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The primary physiological role of the HO system is
2022-08-12
The primary physiological role of the HO system is the protection of dantrolene sodium mg from oxidative stress. These cytoprotective effects are attributable both to the degradation of the pro-oxidant heme and to the positive contribution of the metabolites produced during this degradation, namely
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The HCV NS A protease consists of two subunits NS
2022-08-12
The HCV NS3/4A protease consists of two subunits, NS3 and NS4A. NS3 comprises an N-terminal serine protease domain and a C-terminal RNA helicase domain [12]. NS4A acts as a cofactor, which ties the holoenzyme complex to an intracellular membrane compartment. The presence of the central region of NS4
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GSTP catalyzed reduction of Prdx enhances its peroxidase act
2022-08-12
GSTP1-1 catalyzed reduction of Prdx6 enhances its peroxidase activity. Using standard NADPH/GR/GSH-coupled assays we used cell lysates from the transiently transfected 8-Azido-ATP to measure the influence of GSTP1 allelic variation on peroxidase activity. Specificity for detection of Prdx6 activity
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Despite the rapid development of synthetic ligands the endog
2022-08-12
Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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With this goal in mind we proceeded to explore
2022-08-12
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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In previous work we showed that benzophenanthridines do
2022-08-12
In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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An alternative to the chemoenzymatic preparation of
2022-08-12
An alternative to the chemoenzymatic preparation of glycoproteins is the production through total chemical synthesis or semi-synthesis [2,3,]. Many successful glycoprotein syntheses are based on native chemical ligation (NCL) [11], a reaction where unprotected peptides and glycopeptides of any lengt
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br Evasion strategies for enhanced therapeutic outcomes In o
2022-08-12
Evasion strategies for enhanced therapeutic outcomes In order to increase AED penetration into the CNS, several strategies have been developed over the years to overcome the activity of efflux transporters, by inhibiting their function or by regulating their expression. Due to the high relevance
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After brain injury adenosine levels rapidly
2022-08-12
After brain injury, adenosine levels rapidly increase in the brain [9,10]. As shown in our previous studies, the increased adenosine concentration acts on adenosine A2A receptors (A2ARs), increasing post-traumatic glutamate levels in the brain and exacerbating the severity of injuries [11,12]. Accor
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Bergmann glia cells BGCs are the most abundant glia cells
2022-08-12
Bergmann glia ll-37 (BGCs) are the most abundant glia cells in the cerebellum, comprising more than 90% of the cerebellar glia. These cells span the entire cerebellar molecular layer and encapsulate neuronal somata, dendrites and axons. BGC are involved in neurotransmitter uptake, K+ homeostasis an
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Having shown that some of substitutions Cl CF at the
2022-08-12
Having shown that some of substitutions (Cl, CF) at the 2-position of the thiophene improved rat microsomal stability, and polar groups at the 4-position of the aryl ring had a beneficial effect on stability in both human and rat microsomes, we combined these features in a new set of analogs. Methyl
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FFAR is highly expressed not only
2022-08-12
FFAR1 is highly expressed not only in β cells but also in α aphidicolin (Segerstolpe et al., 2016), which gives the interesting perspective that 20-HETE may function both as an autocrine and as a paracrine regulator of islet cell function (Figure 1A), i.e., acting in symphony with the many other in
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br Glucose metabolism and diet Glucokinase is essential
2022-08-12
Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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br Results br Discussion ER and GR
2022-08-12
Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in
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Previous attempts to minimize the contribution
2022-08-12
Previous attempts to minimize the contribution of the compensatory changes due to chronic loss of Gcgr, have used temporally-controlled reduction of glucagon levels by alpha-cell ablation, glucagon immunoneutralization, and the use of small molecule or antibody glucagon receptor antagonists [10], [3
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