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With an ever increasing incidence rate of type
2022-05-21
With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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RO-3 Next we designed substituents of the
2022-05-21
Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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br Methods br Results and discussion Protein analysis
2022-05-21
Methods Results and discussion Protein analysis of commonly used cell lines (C6, D54-MG, U87, U251 and STTG1) reveals high Quinidine of SXC (Cho and Bannai, 1990, Ye et al., 1999, de Groot et al., 2005, Lyons et al., 2007, Savaskan et al., 2008). Since protein expression can be altered over t
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br Acknowledgements This research was funded by
2022-05-21
Acknowledgements This research was funded by Ministry of Education Malaysia (MOE), and supported by the Department of Nutrition, Exercise & Sports, Department of Drug Design, University of Copenhagen, Denmark and Universiti Malaysia Pahang (UMP), Malaysia. HPLC equipment used for high-resolution
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The energy required to drive the functional process to activ
2022-05-21
The energy required to drive the functional process to actively maintain lens transparency is primarily derived from the metabolism of glucose. Since the lens is avascular and exists in an environment of low oxygen tension, glucose is primarily metabolized by aurora kinase inhibitor glycolysis (Kin
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br Conclusion In conclusion SHP was
2022-05-21
Conclusion In conclusion, SHP289-04 was demonstrated as a potent glucokinase activator. It could normalize the blood glucose level and lipid level in spontaneous type 2 diabetes model KKAy mice. At the same time, it ameliorated the function of islets and liver in KKAy mice. It had been proved to
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br Conflict of interest br Introduction Since
2022-05-21
Conflict of interest Introduction Since its discovery in 1958 [1]the Ca2+-dependent K+ efflux in human red blood porcine (RBC) (further referred to as the Gárdos effect) has been extensively studied (see 2, 3for review) and has been helpful in understanding the role of the Ca2+-activated K+ ch
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By using pharmacological treatment with CBX or transgenic an
2022-05-21
By using pharmacological treatment with CBX or transgenic animals lacking the two major astroglial Cxs, the Double KO mouse, we demonstrated that the gap-FRAP technique was able to detect the total inhibition of GJC with a reduction of about 39% and 38% compared to control, respectively. The residua
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br Galanin in depression A
2022-05-21
Galanin in depression A major impediment in depression research is the lack of validated animals´ models. Animals not only lack consciousness of self, self-reflection and consideration of others but also hallmarks of the disorder such as depressed mood, low self-esteem or suicidal intent are hard
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The schematic diagram of the antagonistic interactions of Zn
2022-05-21
The schematic diagram of the antagonistic interactions of Zn2+ and neurosteroids (NSs) at GABA-A receptors is summarized in Fig. 7. Neurosteroids exhibit powerful seizure protective effects against experimental seizures probably through the potentiation of synaptic and extrasynaptic GABA-A receptor-
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Mallory stained sections showed significant increase in
2022-05-21
Mallory stained sections showed significant increase in collagen fiber deposition around the hepatic nodules together with significant increase in positive immune-reaction to α-SMA in TAA-treated group. This was in accordance with previous studies which reported that myofibroblasts which were develo
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Several other assay parameters were also explored First the
2022-05-20
Several other assay parameters were also explored. First, the thermal dependence of the assay was investigated by measuring the specific activity at different temperatures (Fig. 7). That data show that enzymatic activity increases with increasing temperature. Interestingly, the observed rate increas
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Syt itself does not catalyze lipid mixing and
2022-05-20
Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisely
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A recent novel and important finding is
2022-05-20
A recent novel and important finding is that YAP connects cellular growth with anabolism; YAP suppresses the transcriptional induction of genes which importantly regulate gluconeogenesis in the liver; namely glucose-6-phosphatase catalytic subunit (G6PC) and phosphoenolpyruvate carboxykinase 1 (PCK1
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br Experimental section br Results and discussion br Conclus
2022-05-20
Experimental section Results and discussion Conclusion The evaluation of the inhibitory potential of these derivatives towards eight kinases showed that the brominated hybrids (3k) and (3l) are the most active against the PIM1 and CLK1 kinases. The methylation of the nitrogen K-Ras(G12C) in
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