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Generally replacement of the aryl group was well tolerated
2022-01-15
Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations
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Heterocysts provide the required microoxic environment for t
2022-01-15
Heterocysts provide the required microoxic environment for the oxygen-sensitive N2-fixing nitrogenase enzyme complex. This environment is formed during heterocyst development. Developing heterocysts inactivate photosystem II and degrade antenna pigments, thereby decreasing oxygenic photosynthesis (F
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Ca independent release of L C glutamate and GABA that
2022-01-15
Ca2+-independent release of L-[14C]glutamate and [3Н]GABA that occurs via transporters working in the reverse mode also insignificantly increased in vitamin D3 deficiency despite decreased GAT-3 and EAAC-1 GSK1838705A synthesis and neurotransmitter uptake efficacy Fig. 3, Fig. 6 A). However, the up
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Bacterial GluRS comes in two flavors discriminatory GluRS D
2022-01-15
Bacterial GluRS comes in two flavors, discriminatory GluRS (D-GluRS) and non-discriminatory GluRS (ND-GluRS). While D-GluRS exclusively catalyses the transfer of Glu to tRNAGlu, the ND-GluRS can also glutamylate tRNAGln forming Glu-tRNAGln. The misacylated product is then transformed to Gln-tRNAGln
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The mechanism underlying the anorectic effect of OXM is
2022-01-15
The mechanism underlying the anorectic effect of OXM is well established. It is centrally mediated via GLP-1 receptor activation, confirmed by both pharmacological blockade of the GLP-1 receptor, and using GLP-1 receptor knock-out mice [2], [11], [12]. However, the mechanism by which it increases en
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No specific inhibitor of KCC
2022-01-15
No specific inhibitor of KCC has progressed to clinical trials, however, although compounds like H74 were shown to specifically target KCC over the related Na+-K+-2Cl− cotransporter (NKCC) (Ellory et al., 1990). This molecule, or its related analogues, represent compounds of promise. Simple Mg suppl
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The waiting time for first arrival of
2022-01-15
The waiting time for first arrival of AG957 into the dense fraction of 3–4 min at the normal chloride conductance, and about 30 min with inhibition to about 10% of the normal value, signifies that the Gardos channels in the activated cells become maximally or near maximally activated, corresponding
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br Learning from our ancestors As mentioned earlier homologu
2022-01-15
Learning from our ancestors As mentioned earlier, homologues of all γ-secretase components have been identified in plants and protozoans, some of which have emerged as model systems for the study of γ-secretase independent functions of the presenilins [27]. The moss P. patens was the first plant
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These reports have gradually established G quadruplex
2022-01-15
These reports have gradually established G-quadruplex binding small molecules as promising anti-cancer therapeutic agents. Besides the stabilization of G-quadruplex structures, some of these molecules also serve as diagnostic probes and sensors for G-quadruplexes in vitro and in vivo. Of these, Thio
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These observations are of particular
2022-01-14
These observations are of particular interest in the context of recent conceptual changes regarding the mechanisms by which different types of leukocytes contribute to atherogenesis. Over the last decade, the paradigm of the predominant circulatory origin of lesional macrophages has been challenged
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The anti platelet functions of ZGR were
2022-01-14
The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagati
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br Results br Discussion HIV
2022-01-14
Results Discussion HIV reservoirs represent a major barrier to HIV eradication (Archin et al., 2014, Kimata et al., 2016), and substantial research efforts are being directed toward the goal of identifying and eliminating this obstacle to cure (Archin and Margolis, 2014, Pitman et al., 2018).
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Acknowledgements br Introduction Histamine mediates various
2022-01-14
Acknowledgements Introduction Histamine mediates various physiological functions and pathological actions through its interactions with histamine receptors that belong to the superfamily of seven transmembrane G-protein-coupled receptors (GPCRs) (Haas et al., 2008). Four histamine receptor subty
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The observed tendency for higher
2022-01-14
The observed tendency for higher plasma lactate levels in the aerated thermal exposure suggests increased reliance on BV6 metabolism to maintain function. This finding is supported by a recent study that observed an increased ṀO2 in European perch (Perca fluviatilis) exposed to a hyperoxic rather t
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The overall response rate to afatinib is comparable to
2022-01-14
The 13% overall response rate to afatinib is comparable to a 19% response rate reported by Peters et al. [20] in a separate retrospective series investigating the use of afatinib in more heavily pretreated patients with HER2-mutant lung adenocarcinomas. Our 13% response rate is also comparable to an
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