because of their limited off-targets effects. Besides
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Initially the synthesized compounds from were evaluated for
2022-08-19
Initially, the synthesized compounds from were evaluated for human GSNOR potency before generating additional SAR in order to understand scaffold feasibility and required functionality as illustrated in . Commercially available 4′-hydroxy-[1,1′-biphenyl]-4-carboxylic (-)-p-Bromotetramisole Oxalate
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br Results and discussion br Conclusions
2022-08-19
Results and discussion Conclusions In summary, we generated analogues of the hit compounds 1–3, studied their structure–activity relationships, and created a series of highly potent GPR55 agonists. The most potent agonists among the series were 17a-b, 17e, 17g and 17l with EC50 values below 10
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br Materials and methods br
2022-08-18
Materials and methods Results Discussion The redox domain that spans the region between amino Naringin positions 35 and 127 of the major human AP endonuclease, APE1, regulates the sequence-specific DNA binding of various transcription factors [[52], [85]]. The existent crystal structures o
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br Materials and methods br Results br Discussion
2022-08-18
Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the Pyocyanin of neurons and glial c
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