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Further insight in how exactly galanin might inhibit
2021-12-06
Further insight in how exactly galanin might inhibit seizures was obtained from galanin transgenic mice. It occurred that the altered susceptibility to seizures was in direct correlation with glutamate release from hippocampal slices obtained from these animals (Fig. 2(b)). While no differences were
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With the identification of small
2021-12-06
With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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Regulation of FGF signalling is critical to ensure a
2021-12-06
Regulation of FGF signalling is critical to ensure a balanced response to receptor stimulation. This occurs largely through negative feedback mechanisms, including receptor internalisation via ubiquitination (Wang et al., 2002) and induction of negative regulators, for example SPRY, SPRED 1 and 2 an
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Fibroblast growth factor receptors FGFRs play an essential r
2021-12-06
Fibroblast growth factor receptors (FGFRs) play an essential role in the regulation of cell survival, proliferation, migration and differentiation. FGFRs are a family of receptor tyrosine kinases (RTKs) exhibiting an extracellular immunoglobulin (Ig)-like ligand binding domain, a transmembrane domai
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Interestingly the subcellular localization of FBPase in hepa
2021-12-06
Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Pramipexole reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the abi
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Septic shock a condition where
2021-12-06
Septic shock, a condition where endothelium-derived substances most likely play an important role, is often accompanied by cardiac dysfunction, pulmonary hypertension, systemic hypotension and impaired oxygen utilisation with systemic acidosis (Vincent, 1998). Experimental endotoxaemia shows a simil
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Some years ago it has been
2021-12-06
Some years ago, it has been described that CD45RA+ CD62L+ naïve CD4+ T DCPIB can be further differentiated into two distinct subpopulations by analysing their surface expression of CD31(Kimmig et al., 2002a; Kohler and Thiel, 2009; Kohler et al., 2005b). CD31+ thymicnaive CD4+ T cells are enriched
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The need for an inflammatory risk profile
2021-12-06
The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab
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To assess whether this coupling mechanisms
2021-12-06
To assess whether this coupling mechanisms might operate also in a native system of untransfected cells, we select a cell line SH-SY5Y neuroblastoma that is known to express both the dopamine transporter and the M-currents (Jiang et al., 2004; Wickenden et al., 2008). These experiments were performe
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elvitegravir br Acknowledgments The financial support from t
2021-12-06
Acknowledgments The financial support from the National Natural Science Foundation of China (Nos. 31460422 and 31060210), the Natural Science Foundation of Jiangxi Province, China (20171BAB204029 and 20143ACB20006), the Project of Science and Technology of Jiangxi Provincial Education Department,
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It was previously proposed that glucagon
2021-12-06
It was previously proposed that glucagon acts in the liver, in which a signal is produced and relayed to the ABT via vagal nerves [8], [36], [37]. The concept that the liver is the primary target site was supported by the studies reporting that the glucagon receptor is localized in the liver but not
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br Introduction Connexins are transmembrane proteins that al
2021-12-06
Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent Flavin adenine dinucleotide receptor via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nu
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In order to address the
2021-12-06
In order to address the Cyp inhibition issue, we tested the possibility of further changes in the heterocycle combined with reducing the electron density in the ring system by swapping the central aniline nitrogen atom for a ketone. details the synthesis of these analogs, which started with 7-bromo
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We have previously designed an azobenzene
2021-12-04
We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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rifampicin Herein we describe the design and optimization of
2021-12-04
Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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