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As mentioned previously dopamine plays a
2021-01-20
As mentioned previously, dopamine plays a crucial role in reducing prefrontal cortical suppression to the amygdala (Rosenkranz and Grace, 2001) and prefrontal cortex mediated amygdala supression has recently been associated with vagal regulation of HRV (Sakaki et al., 2016). In addition, evidence ha
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The second part of this study evaluated the role
2021-01-20
The second part of this study evaluated the role of CK1 in the eFABP4 cellular uptake in endothelial cells. By blocking CK1 expression using a specific siRNA, we corroborated that the presence of CK1 was fundamental for FABP4 cellular uptake and internalization in endothelial cells, thus decreased m
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We found that both DDR and
2021-01-19
We found that both DDR1 and DDR2 ECD increased matrix mineralization as compared to native cells, with the effect of DDR2 ECD being more prominent. Both soluble (DDR2/ECD) and membrane-bound DDR2 ECD (DDR2/-KD), when compared to wild-type cells, induced larger mineral deposits. In this regard, a rec
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br Cysteine proteases as molecular targets for trypanosomati
2021-01-19
Cysteine proteases as molecular targets for trypanosomatid diseases Approaches relying on a molecular target, such as SBDD and target-based screening, have supported outstanding scientific developments in current pharmaceutical R&D. By integrating experimental and computational methods, these str
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Each of the CYP enzymes alluded to above are
2021-01-19
Each of the CYP450 enzymes alluded to above are highly selective catalysts, in that, the three aryl coupling reactions en route the biosynthesis of 1 are catalyzed by three different CYP450 enzymes in a sequential manner (Fig. 1). In sharp nrf2 keap1 is the recently described marine bacterial CYP450
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Introduction Cytochrome P CYP A is the most
2021-01-19
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The glycine transporter level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and tox
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The corticotropin releasing factor CRF
2021-01-19
The corticotropin-releasing factor (CRF) also referred to as corticotropin-releasing hormone, is a key mediator of mammalian endocrine, behavioral, autonomic, and immune responses to stress (Vale et al., 1981, Owens and Nemeroff, 1991, Bale and Vale, 2004). Within the hypothalamic–pituitary–adrenal
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br Outcome of COX overexpression Although a causal role
2021-01-19
Outcome of COX-2 overexpression Although a causal role for COX-2 has been proposed, mechanisms by which COX-2 function contributes to the pathogenesis of hyperplastic disease are not well defined. To examine if there is any correlation between COX-2 and p53 protein levels, Kumagai et al. [15] rec
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What is the predominant mechanism underlying the benefits of
2021-01-19
What is the predominant mechanism underlying the benefits of udenafil, i.e. the vascular vs. myocardial effect? Lewis et al. suggested that the benefit of sildenafil in HFrEF would be derived from augmented RV systolic function that mainly results from pulmonary vasodilation, suggestive of the ‘vasc
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Therefore the SPH algorithm in AUTODYN
2021-01-19
Therefore, the SPH algorithm in AUTODYN-3D™ was used to simulate the experiment in Ref. [5] to verify the credibility of the numerical simulation method by results that could be measured accurately. Then the verified numerical simulation method was used to simulate BAD generated by RHA subjected to
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One possible pitfall of using EPAC activators in the
2021-01-19
One possible pitfall of using EPAC2 activators in the treatment of T2DM is their potential to increase glucagon levels. As discussed previously, although the ability of EPAC2 to increase glucagon expression and production is controversial, several studies show that this protein increases Gcg mRNA le
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Acidosis has lethal consequences but alkalosis due
2021-01-19
Acidosis has lethal consequences, but alkalosis (due to chloride depletion, potassium depletion, and excess mineralocorticoid) is not tolerated as well (Luke and Galla, 2012). In this regard, efforts to restore pH to normal physiological level, in the most benign way should be the goal of researcher
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PSB 1115 sale Potential break through technology poised to o
2021-01-19
Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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Both receptors belong to the large family of
2021-01-19
Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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It is particularly notable that CYP D appears to
2021-01-19
It is particularly notable that CYP2D6 appears to be the most stable of the major CYP450 Mizoribine in its expression over time in vitro and appears to be least affected by culture conditions and sample to sample variability (i.e., CYP2D6 expression is remarkably consistent over time and between in
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