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Transcriptional translational modulators The discovery that
2021-12-27
Transcriptional/translational modulators. The discovery that β-lactam antibiotics like ceftriaxone enhance the in vivo expression of EAAT2/GLT-1 [31] has pioneered a completely new approach to EAAT modulation, with several additional EAAT activators following in its trail (Figure 2b) [32, 33, 34•, 3
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br Ligand binding free energies In order to compute
2021-12-27
Ligand-binding free energies In order to compute the absolute free Vatalanib 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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5-alpha reductase inhibitors To confirm that these were bona
2021-12-27
To confirm that these were bona fide interactions, we investigated whether the potassium channel subunits or Tmem263 formed complexes with GLT-1 or DAT after immunoprecipitation. Lysates of HEK-293 cells previously cotransfected with HA-GLT-1 or HA-DAT, and either YFP-Kv7.3, YFP-Kv7.2 or YFP-Kv7.5 w
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Transmembrane AMPA receptor regulatory proteins TARPs
2021-12-27
Transmembrane AMPA receptor regulatory proteins (TARPs) are a relatively newly discovered protein family. Prototypic TARP, stargazin, was found by a spontaneous mutation in ataxic stargazer mouse line as a homologous protein to γ1 calcium channel subunit (Letts et al., 1998). The role of stargazin i
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br Introduction Farnesoid X receptor FXR
2021-12-24
Introduction Farnesoid X receptor (FXR) is a bile Dopamine HCl 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) that
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More specific quantitative assays for DiXaIs are based on th
2021-12-24
More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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br Characterization of quantal exocytosis by
2021-12-24
Characterization of quantal exocytosis by amperometry A secretory vesicle experiences four phases during exocytosis: (i) cargo packaging & translocation, (ii) vesicle docking & priming; (iii) fusion pore formation; (iv) fusion pore expansion and cargo secretion (Fig. 1a). The release of monoamine
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To our knowledge the putative role of
2021-12-24
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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The synthesis of substituted pyrimidinone carboxamides
2021-12-24
The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of Boc-MLF provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to afford inseparabl
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Our results further indicate that
2021-12-24
Our results further indicate that low expression of p300/CBP in CRC is directly associated with poor clinical therapeutic outcome of 5-FU treatment, potentially providing a new set of biomarkers to predict chemo-sensitivity. Although the ability of low expression of p300/CBP to predict poor prognosi
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The present results indicate that oxidative
2021-12-24
The present results indicate that oxidative damage in CFS muscles is not due to the decline in the efficiency of antioxidative enzymes. This suggests that there is an increase in the generation of reactive oxygen species consistent with a mitochondrial origin of the damage. Mitochondria represent th
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Activity of compound in rat brain tissue highlights
2021-12-24
Activity of compound 10 in rat 1115 mg tissue highlights the potential to use this new class of allosteric sGC inhibitors to study the role of the NO—sGC—cGMP signalling pathway in the brain. Reducing amounts of cGMP in cells would have implications in downstream signalling proteins, such as cGMP-de
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In addition to gonadotropes GnRHRs have also been
2021-12-24
In addition to gonadotropes, GnRHRs have also been detected on somatotropes, lactotropes, thyrotropes, melanotropes, somatolactin (SL) cells, and/or corticotropes using immunohistochemical, radioligand-binding, or mRNA expression approaches across species; including fishes, rats, and humans (La Rosa
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Mapping and separation of the anti
2021-12-24
Mapping and separation of the anti-GlyT1C epitopes allowed us to verify the existence of calpain cleavage sites in isolated mouse synaptosomes. In order to allow calcium to enter the intrasynaptosomal compartment and activate endogenous calpain, we incubated synaptosomes in hypoosmotic high (200μM)
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The need for an inflammatory risk profile was recently
2021-12-24
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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