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Regarding A Rs and A ARs basal
2024-06-11
Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg
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br Trauma and ACEs screening the past
2024-06-11
Trauma and ACEs screening: the past, present, and future Traditionally, allopathy’s biomedical model has utilized an etic perspective; the outsiders’ view of the problem. Development of diagnostic screening tools requires an etic approach, which relies heavily on a completely objective perspectiv
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In an AP scenario several inflammatory mediators are
2024-06-11
In an AP scenario, several inflammatory mediators are produced locally to orchestrate an immune response. Eicosanoids are among those molecules and represent a class of lipid mediators synthesized from arachidonic dofetilide through the action of cyclooxygenases or lipoxygenases to generate prostag
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br Materials and methods br Results br Discussion We have
2024-06-11
Materials and methods Results Discussion We have developed a high-throughput functional genomic screen that allows the identification of genes that confer drug resistance. Several factors have been identified which must be taken into account to develop a reliable screen. In particular, cons
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br Autophagy in hemorrhagic stroke About
2024-06-11
Autophagy in hemorrhagic stroke About 87% of all strokes cases are ischemic, the rest being hemorrhagic. ICH and SAH are the two major categories of hemorrhagic strokes (Bruder et al., 2014). Both types of stroke are associated with a high mortality and morbidity rate. The corresponding animal mo
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Pyrimidine is the important pharmacology core in
2024-06-11
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the SB 431542 core as well
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Compound was docked into the active site
2024-06-11
Compound was docked into the active site of Aurora B kinase using Tripos sybyl-X ver. 2.1.1. The crystal structure of human Aurora B kinase cocrystallized with its potent inhibitor VX-680 was used for the docking analysis (PDB ID: ). The most likely binding conformations were selected based on the
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Analysis of ASK crystal structures
2024-06-08
Analysis of ASK1 crystal structures as well as an investigation of how gyy sale 4 might bind were undertaken to understand opportunities for engaging Gln756. To this end a docking model derived from PDB 3VW622 was used to predict the binding mode of amide 4 in the ASK1 active site as shown in Fig.
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br Activity and expression of aromatase
2024-06-08
Activity and expression of aromatase in the hippocampus The brain, like the adrenals, gonads and the placenta, is a steroidogenic organ. This paradigm emerged from studies carried out as early as the 1980s by Baulieu and co-workers; these studies showed that steroids such as pregnenolone and dehy
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Recently competitive inhibitors of arginase have been develo
2024-06-08
Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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L002 We also explored the possibility that this PKC activati
2024-06-08
We also explored the possibility that this PKC-θ activating protein could operate on the auto-phosphorylation process of the kinase, a specific event accompanying PKC activation [32]. The heated PKC-θ immunoprecipitate from metaphasic cells was then added to PKC-θ isolated both from interphasic or m
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Using the same techniques we found that
2024-06-08
Using the same techniques, we found that UCP3 also has a half-life of between 1 and 4h [117]. In yohimbine hydrochloride to UCP2 and UCP3, UCP1 and ANT had much longer half-lives and could not be degraded in the cell-free reconstituted system, suggesting their degradation is not mediated by the cyt
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indole 3 butyric acid Physical and chemical preservatives su
2024-06-08
Physical and chemical preservatives such as ultraviolet and ɣ-rays irradiation, sulphur and aluminium phosphide fumigation, etc, have been introduced to inhibit the growth of fungi. Nevertheless, due to the potential decomposition reactions and residues, as well as their own potential toxicity, and
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Since primitive societies plants herbs and seeds rich in
2024-06-08
Since primitive societies, plants, herbs and seeds, rich in phytochemicals, were used due to their benefits in human health. These molecules were shown to present a diverse array of action mechanisms, including antioxidant activity, enzyme stimulation, hormones mimicking and by interfering with DNA
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The Irbesartan Diabetic Nephropathy Trial enrolled patients
2024-06-08
The Irbesartan Diabetic Nephropathy Trial enrolled patients with type 2 diabetes, proteinuria of at least 0.9 g/24 h, BP >135/85 mmHg and moderate kidney impairment (creatinine 88 to 265 µmol/L in women or 106 to 265 µmol/L in men). Patients were randomized to receive irbesartan (titrated from 75 to
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