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br Acknowledgements br Introduction L Rhamnosidases EC are
2020-01-25
Acknowledgements Introduction α-L-Rhamnosidases (EC 3.2.1.40) are glycosyl hydrolases (GHs) that cleave terminal α-l-rhamnose from a large number of natural products [1]. The action of α-L-rhamnosidases (α-RHAs) has been reported, among others, on different complex substrates such as heteropol
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br Conflicts of interest br Acknowledgements This work was
2020-01-25
Conflicts of interest Acknowledgements This work was supported, in part or in whole, by the grants from the National Natural Science Foundation of China (11802056, 11772088), the China Postdoctoral Science Foundation (2018M640904), and the Fundamental Research Funds for the Central Universitie
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Covalent inhibitors are well suited for targeting the
2020-01-25
Covalent inhibitors are well suited for targeting the E1 Z-IETD-FMK of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in circ
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It is reported that sympathetic
2020-01-25
It is reported that sympathetic nerve activity is increased in the SHR strain compared with that in the WKY strain (Judy and Farrell, 1979, Lundin et al., 1984, Sugimura et al., 2008) and NA content is increased in the CB of the New Zealand strain of hypertensive rat compared with that in normotensi
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These data raised from human tissues suggested a potential
2020-01-25
These data raised from human tissues suggested a potential link between TGF-β1 signaling and linear invadosome machinery that may explain TGF-β involvement in HCC progression and invasion. Using HCC cultured cells, we confirmed that TGF-β1 stimulation increases the production and secretion of collag
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While previously reported optimizations on compound focused
2020-01-23
While previously reported optimizations on Flutamide focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore new che
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Grapiprant is a selective antagonist
2020-01-23
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Future advances in the in vivo
2020-01-23
Future advances in the in vivo molecular imaging of enzyme activity will greatly benefit from the progress towards the quantitative detection of enzymes. Quantitative imaging requires knowledge of both the location and concentration of a specific enzyme, which is dependent on the simultaneous measur
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br Experimental Procedures br Author
2020-01-23
Experimental Procedures Author Contributions Acknowledgments Introduction The intestinal mucosal barrier surface is constantly exposed to food antigens, beneficial microbes, pathogens, and a multitude of other environmental stimuli (Turner, 2009). Innate lymphoid 5959 receptor (ILCs) ar
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br Materials and methods br Results
2020-01-23
Materials and methods Results Discussion Innate immunity plays an essential role in the control and elimination of bacterial infection through production of inflammatory cytokines (Liu et al., 2015). Production of inflammatory cytokines requires the recognition of bacterial pathogen-associa
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The aim of this paper is to
2020-01-22
The aim of this paper is to study the long-term socioeconomic impacts of local heat entrepreneurship from 2000 to 2016. The analysis focuses on impacts of the biomass-based district heat production on employment and income in a small peripheral community, called Eno, located in North Karelia, Finlan
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ApoE is secreted from astrocytes glia into the
2020-01-22
ApoE is secreted from astrocytes/glia into the interstitial fluid and is important for metabolizing Aβ because of its propensity for binding Aβ as a cholesterol and phospholipid acceptor in reverse cholesterol transport [8]. Aβ oligomers show a direct toxicity to neurons, and ApoE inhibits oligomer
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Cyclosporine NEORAL Oral Solution Novartis
2020-01-22
Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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br Results br Discussion PKR is
2020-01-22
Results Discussion PKR is activated by viral dsRNA and exerts its antiviral effect through phosphorylation of eIF2a. Because eIF2a phosphorylation leads to attenuation of protein synthesis, many viruses have evolved mechanisms to block or suppress PKR activation. Some viruses use alternative t
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br RING type E s and their substrates There is
2020-01-22
RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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