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With the exception of R none
2022-03-10

With the exception of R5.40310, none of the other residues would appear to be in a position to mediate direct agonist interactions in the active state GLP-1R structures. ECL2 within the GLP-1R is important for affinity and efficacy of both extended and processed GLP-1 peptides [24]. Though distal fr
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Murine models of sickle disease have
2022-03-10

Murine models of sickle disease have been valuable tools in the study of human SCD pathogenesis [15], [16], and will continue to be central to development of novel approaches to disease treatment. The SAD mouse model of sickle disease is particularly remarkable for its erythrocyte dehydration phenot
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Emergent studies have recently shown
2022-03-10

Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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br Discussion The model of a NVU
2022-03-10

Discussion The model of a NVU described by Mathias et al. (2018) has been implemented on the macro scale (see Kenny et al. (2018b)) via a 2D cerebral tissue slice coupled to a vascular tree. In particular, further communication within the tissue slice has been implemented via extracellular ion el
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br Gap junctions hemichannels and connexins Molecular charac
2022-03-10

Gap junctions, hemichannels and connexins: Molecular characteristics and function Cell-to-cell communication is of extreme importance in tissue homeostasis, which is maintained by transmission of regulatory signals (Fig. 1). Intercellular communication via gap junctions (GJs) represents one of th
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However protection against kainic acid induced
2022-03-10

However, protection against kainic acid-induced injury was not found by Lin et al. (2003) in the rats with AAV-GAL vector-mediated galanin overexpression, even though these animals, as mentioned earlier, exhibited attenuated of seizure severity. Although the reason for the controversy between the st
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br Acknowledgments This research was supported in part by Na
2022-03-10

Acknowledgments This research was supported in part by National Institutes of Health IDeA Program COBRE grant GM110732; a USDA National Institute of Food and Agriculture Hatch project; and the Montana State University Agricultural Experiment Station. Introduction Propofol (2,6-Diisopropylphen
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Considering together the conformational docking and SAR resu
2022-03-10

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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br FAAH regulation of ECB signaling ECBs are
2022-03-10

FAAH regulation of ECB signaling ECBs are fatty Hydrochlorothiazide amides and monoacylglyerols functioning as neuromodulator lipids that exhibit rapid (within seconds) on-demand biosynthesis in response to neuronal activation, and are subsequently degraded by specialized catabolic enzymes. There
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During the activation of the coagulation cascade factor Xa
2022-03-10

During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium HNGF6A on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit platele
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FXa is a vitamin K dependent
2022-03-10

FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 AI-3 and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102 exhibits the trypsin-like β-barrel structure [12]. The active s
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The biochemical cell culture activities
2022-03-10

The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chloride
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Despite such extensive analysis of Gcn
2022-03-10

Despite such extensive analysis of Gcn5 homologs, the function of C. albicans Gcn5 (CaGcn5) is not well understood. Therefore, in this study we investigated the role of CaGcn5 in filamentous growth, invasive growth and stress response of C. albicans. We also examined the subcellular distribution of
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As evidenced by SARs and crystallographic data HO
2022-03-10

As evidenced by SARs and crystallographic data, HO-1 has at least three main crucial regions for inhibitor binding. The most crucial area, the so-called eastern region, is able to allocate the azole ring that represents the first anchoring point by establishing a coordination binding to the heme fer
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The endocytic inhibitors MDC and CPZ
2022-03-10

The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat
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