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Similarly Somavarapu and Kepp constructed a
2022-03-22

Similarly, Somavarapu and Kepp [29] constructed a PS1 homology model using 4HYG as a template, plus modeling the TM6-TM7 intracellular segment (amino acids 273 to 374). In this study, the authors considered for the first time the mature and immature (not autoproteolyzed) forms of PS1 component, sinc
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Recently a lot of synthetic FFA agonists
2022-03-22

Recently, a lot of synthetic FFA1 agonists containing acidic moieties have been reported (Fig. 1) [13], [14], [15], [16], [17], [18], [19], [20], [21]. Notably, most of FFA1 agonists usually have the common biphenyl scaffold, which resulted in a relative deprivation in structure types of agonists [2
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FFAs concentration response curves for increasing intracellu
2022-03-22

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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The F P concentration reported for a resting rabbit
2022-03-22

The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase
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Liver and muscle isozymes have been found in vertebrate tiss
2022-03-22

Liver and muscle isozymes have been found in vertebrate tissues [2], [5], [6]. The liver FBPase is recognized as a regulatory enzyme of gluconeogenesis. The muscle isozyme participates in the glycogen synthesis from lactate and in the regulation of glycolysis [7], [8], [9]. The basic difference betw
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Several observations about structure activity relationships
2022-03-22

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic NVP-BEP800 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage
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T7 High Yield RNA Compounds and were evaluated for their pha
2022-03-22

Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure w
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Although HK localizes mainly to either the
2022-03-22

Although HK localizes mainly to either the cytosol or mitochondria [29], [30], [31] and cardioprotection is associated with increased mitochondrial HK binding, some studies have identified a component of HK located in intracellular vesicles within the cardiomyocyte [48], [61], supporting older data
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Much evidence has demonstrated that
2022-03-21

Much evidence has demonstrated that the differential HER2 level between normal tissue and a tumor helps to define HER2 as an ideal diagnostic and treatment target. Thus, HER2 status can be incorporated into a clinical decision, along with other prognostic factors, such as the sildenafil mesylate re
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Flubendazole mg The Rab to Rab switch on
2022-03-21

The Rab5 to Rab7 switch on endosomes co-occurs with the release of the Rab5 GEF Rabex5 from endosomes, which prevents further Rab5 activation [5]. In addition, the Rab5 GAP is recruited to inactivate remaining Rab5 [67]. Recent data suggest that another GAP, TBC1D5, which binds the retromer complex,
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In addition during the preparation
2022-03-21

In addition, during the preparation of this manuscript, Oka et al. [7] demonstrated that LPA acts as receptor ligand for GPR35 and that LPA is more potent than KYNA in eliciting a calcium mobilization (EC50: 30nM vs. 39μM for LPA and KYNA, respectively). Other endogenous GPR35 ligands, therefore, mi
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Intranasal immunization can induce the activation of IgA sec
2022-03-21

Intranasal immunization can induce the activation of IgA-secreting plasma cell precursors that are present in NALT and induce IgA antibody-secreting cells; these cells express l-selectin (+), allowing migration to the lymphatic nodes, as well as α4β1 (+), CXCR4 (+), and CCR10 (+), which facilitate m
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Spatial working memory improved in the Balb c strain
2022-03-21

Spatial working memory improved in the Balb/c strain at a dose of VU0410120 (i.e., 30mg/kg) that disrupted spatial working memory in the Swiss Webster comparator strain. Consistent with a recent PET study in rhesus macaques suggesting a relationship between the extent of the dose-dependent occupancy
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In conclusion atorvastatin but not pravastatin impaired gluc
2022-03-21

In conclusion, atorvastatin but not pravastatin impaired glucose utilization in C2C12 cells and glucose tolerance in HFD mice, which may be partly due to the inhibition of GLUT4 translocation in muscle cells. The decrease in the cholesterol level induced by atorvastatin may partly account for the in
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Ketamine has recently been found to exert rapid and sustaine
2022-03-21

Ketamine has recently been found to exert rapid and sustained antidepressant effect. Single dose ketamine can have an efficacy of up to 1 week [20]. Furthermore, ketamine is an effective drug against refractory depression [21,22]. The antidepressant mechanism of ketamine is still unclear. Whether CO
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