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A novel series of DHODH inhibitors was
2019-08-21
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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Studies of LRRK tagged with green fluorescent protein reveal
2019-08-21
Studies of LRRK2 tagged with green fluorescent protein revealed the presence of monomeric LRRK2 in the glatiramer acetate of living cells, while LRRK2 oligomers were found in the proximity of the plasma membrane, suggesting that both oligomerization status and compartmentalization of LRRK2 defines
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In summary the reduction of one or more pro
2019-08-21
In summary, the reduction of one or more pro-inflammatory cytokines, such as TNF-α, IL-1β, IL-6, IL-8 was observed in almost all the monoterpenes studied. Increased levels of the anti-inflammatory cytokine IL-10 was shown to play a prominent function in the anti-inflammatory effect of monoterpenes,
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Currently approved anti obesity drugs for long term use such
2019-08-20
Currently approved anti-obesity drugs for long term use such as orlistat, lorcaserin and liraglutide are efficient in reduction of weight gain but are limited in usage due to their adverse effect profile and higher cost (Krentz et al., 2016; Mopuri and Islam, 2017). In BW 723C86 hydrochloride msds
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In previous works Gotor Vila et al
2019-08-20
In previous works (Gotor-Vila et al., 2017c), differences in solubility between the two carriers used during formulation were evidenced. Summarizing, maltodextrin (BA3 product) resulted in a much more soluble product since this polysaccharide is typically composed of an amount of reducing sugars bet
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br Acknowledgements The study of RING type E
2019-08-20
Acknowledgements The study of RING-type E3s continues to grow extremely rapidly. We regret that it was possible to only cite a fraction of the outstanding primary publications in this field. This work was supported by the National Institute of General Medical Sciences grants R01 GM088055 and R01
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Dipeptidyl peptidase inhibitors DPP is or gliptins
2019-08-20
Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit neuroscience peptides secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good e
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Oxidation of N hydroxyguanidine by DbH was studied
2019-08-20
Oxidation of N-hydroxyguanidine 1 by DbH was studied by HPLC and some oxidation products for 1 could be characterized. The compounds generally observed with iron-containing systems are 4-methoxyphenylurea 11 and 4-methoxyphenylcyanamide 12 (Fig. 2). Oxidation of N-(4-chlorophenyl)-N′-hydroxyguanidin
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Another mechanism underlying on the
2019-08-20
Another mechanism underlying on the toxicity of dopaminergic neurons might be related to dopamine-dependent initial oxidative stress [60]. Dopamine Kif15-IN-1 mediated by monoamine oxidase (MAO) can produce hydrogen peroxide as a by-product, and excess dopamine can undergo auto-oxidation to quinone
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DNA damage represents a persistent threat to genomic stabili
2019-08-20
DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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Numerous studies have pointed to the DGAT
2019-08-20
Numerous studies have pointed to the DGAT reaction being critical for TAG assembly and in several cases it has been shown to limit carbon flux from lipid precursors towards TAG accumulation [12]. Thus, in Brassica napus, the DGAT substrate, diacylglycerol (DAG), accumulates during periods of rapid l
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Direct coupling between DNA methyltransferase enzymes and po
2019-08-19
Direct coupling between DNA methyltransferase enzymes and posttranslational modifications on histone proteins has been observed in mammals. For example, DNMT3A recognizes unmodified H3 through an ATRX-DNMT3-DNMT3L (ADD) domain, and its activity is inhibited by methylation of H3 at K4 (Li et al., 201
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ASC was reported as a potent antiviral and
2019-08-19
ASC was reported as a potent antiviral and antifungal agent, and its derivatives could modulate a variety of physiological activities, such as anti-tumor, anti-metastatic, and anti-diabetic activities in animals. Mie Tsuruga et al. found that 4-o-methylascochlorin had immunosuppressive activity, but
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br Oxidoreductase like MEM for prodrug activation br
2019-08-19
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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Ultrasound is an acoustic wave with
2019-08-19
Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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