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In summary through medicinal chemistry design and computer
2021-10-27
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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Previously we have shown that ghrelin and cannabinoids stimu
2021-10-27
Previously, we have shown that ghrelin and cannabinoids stimulate hypothalamic AMPK activity (Kola et al., 2005). In contrast, both the orexigenic compounds have inhibitory effects on AMPK activity in the liver and visceral fat (Kola et al., 2005). In this study, we were able to reproduce our previo
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br Experimental section br Acknowledgements This
2021-10-27
Experimental section Acknowledgements This study was supported by grants from the National Natural Science Foundation of China (Grants 81673299 and 81273376). Introduction Free fatty acids (FFAs) are important metabolic fuels and those that are polyunsaturated are essential components of t
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Several transgenic and knockout congenic mouse models have
2021-10-27
Several transgenic and knockout/congenic mouse models have been generated in order to assess the role of FFAR1 for proper insulin secretion and maintenance of glucose homeostasis. The results obtained with three different receptor knockout mouse models were not consistent. The protection against hig
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br Conclusion We have demonstrated
2021-10-27
Conclusion We have demonstrated that ETB receptors negatively regulate the expression of AT1 receptors in renal proximal tubule 3,4-DAA from WKY rats but not in SHRs. Short-term activation of the ETB receptor increases AT1 receptor phosphorylation in WKY cells but decreases it in SHR cells. We c
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br Discussion Considering cardiovascular risk factors there
2021-10-27
Discussion Considering cardiovascular risk factors, there was a significant difference in prevalence of dyslipidemia in both groups, 57.5% in HIV-infected stroke patients compared to 8.9% in the HIV-uninfected patients. These results are similar to that of Chow et al. who found a dyslipidemia pre
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The finding that a peptide consisting of
2021-10-27
The finding that a peptide consisting of d-amino acids binds to LSD1-CoREST1 with equal affinity as the l-amino Ro3306 ligand indicates that the assays detect a generally non-specific association between two highly charged molecules. Nonetheless, p53-CTD is an effective inhibitor of LSD1 and its bin
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There is abundant literature about different
2021-10-26
There is abundant literature about different functional aspects of the cannabinoid system (Badal et al., 2017, Balenga et al., 2011, Henderson-Redmond et al., 2016, Nair et al., 2015); however, not a great deal is known about the mechanism by which ethanol impacts its function in connection to the i
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br Niacin has long been
2021-10-26
Niacin () () has long been used for the treatment of lipid disorders and for the prevention of cardiovascular disease, the leading cause of death in the U.S., as a result of its ability to raise high-density lipoprotein (HDL) levels. Recent mechanistic investigations have shown that niacin may exe
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br Introduction Adipose tissue AT
2021-10-26
Introduction Adipose tissue (AT), in addition to its function as g 36 australia storage, is an important endocrine organ and it secretes adipokines (Ahima, 2006). Adipose tissue is related to different physiological processes such as energy metabolism, insulin sensitivity, and inflammation. One
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Transient forebrain ischemia in rodents induces a
2021-10-26
Transient forebrain ischemia in rodents induces a reduction in expression of mRNA encoding the AMPA receptor subunit GluR265, 66, 67, 68, 69 (Fig. 3). gluR2 mRNA expression is markedly reduced in the CA1 region (the α-Bungarotoxin region most vulnerable to ischemia-induced damage), but not in the C
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Multiple mechanisms have been suggested by which glucagon ca
2021-10-26
Multiple mechanisms have been suggested by which glucagon can increase energy expenditure although none have been conclusively proven to be responsible. Both enhanced gluconeogenesis and enhanced protein turnover secondary to hyperglucagonaemia have been suggested as the reason for the increased met
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br Redox cancer therapy The
2021-10-25
Redox cancer therapy The understanding of ROS mechanisms supported the development of two parallel anticancer strategies based on ROS modulation, the use of antioxidants for cancer prevention and the use of ROS inducers to exacerbate oxidative stress to lead cancer s equol to death [27], [133].
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The newly synthesized compounds were evaluated
2021-10-25
The newly synthesized compounds were evaluated for their FAAH inhibitory activity in vitro. In addition, molecular modeling, selectivity and reversibility behavior of the new class of FAAH inhibitors are presented in this article. Results and discussion The potency of inhibition on the human rec
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Genome wide binding and transcriptome analyses demonstrate t
2021-10-25
Genome-wide binding and transcriptome analyses demonstrate that Fbxl10 directly binds the Areg, Mdk, Lmnb1, Thbs1, Mgp and Cxcl12 locus and thereby might influences the expression of these migration associated genes. The expression of epidermal growth factor (EGF)-like molecule Amphiregulin (Areg)
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