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In the present work we have investigated the reactivity of
2019-10-14
In the present work, we have investigated the reactivity of N-aryl-N′-hydroxyguanidines 1a–d (see Scheme 1 for structures) with the water-soluble Cu(II) complex 8. Using EPR and UV–Visible spectroscopy, we have shown that the studied N-aryl-N′-hydroxyguanidines 1a–d can bind and transfer electrons t
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DMXAA The biological significance of DNA ligases is attribut
2019-10-14
The biological significance of DNA ligases is attributed to their function in DNA replication, recombination and/or DNA repair [1], [2]. In vertebrates, three different DNA ligases I, III and IV are recognized. DNA ligase I is essential for the Okazaki fragments’ ligation during lagging-strand DNA s
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Compound was synthesized by the directed
2019-10-14
Compound () was synthesized by the directed -metallation procedure (DOM) at the stage of the amide using butyl lithium and dry ice as CO source for the introduction of the carboxylic group. Thiophene amides were prepared from commercial 3-thiophenecarboxylic Nintedanib by conversion into the acid
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Compounds and were synthesized according to
2019-10-14
Compounds and () were synthesized according to . Reductive amination of ethyl acetoacetate with aniline afforded ester . Saponification of followed by intramolecular Friedel–Crafts acylation afforded ketone . Amide formation with benzoyl chloride followed by a reductive amination yielded compound .
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br Conclusions br Acknowledgment br Introduction
2019-10-12
Conclusions Acknowledgment Introduction The role of cholesterol metabolism during multiple sclerosis (MS) is debated and the underlying physiopathology largely unknown. Dyslipidaemia is associated with worsening inflammatory activity and MS disease progression [1], [2], [3]. In the mouse mo
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capivasertib mass Third DGK protein stabilization by myristi
2019-10-12
Third, DGKδ2 protein stabilization by myristic capivasertib mass is cell line specific. Myristic acid had no obvious effects on DGKδ protein stability in the liver cell line HepG2, pancreas cell line MIA-PaCa-2 and neuronal cell line Neuro-2a cells (Fig. 5). Although myristic acid moderately increa
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Western blotting Western blotting was
2019-10-12
Western blotting: Western blotting was performed following the standard protocol as previously described [16]. All the images were collected using the Odyssey Fc imaging system (Li-COR Biosciences). In vitro kinase assays were performed on ∼1 μg of purified CDK5/p35 complex in 30 μL of kinase buffe
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br Functional significance Defects of the lysyl hydroxylases
2019-10-12
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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In addition to PDCA we also
2019-10-12
In addition to 2,4-PDCA, we also tested other broad-spectrum 2OG oxygenase inhibitors as vCPH inhibitors. N-Oxalyl glycine (NOG, IC50 = 21.2 ± 2.1 µM), a close 2OG isostere, and IOX1 (IC50 = 47.2 ± 2.7 µM), which is a relatively broad-spectrum JmjC demethylase inhibitor, were not as potent in inhibi
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CP-809101 hydrochloride clinical Overall we found that all h
2019-10-12
Overall, we found that all hormone treatment groups were able to learn spatial working and reference memory tasks, as shown by their performance across days on the WRAM (days 2–12, collapsed across the 4 trials) and the MWM (days 1–5, collapsed across the 4 trials). During the acquisition phase of t
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Introduction Enzymes have higher selectivity
2019-10-12
Introduction Enzymes have higher selectivity, specificity and efficiency than chemical catalysts. Due to their properties and their green chemistry, biocatalysts are widely used in food, textile and pharmaceutical industry [1], [2]. A high efficient biocatalyst for industrial applications must be s
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br Introduction Detection of driver mutations in patients wi
2019-10-12
Introduction Detection of driver mutations in patients with advanced non-small cell lung cancer (NSCLC) is critical because they receive great benefit from kinase inhibitors [[1], [2], [3], [4]]. However, it is often difficult to obtain tumor tissue in advanced NSCLC patients. Cell-free DNA (cfDN
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COH inhibited global SUMOylation in cells
2019-10-12
COH000 inhibited global SUMOylation in SB273005 and blocked the E1 catalyzed attachment of SUMO to the corresponding conjugating enzyme Ubc9, but not the attachment of ubiquitin or NEDD8 to their respective E2s, confirming inhibition and specificity in cellulo. Consistent with previous studies inac
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br Materials and methods br Results
2019-10-12
Materials and methods Results Discussion In this paper, we have demonstrated application of the glmS ribozyme reverse genetic tool for chemogenomic profiling in Plasmodium spp. This tool can provide robust attenuation of expression for different target genes, across different strains varyin
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Both progesterone and the calcium ionophore A rely on
2019-10-11
Both progesterone and the calcium ionophore A23187 rely on the synthesis of cAMP by sAC to elicit exocytosis in human sperm (Fig. 2E-H and [8], [60]). We had reported earlier that digestion of endogenous cAMP with recombinant cAMP-specific phosphodiesterase 4D [9] or inhibition of its synthesis with
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