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During the past decade it became increasingly
2019-10-09

During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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The total reduced glutathione content was determined in both
2019-10-09

The total reduced glutathione content was determined in both prostaglandin receptor to examine whether retinol was decreasing glutathione concentrations and thus decreasing the conjugation of NAPQI. Total hepatic (3.9±0.3 vs 4.9±1.0 μmol/g, retinol vs untreated, respectively) and renal (0.4±0.1 vs 0
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The development of C S mutation has
2019-10-09

The development of C797S mutation has been reported in vivo in a small cohort (15 subjects) of EGFR T790M positive patients progressing after Osimertinib: this tertiary mutation was found, using a droplet digital PCR (ddPCR) assay, in 40% of patients after AR to this agent, while 33% of the cases ex
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We found that the postnatal absence of norepinephrine
2019-10-09

We found that the postnatal absence of norepinephrine yields differing effects depending on noradrenergic receptor type and sr9011 mass region. The density of α1-AR, indicated by [3H]prazosin binding was similar between Dbh+/− and Dbh−/− mice except for a significant increase in hippocampus in Dbh−
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Then we explored the MCLEIA methodology parameters including
2019-10-09

Then, we explored the MCLEIA methodology parameters including precision, accuracy and specificity. In the 0.5–128 ng/mL, the standard curve equation was = 0.5014 + 1.769 ( was log, was RLU/RLU with a correlation coefficient of 0.9907) (). On the one hand, same sample (0.5, 4.0, 32.0 ng/mL) detecte
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cAMP mediated signaling pathways are
2019-10-08

cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, doxercalciferol kinase of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased
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Several studies have shown that independently of body weight
2019-10-08

Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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Several studies highlighted the potential of EOCs to promote
2019-10-08

Several studies highlighted the potential of EOCs to promote adverse effects on aquatic organisms. It was reported the toxicity of BPA to invertebrates and fish, and the effect of lipophilicity on toxicity was analyzed (Mathieu-Denoncourt et al., 2016). There was reported the effects of PPCPs on aqu
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br Substrate Specificity Discrimination and
2019-10-08

Substrate Specificity, Discrimination, and Binding Energy In 1 25-dihydroxyvitamin d3 to catalytic efficiency, which can be gauged in reference to an absolute scale of ‘catalytic perfection’ 10, 11, specificity is a relative concept because it requires comparison between given alternative substra
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Introduction Pain is frequently the first clinical
2019-10-08

Introduction Pain is frequently the first clinical symptom of head and neck carcinoma. Indeed, pain is the initial reason leading ∼70% of cancer patients to seek professional assistance (Lam & Schmidt, 2011; Rettig & D’Souza, 2015; Schmidt, 2014). Clinically, cancer-induced facial pain can be evoke
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br Localization of D receptors in striatum One
2019-10-08

Localization of D2 receptors in striatum One characteristic of D2Rs that has complicated their study is their expression in multiple neuronal populations within striatum, both pre- and postsynaptically (Beaulieu and Gainetdinov, 2011). In addition to spiny projection neurons (SPNs), which are the
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CAA is a carcinogenic metabolite of vinyl chloride forming
2019-10-08

CAA is a carcinogenic metabolite of vinyl chloride, forming several different DNA adducts including the cyclic Ac-DEVD-AFC adducts 3,N4-ethenocytosine (εC), 1,N6-ethenoadenine (εA), N2,3-ethenoguanine (εG), and 1,N2-ethenoguanine (1,N2-εG), with the A and C cyclic adducts the most predominant, and a
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br Conclusion AS SP the first line treatment still remains
2019-10-08

Conclusion AS+SP, the first-line treatment, still remains highly effective in Pakistan following its introduction in 2007. However, molecular data indicate that SP resistance is being established in Pakistan, although mutations that confer a high risk of SP treatment failure are rare or non-exist
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The authentic PPase was purified from B
2019-10-08

The authentic PPase was purified from B. subtilis as described previously [21], whereas the recombinant enzyme was purified to homogeneity from E. coli by a simplified procedure including only phenyl-Sepharose CL-4B column chromatography and DEAE-HPLC [21]. About 26 mg of pure enzyme was obtained fr
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With a favorable spectrum of CRTh
2019-10-08

With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
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