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br Introduction G protein coupled receptors
2022-05-09
Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign
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br Conflicts of interest br Acknowledgements This research w
2022-05-09
Conflicts of interest Acknowledgements This research was supported by grants from National Research Foundation, Korea (NRF-2017RIDIA3B04033313) and Yeungnam University (216-A-061-042). Introduction Kluyveromyces lactis is a yeast that produces one of the ß-galactosidases (ß-gals) most wide
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br Introduction Farnesoid X receptor
2022-05-09
Introduction Farnesoid X receptor (FXR) is a bile nuclear receptor regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) t
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In addition several other considerations were made for
2022-05-09
In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty Probenecid mg receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were
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Fatty acid amide hydrolase FAAH is
2022-05-09
Fatty LY 303511 synthesis amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion
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Our results on the other hand shows that there is
2022-05-09
Our results, on the other hand, shows that there is no upregulation of ETBR on the spinal cord after SCI, but there is a significant difference of mRNA on days 2, 7 and 28 on the SCI group on the spinal cord and no changes on the DRG, suggesting that the spinal cord injury may reduce the renovation
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To solve the atomic structures
2022-05-09
To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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Recent evidence suggests that HCA can also mediate
2022-05-07
Recent evidence suggests that HCA2 can also mediate antineuroinflammatory effects [63]. Studies in this field were initiated when monomethyl fumarate, the metabolite of DMF, was shown to be an agonist of HCA2[5]. DMF at the same time was shown to not only have beneficial effects in the treatment of
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Next we designed substituents of the
2022-05-07
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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This resembles a vicious cycle since BBB
2022-05-07
This resembles a vicious cycle since BBB disruption and inflammation are thought to be caused by epilepsy, but other contributing factors are also known to be their cause, such as peripheral infection, autoimmunity, Hydroxyzine 2HCl trauma and stroke that also underlie epilepsy [18]. Additional tri
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GKRP binds to the inactive super
2022-05-07
GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t
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br Introduction GPR also known as free fatty acid receptor
2022-05-07
Introduction GPR40 (also known as free fatty bafilomycin a1 autophagy receptor 1), a member of the G-protein coupled receptor (GPCR) family, is expressed in pancreatic beta cells, intestine and the central nervous system (Bekinschtein et al., 2008; Itoh et al., 2003). It is activated by medium-
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br Conflict of interest br Acknowledgments The research was
2022-05-07
Conflict of interest Acknowledgments The research was funded by the Major Programs of Pharmaceutical research project of Jiangsu Province (Q2018044). Introduction Lipids are important regulators of cell death. In mammalian cells, both apoptotic and non-apoptotic cell death pathways can be
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The deduced amino acid sequences
2022-05-07
The deduced amino AZD2932 sequences of all scIPPSs display high similarity, and sequence alignments reveal seven conserved regions [2]. Regions II and VI contain the substrate-binding regions, with two characteristic aspartate-rich motifs (DDx(xx)xD; where x represents any amino acid residue). Regi
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br Materials and methods br Results br
2022-05-07
Materials and methods Results Discussion Cell migration not only plays major roles in physiological events, such as embryo implantation, embryogenesis, morphogenesis, neurogenesis, angiogenesis, wound healing and inflammation [[29], [30], [31]], but it is also implicated in the pathophysiol
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