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br Conclusions In the present study decreased AChE and
2020-11-12
Conclusions In the present study, decreased AChE and increased BuChE and BeChE activities were observed in greenhouse workers relative to control subjects; however, these changes cannot be related to OP exposure but likely to pesticide-induced oxidative stress or a mild inflammatory state. The in
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In contrast to AChE BuChE Table
2020-11-12
In contrast to AChE, BuChE (Table 2) exhibited a measurable time-dependent inactivation only with ponceau stain 2 among the four acetophenones in this study. Values of Ki obtained from steady-state inhibition of BuChE by all four acetophenones were, as noted in the Results, 10- to 200-fold greater
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Although BPA has been proven
2020-11-12
Although BPA has been proven to cause many health issues such as obesity and neurological toxicity (Rubin, 2011), the effects and mechanisms of BPA on the human tumorigenesis and cancer development are still not well illustrated. In the present study, we found that 10 to 10M BPA significantly promot
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ROS generation is crucial for NETs
2020-11-12
ROS generation is crucial for NETs release upon both physiological or pathogenic stimuli [16,30]. In our study, we further verified this conclusion by demonstrating that SRA stimulation by Poly I enhanced intracellular ROS levels while scavenging of ROS by anti-oxidant agents effectively abolished t
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br Materials and Methods br
2020-11-12
Materials and Methods Results Discussion The spatial properties of receptor-ligand interactions can influence receptor activation and signal propagation, but studying this phenomenon requires the development of systems capable of recapitulating complex biophysical traits. In this study, we
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EP receptors belong to the family
2020-11-12
EP1–4 receptors belong to the family of G protein-coupled receptor (GPCR). Trafficking events such as externalization, internalization, recycling and degradation dynamically regulate GPCR cell surface density. A fast-rate of internalization and degradation reduces GPCR surface density to desensitize
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Methods br Results First we compared A plaque
2020-11-12
Methods Results First, we compared Aβ plaque number, Aβ concentration, and neurobehavior functions between naive APP/PS1 and APP/PS1xEP1−/− mice. Significantly lower Aβ burden in APP/PS1xEP1−/− mice was evidenced by fewer plaques in the hippocampal area and a lower concentration of soluble Aβ42
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Two GPCR subtypes of interest in the myocardium
2020-11-12
Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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As retinol was not inducing any of
2020-11-12
As retinol was not inducing any of the isoforms of CYP450 responsible for the bioactivation of paracetamol, we decided to examine retinol's effect on renal and hepatic glutathione to determine whether retinol was potentiating hepatotoxicity through a mechanism of glutathione depletion. Studies, util
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KN-93 Our research has demonstrated that the absolute bioava
2020-11-12
Our research has demonstrated that the absolute bioavailability of oxymatrine, having a similar structure with OSC, was only 6.79±2.52%. About 50% of OSC was converted to its active metabolite SC in vivo; hence, the absolute bioavailability of OSC was speculated to be poor as well [24]. Understandin
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The UPP broadly involves proteolysis in biochemical processe
2020-11-12
The UPP broadly involves proteolysis in biochemical processes and is a potential target for cancer therapy. The UPP degrades unfolding or damaged proteins by an ATP-dependent mechanism (Ciechanover, Elias, Heller, Ferber, & Hershko, 1980). It also plays an important role in semagacestat regulation,
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Based on the above background
2020-11-12
Based on the above background, gliptins may exert natriuretic and diuretic effects as well [[112], [119]]. In accordance with this, Girardi and co-workers have demonstrated a physical interplay between DPP-4 and the NHE3 exchanger in the brush-border epithelium of the proximal renal tubule, suggesti
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QSAR based on the D structures
2020-11-11
QSAR based on the 3D structures of ligands plays an important role in the ligand-based drug discovery and design [12]. Comparative molecular field analysis, CoMFA [11], and comparative molecular similarity index analysis, CoMSIA [12] are among the most popular QSAR models. They focus on changes in 3
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Besides by substrate and product KSTDs may also be inhibited
2020-11-11
Besides by substrate and product, Δ1-KSTDs may also be inhibited by other steroids. N. simplex ATCC 6946 Δ1-KSTD was strongly inhibited non-competitively by dicortinone (60), a steroidal dimer, and by bis-1-dehydrodicortinone, with values of 0.7 and 0.75 μM, respectively. This enzyme was also inhib
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Widely expressed mammalian adhesion receptors for fibrillar
2020-11-11
Widely expressed mammalian adhesion receptors for fibrillar collagens include the α2β1- and α11β1-integrins and the discoidin domain receptors (DDRs), DDR1 and DDR2 (Leitinger, 2011). Integrins and DDRs bind distinct and separate motifs in native fibrillar collagen (Curat et al., 2001, Vogel et al.,
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