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br Introduction Glucokinase GCK hexokinase
2021-10-29

Introduction Glucokinase (GCK, hexokinase IV) is a monomeric enzyme that catalyzes the ATP-dependent conversion of glucose to glucose 6-phosphate, the first and rate-limiting step of glycolysis in the liver and pancreas [1,2]. GCK was first discovered in the early 1960's, and shortly thereafter i
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br Introduction The glucagon receptor GCGR is a G
2021-10-29

Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m
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motilin receptor Inhibitors of the G rdos effect
2021-10-29

Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic
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Analysis of the i motif structures during
2021-10-29

Analysis of the i-motif structures during biased unfolding of G-quadruplexes leads to the conclusion that at acidic pH the i-motif is absolutely unaffected by that process. The hydrogen bonds within the i-motif are intact (Fig. 3D) and they only fluctuate around mean values. On the other hand, the i
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All of the abovementioned effects of PUFAs
2021-10-29

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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Considering together the conformational docking
2021-10-29

Considering together the conformational, docking and SAR results of this and of previously published papers, a three points pharmacophore model can be developed considering the indispensable residues of SRSRY derived antagonists, namely Arg89, Arg91 and Tyr92. This model is shown in Fig. 10, and req
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To date the underlying mechanism of ropivacaine in
2021-10-29

To date, the underlying mechanism of ropivacaine in inducing neurotoxicity remains unclear. Cell death was intimately involved in local-anesthetic neurotoxicity [6,18]. Two classic signaling pathways triggered cell death: the extrinsic pathway and the intrinsic pathway [12]. Our study demonstrated t
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To our knowledge the putative role of ET
2021-10-29

To our knowledge, the putative role of ET-1 and ETB-R in oligodendroglioma progression was not documented so far. Using primary cultures of grade B oligodendroglial tumor cells, we have here assessed the functionality of ETB-R expression in these tumors. Confocal microscopy analysis confirmed the st
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Genome wide binding and transcriptome analyses demonstrate
2021-10-29

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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br Materials and methods br
2021-10-29

Materials and methods Results Discussion Type I ECa is associated with estrogen excess, obesity and hormone-receptor positivity. However, the function of ERα on ECa is considered complicated. The expression of ERα is reduced in grade III ECa clinical samples [13]. The high ERα expression is
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Sometime ago we have described diamino triazines as histamin
2021-10-29

Sometime ago we have described diamino-1,3,5-triazines as histamine H4R ligands,12, 13 and aryl derivatives of the 1,3,5-triazine, which attenuated inflammatory and nociceptive response in vivo in the rodent models of inflammation induced by JNJ-26854165 synthesis and zymosan. In this work we descr
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Furthermore increased plasma levels of endoglin have
2021-10-28

Furthermore, increased plasma levels of endoglin have been associated with diabetic complications (Valbuena-Diez et al., 2012). The involvement of soluble endoglin in a number of widespread pathologies demonstrates that endoglin is not only marker of endothelial integrity but also a causative factor
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SB 242084 The importance of FXR FGF signaling in BA homeosta
2021-10-28

The importance of FXR-FGF15/19 signaling in BA homeostasis is illustrated by various BA malabsorption syndromes. Clinically, BA malabsorption causes diarrhea due to high BA concentrations in the colon that lead to secretion of water and electrolytes and stimulation of propulsive contractions [36]. P
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br Ligand binding free energies In order to
2021-10-28

Ligand-binding free energies In order to compute the absolute free 5-hme-CTP associated with binding a ligand to a flexible iGluR LBD, a theory that accounts for all the principal thermodynamic contributions from ligand docking and LBD closure had to be developed. This was accomplished using an
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pHi regulation in astrocytes has been examined primarily
2021-10-28

pHi regulation in astrocytes has been examined primarily in cell culture rather than in situ. Two HCO3−-dependent transporters, NBC and Na+-driven Cl-HCO3 exchange (NDCBE), have been described [10,16], in addition to Cl-HCO3 anion exchange (AE) [96]. Culture studies indicate that NHE is the principa
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