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Based on the above considerations the galactosidase gene fro
2021-11-09
Based on the above considerations, the β-galactosidase gene from Exiguobacterium acetylicum MF03 (not previously reported) was cloned, expressed and purified with the aim of assessing the potential of this novel enzyme for catalyzing reactions of synthesis and hydrolysis of glycosides. Because of E.
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In conclusion we have shown that the brain penetrating abili
2021-11-09
In conclusion, we have shown that the brain penetrating ability of heteroaryl piperazine and piperadine ureas can be modulated through small structural changes to the heteroarenes, the piperazine or piperidine core, and the biaryl ether tail. Compounds exhibiting / ratios ranging as high as 4.2:1 to
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When studying the potential of HATi
2021-11-09
When studying the potential of HATi for the treatment of inflammatory lung diseases, investigating lung tissue specific effects may be particularly relevant since local administration of small molecule inhibitors in lung tissue is possible and is already applied for inhaled glucocorticoids in the tr
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br Dual acting HR antagonists While the
2021-11-09
Dual-acting HR antagonists While the present medicinal chemistry efforts are mainly focused on selective ligands targeting GPCRs, and particularly on H1R, H3R and H4R selective antagonists/agonists, there were and, also, still are several efforts to develop dual acting H1R/H2R, H1R/H3R and H3R/H4
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The other possibility for the
2021-11-09
The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,
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br Acknowledgements This work was supported by grants from
2021-11-09
Acknowledgements This work was supported by grants from the Agencia Nacional de Promoción Científica y Tecnológica (PICT2013-0495, PICT2016-1821), and from CONICET (PIP 2013-562), as well as from Fundación René Barón and Fundación Williams. Introduction Histamine poisoning, also known as scom
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Membrane based integrative treatment processes emerge as pot
2021-11-08
Membrane based integrative treatment processes emerge as potential solution compared to the conventional techniques. Gisi et al. (2009) presented a treatment scheme for tannery wastewater consisting of a biological pre-treatment and then a polymer as coagulant followed by reverse 98059 with a plane
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things br Discussion Regulation of redox homeostasis is crit
2021-11-08
Discussion Regulation of redox homeostasis is critical in the maintenance of normal cell functions, and both glutathione S-transferase and peroxiredoxin enzymes are important contributors to this process. There are numerous reports of aberrant expression patterns of GSTP linked with cancer and wi
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The experiments reported herein were designed to test whethe
2021-11-08
The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w
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br Endogenous and synthetic ligands of GPR There are
2021-11-08
Endogenous and synthetic ligands of GPR55 There are currently limited commercially available synthetic agonists and antagonists that are specific for GPR55. A large number of studies have investigated the pharmacology of GPR55 4, 23, 25, 30, 31, 32, 33, 34, 35, with contradictory findings reporte
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Ironically another series of studies examining the role
2021-11-08
Ironically, another series of studies examining the role of EAATs in CNS injury and disease suggest that under some pathological conditions, the operation of the EAATs is not protective, but actually contributes to the excitotoxic process (Rossi et al., 2000). The transporters do so by serving as th
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br The concept of the axo myelin synapse
2021-11-08
The concept of the axo-myelin ‘synapse’ Axons can release glutamate in a Ca+-dependent and independent manner (reviewed in [13,69]). Glutamate released from axons activates GluRs located in myelin, a feature that gave rise to the idea of the axo-myelin ‘synapse’ by analogy with classical synaptic
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In order to elucidate the reasons of high efficacy of
2021-11-08
In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen (-)-epicatechin of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μM), wh
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FFAs concentration response curves for increasing intracellu
2021-11-08
FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto
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5,7-Dichlorokynurenic acid receptor Recent evidence indicate
2021-11-08
Recent evidence indicates that prolonged vasoconstriction of conductance and resistance arteries involves VSMCs 5,7-Dichlorokynurenic acid receptor polymerization, through activation of small GTPases [4] and a subsequently transition to a more solid rheology [5]. Actin polymerization occurs in two
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