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Focal adhesion kinase Fakir et
2021-09-27
Focal adhesion kinase (Fakir et al., 2006), also known as non-receptor tyrosine kinase (PTK2), is a 125-kDa protein that regulates cell migration, adhesion, proliferation, and survival (Tavora et al., 2014; Yang et al., 2016; Tian et al., 2017). Many studies have observed FAK overexpression and/or h
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br Formation of secretory vesicles and trafficking toward pl
2021-09-27
Formation of secretory vesicles and trafficking toward plasma membrane Insulin and other components of the secretory granules are sorting and providing certain cues for E-64-d off the adjacent TGN membrane, forming immature secretory clathrin coated vesicles (Gehart and Ricci, 2013). Bin/Amphiphy
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We examined the expression of notch in the brains
2021-09-27
We examined the expression of notch-1 in the brains of mice following morphine or oxycodone tolerance. The results showed that notch-1 levels did not change following morphine or oxycodone tolerance, with or without the treatment of IRL-1620. This indicates the possibility that morphine or oxycodon
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br Drugs approved or in development
2021-09-27
Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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P Benzoxaborole substituted macrocyclic compounds
2021-09-27
P4-Benzoxaborole-substituted macrocyclic compounds based on ITMN-191 scaffold were prepared using a general scheme as shown in . ITMN-191 was prepared by following a patent procedure. The P4 BOC group was removed by treatment with TFA in dichloromethane to give amine . The coupling of the amine to 6
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Compound containing dimethylglutarimide P cap P propyl
2021-09-27
Compound containing, dimethylglutarimide P-cap, P propyl group, α-methylbenzyl urea resulted in inhibitor with much improved binding (=0.064μM) and EC=0.3μM. This was an aza-peptide analog with an EC comparable to our first generation clinical candidate . Analog was evaluated for its selectivity aga
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A nitric oxide donor glyceryl trinitrite
2021-09-27
A nitric oxide donor, glyceryl-trinitrite, and the substrate for nitric oxide, l-arginine, have been used to treat preterm labor. However, these studies are preliminary. The beneficial effect of nitric oxide donors needs to be confirmed by more controlled studies. The probable pitfall of using nitri
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In addition to these effects on metabolic
2021-09-27
In addition to these effects on metabolic function in cardiac cells, this study also demonstrates changes in the expression of hypertrophic genes and proteins subsequent to GPR119 activation. Again this occurred in a distinct pattern dependent on palmitate exposure. Of interest SOCS3 mRNAs were decr
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The activation of the ERK pathway
2021-09-27
The activation of the ERK pathway may participate in the sensitization of primary afferents in pain transmission (Ji et al., 2009, Lai et al., 2011); the blockade of ERK activation in the DRG can decrease mechanical and heat hypersensitivity in inflammatory pain. IL-10 can inhibit phosphorylation of
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br Acknowledgments This research was supported
2021-09-26
Acknowledgments This research was supported by a grant from the Korea Health Technology R&D Project through the Korean Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (grant number: HI17C0616). Dr. Jun-Mo Yang was supported by the Natio
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A main finding of this study
2021-09-26
A main finding of this study was that the impact of exogenous insulin on hippocampal memory and glucose utilization was GluT4-dependent. Although insulin was administered directly to the hippocampus, it is important to point out that such administration does indeed have physiological relevance; that
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However ghrelin has a short half life of
2021-09-26
However, ghrelin has a short half-life of 15–20 min, because it is a natural peptide containing 28-amino acids, its clinical usefulness as a therapeutic agent may be limited (Mosińska et al., 2017; Vestergaard et al., 2007). Hence, many efforts have been made to elucidate the smallest segment of ghr
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Artemisinine It is important to underline that although ghre
2021-09-26
It is important to underline that Artemisinine although ghrelin increases the motivation to eat even in fed state, its effects on food intake and reward are blunted in obese animal models (Zigman et al., 2016). This emphasizes also the interconnection between homeostatic regulation of food intake a
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The GAL also modified HT system
2021-09-26
The GAL(1–15) also modified 5-HT system (Millon et al., 2015). Using a rat medullary raphe-derived cell line RN33B, we observed that GAL(1–15) significantly decreased the 5-HT immunoreactivity in the RN33B third (p Conclusion All these data emphasized the role of GAL and its N-Terminal fragment (
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Angiotensin I (human, mouse, rat) Similarly spectrophotometr
2021-09-26
Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant Angiotensin I (human, mouse, rat) band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a
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