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Several highly selective COX inhibitors coxibs have been rep
2020-09-19
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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Magnified regions of the upregulated proteins
2020-09-19
Magnified regions of the upregulated proteins identified by MALDI-TOF are shown in Fig. 2. The identified proteins were phosphoglycerate kinase, fructose-bisphosphate aldolase class II, alcohol dehydrogenase, phosphoglyceromutase, 6-phosphogluconolactonase, malate dehydrogenase, alkyl hydroperoxide
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br Selection of ions for
2020-09-19
Selection of ions for GaN Systems sample test Sample construction analyses has been provided to analyze the beam penetration of several ions of the cocktail in the component. An X-ray and optical view of GaN System devices parts is presented at Fig. 5, Fig. 6 respectively. The drain and source el
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Introduction Safety critical systems are defined
2020-09-19
Introduction Safety-critical systems are defined as those systems where failure could result in the loss of life or injury to people, damage to equipment or to the environment [9]. Safety standards, e.g., [41], [17], [18], [6], [38], expect appropriate safety analysis tasks to be integrated within
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br Functional significance Defects of the lysyl hydroxylases
2020-09-19
Functional significance Defects of the lysyl hydroxylases LH1, LH2, and LH3 impair collagen secretion and stability in the extracellular matrix, and cause rare connective tissue disorders such as Ehlers-Danlos type-VI [27], Bruck syndrome [28], and skeletal dysplasia [29], respectively. Elucidati
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br Conclusions In a former study we compared the modulating
2020-09-19
Conclusions In a former study we compared the modulating potential of halogenated 1H-benzimidazole derivatives towards CK2 catalytic subunits. Now we were interested if similar differences are also obtained using completely different substances. Some of these natural occurring compounds were alre
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Next to organophosphates carbamates and metals
2020-09-19
Next to organophosphates, carbamates and metals, cholinesterase activity can also be affected by other pesticides, such as newer generation neonicotinoid insecticides (NN). NNs do not inhibit AChE activity via the organophosphate-sensitive binding site of the enzyme, but rather, by acting as a struc
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transketolase Several CHK inhibitors have been reported in t
2020-09-19
Several CHK-1 inhibitors have been reported in the literature. Of these, UCN-01 (7-hydroxystaurosporine) is a potent inhibitor of CHK-1 (=5.6nM), , and has modest selectivity among other kinases. UCN-01 is currently in clinical trials. Other CHK-1 inhibitors reported in the literature include indaz
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br Discussion Variable estradiol effects on cell proliferati
2020-09-19
Discussion Variable estradiol effects on cell proliferation have been reported according to animal species, tissues, and type of estrogen receptor [16,21,22,[29], [30], [31]]. In the kidney, 17βE was found to increase [3H]-thymidine incorporation in primary rabbit kidney proximal tubule sonidegib
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In this work we fabricated
2020-09-19
In this work, we fabricated a kind of multifunctional nanoparticles, based on HAuNS coated by chitosan-stearic Diclofenac copolymer (CSO-SA), which was employed frequently to form micelles for hydrophobic drug delivery in our previous work [21], [22]. The nanoparticles can encapsulate DiR efficient
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Pasireotide Our results indirectly support the combination
2020-09-19
Our results indirectly support the combination of resveratrol and hesperatin treatment for PDN, as this induces GLO1 activity in patients (Xue et al., 2016), as well as metformin, an FDA-approved anti-diabetic treatment, which acts as an MG scavenger to reduce MG levels in type 2 diabetic patients (
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br Results br Discussion The ubiquitin
2020-09-18
Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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DUBs are involved in cell cycle regulation and DNA
2020-09-18
DUBs are involved in muscarinic receptor antagonists regulation and DNA damage pathways and since, in cancer and different stress conditions all the proteins which regulate cell cycle and DNA damage/repair are either up/down regulated (Singh et al., 2013, Singh et al., 2011, Kumar and de Massy, 201
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There is literature precedence for the metabolic
2020-09-18
There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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The results described in the
2020-09-18
The results described in the present study confirm key restrictions on reaction conditions which must considered to maximize reactor productivity. Increased viscosity should be avoided for the amination of ketones by L-AmDH, as a 4-fold increase in viscosity can lower the reaction rate by as much as
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