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br Activatable MRI probes MRI is commonly used in
2020-12-02
Activatable MRI probes MRI is commonly used in clinics around the world and has the advantages of outstanding tissue-penetration depth and extremely high spatial resolution for in vivo imaging [33]. MRI has relatively poor sensitivity and usually requires 98 9 agents to enhance the imaging contr
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Previous studies demonstrated that cPLA
2020-12-02
Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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br Materials and methods br Results br
2020-12-02
Materials and methods Results Discussion In rodent species, CYP2E1 and CYP2B have been implicated in CCl4 metabolism. In this study, we used expressed human CYP2E1 to show that this enzyme is a high-affinity catalyst responsible for low-dose CCl4 metabolism. Studies employing an inhibitory
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Due to the high attractiveness of E and E ligases
2020-12-01
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), sodium butyrate (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 200
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Expression of MGMT in human cells can be switched
2020-12-01
Expression of MGMT in human 7915 can be switched off by enzymatic methylation of a cytosine residue in the MGMT promoter sequence. In this regard, both MGMT and the mismatch repair function MLH1 belong to a subset of DNA repair genes that are subjected to epigenetic control. In consequence, about o
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Analysis of Table shows that compound b
2020-12-01
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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XAP044 G DH has gained interest because of its broad substra
2020-12-01
G3DH has gained interest because of its broad substrate specificity and site-selective oxidation properties [9,10]. The conversion product, 3-ketoglycoside, possesses potential as a starting material for the chemical industry such as in polymer and surfactants because the keto group becomes a specif
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Since anti MMP Therapy anti iNOS therapy TNF
2020-12-01
Since, anti-MMP Therapy [9], anti-iNOS therapy [10], TNF-α and IL-1β inhibitor (Diacerhein) [11] etc. are some of the disease modifying anti-osteoarthritis drugs have been used. But their action based on the evidence from the clinical trial and scientific literature suggesting the therapeutic effica
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The IP R is a ubiquitously
2020-12-01
The IP3R is a ubiquitously expressed Ca2+-release channel from the ER, activated by IP3, produced upon cellular stimulation by hormones, growth factors or neurotransmitters. Three genes are coding for the IP3R and their gene products (IP3R1, IP3R2, IP3R3) assemble in functional homo- or heterotetram
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Six substrate recognition sites SRS SRS have been
2020-12-01
Six substrate recognition sites (SRS1-SRS6) have been identified at positions 102-123, 204-209, 238-244, 301-319, 374-382 and 483-492 (Table 2, underlined residues) based on Gotoh's proposal [30]. CYP3A163 displays the similar characteristic long sequences between helices F and G presenting two addi
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Acidic substituents showed moderate biochemical
2020-12-01
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic MMP-2 Inhibitor II mg were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their b
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Introduction Eicosanoid lipid prostaglandin D PGD is the maj
2020-12-01
Introduction Eicosanoid lipid prostaglandin D2 (PGD2) is the major prostaglandin produced by activated mast tnf alpha inhibitors (Lewis and Austen, 1981). The physiological function of PGD2 is mainly mediated by two G protein-coupled receptors (GPCRs), PGD2 receptor 1 and 2 (DP1 and DP2), which sha
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17-aag Converging evidence suggests that reduced glutamate t
2020-12-01
Converging evidence suggests that reduced glutamate transmission in the LS is linked to increased anxiety-like behaviors (Radulovic et al., 1999, Henry et al., 2006, Bakshi et al., 2002, Liu et al., 2004). Therefore, attenuated CRF1 receptor-mediated excitatory transmission in the LS following ASV-t
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br Methodology The following subsections describe
2020-12-01
Methodology The following subsections describe the steps of the Systematic Literature Review (SLR) process we followed [9]. Results In our review of the literature, we used the definitions provided by the IEEE Standard Computer Dictionary [15] to categorize the claims about the effectiveness
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Indeed some studies that examined the morphine response have
2020-12-01
Indeed, some studies that examined the morphine response have reported that the (C) allele of rs4818 was associated with a low dose administered compared to that given for individuals with the (G) allele (Rakvag et al., 2008). In a publication about Tunisian patients with cancer by Chatti et al. (2
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