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Introduction The brain contains abundant fatty acids which s
2022-03-22
Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in dev
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It is important to control hyperglycaemia because it
2022-03-22
It is important to control hyperglycaemia because it can contribute to serious complications. Hyperglycaemia can be managed by maintaining stable blood glucose levels inside the normal range. This can be achieved by various strategies such as diet, medications and exercise (O’Keefe & Bell, 2007). Se
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Nevertheless in the brain we found that trehalose phosphoryl
2022-03-22
Nevertheless, in the brain, we found that trehalose phosphorylates AMPK, which is a metabolic sensor. AMPK is known to be transiently activated in muscle by acute exercise [21,22]. Bayod et al. also reported that AMPK was significantly activated in both the cerebral cortex and hippocampus in exercis
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The usefulness of GIP R antagonism for the treatment of
2022-03-22
The usefulness of GIP-R antagonism for the treatment of obesity-diabetes has been revealed in numerous studies employing knockout or chemical blockade of GIP-R signalling.*88, 89, *90, 91, 92, 93, 94, 95, 96, *97 For example, sub-chronic daily administration of (Pro3)GIP to ob/ob mice results in sig
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Recently they reported an enyne chemotype agonist Fig with l
2022-03-22
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral Oseltamivir acid mg (tmax=15min) and a decent pharmacokinetic pro
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High lipophilicity of seems to
2022-03-22
High lipophilicity of seems to cause poor PK profiles. First we replaced the phenyl ring of compound with various hetero aromatic rings to reduce lipophilicity, (). The synthesis of pyridine derivative was shown in . (2′,6′-Dimethylbiphenyl-3-yl)methanol () was reacted with 2,5-dibromopyridine i
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Our paper also contributes to the
2022-03-22
Our paper also contributes to the large, but hitherto inconclusive literature that studies the effects of option-based compensation or convexity in compensation on corporate risk-taking policies. On the one hand, some studies document a positive relationship by showing that convexity increases lever
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Dysregulation of the HPA axis resulting in alteration to bot
2022-03-22
Dysregulation of the HPA axis, resulting in alteration to both baseline and stress-induced glucocorticoid levels (e.g., cortisol and corticosterone), has been implicated in several diseases and psychopathologies, including anxiety (McEwen et al., 2015, 2016; Shin and Liberzon, 2010). For example, ba
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The translational relevance of our
2022-03-22
The translational relevance of our findings remains uncertain at this point. On the one hand, there have been reports to suggest that boosting KDM4 activity may engender beneficial effects in vivo. For instance, Li et al. have show that KDM4 interacts with β-catenin to mediate Wnt signaling in hepat
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The histamine H receptor H R amino acids is
2022-03-22
The histamine H3 receptor (H3R; 326–445 amino-acids) is located on histaminergic neuron somata, dendrites and axon varicosities, as well as on the axon varicosities and somata of other neurons, providing negative feedback to inhibit histamine synthesis and the release of histamine or other transmitt
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br Although there are growing bodies of research dealing
2022-03-22
Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a
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In hypoxic breast cancer cells BNIP mediated autophagy activ
2022-03-22
In hypoxic breast cancer cells, BNIP3-mediated autophagy activation and elevation of amino Clarithromycin levels were notable. BNIP3, a BCL-2 family protein, is known to be transcriptionally regulated by HIF-1α and to be involved in cancer cell death in hypoxic conditions [51]. As a link to autopha
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An important aspect of macrophage biology highly influenced
2022-03-21
An important aspect of macrophage biology, highly influenced by HO-1 activity, is macrophage polarization. The broadest classification, based on the in vitro stimulation, surface marker expression, and inflammatory cytokines production, describes macrophages as classically activated, proinflammatory
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The different NO stimulated and ODQ inhibited cNMP patterns
2022-03-21
The different NO-stimulated and ODQ-inhibited cNMP patterns in terms of absolute and relative magnitude and time course reported herein suggest distinct functional roles of cGMP, cCMP and cUMP. Therefore, it will be necessary to dissect cellular effects of these cNMPs in numerous cell systems. For t
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The use of antiinflammatory agents has been suggested as
2022-03-21
The use of antiinflammatory agents has been suggested as a potential treatment in HF. One strategy targeted tumor necrosis factor (TNF) in HF,, but the negative results of the clinical trials have been discouraging., Other clinical trials have attempted to suppress proinflammatory cytokine product
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