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In agreement with the study on
2020-04-29
In agreement with the study on porcine microsomes (Ekstrand et al., 2015), our results indicated a somewhat higher degree of inhibition of CYP2E1 activity in the male pools compared to females. Nevertheless, the degree of this STA4783 inhibition did not reach 50%, indicating that quercetin is unlik
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Since cognitive disturbances are core
2020-04-29
Since cognitive disturbances are core features of PTSD [3,4], and in some studies COMT Val158/108Met was associated with cognition [10] and hippocampal volume [12], the hypothesis was that carriers of the Met allele will show better cognitive performance compared to Val/Val carriers in PTSD. The aim
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Based on the similar activities
2020-04-28
Based on the similar activities of Rad6p and Cdc34p (i.e., both are E2 ub-conjugating enzymes) on ubiquitinylation of p33 replication protein, we propose that Rad6p and the plant Ubc2p mono- and bi-ubiquitinate the viral replication proteins in order to facilitate the recruitment of the cellular ESC
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br The DDR kinase domain The DDR
2020-04-28
The DDR1 kinase domain The DDR1 intracellular kinase domain shares the typical structure of other kinase domains (Fig. 1). However, how DDR1 kinase is activated upon collagen binding is poorly understood. It is thought that the process is fundamentally different from the accepted paradigm of liga
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Cys LT have been shown to be
2020-04-28
Cys-LT have been shown to be critical for stimulation of monocytes to produce various proinflammatory factors [32,67]. Fig. 3 shows results obtained with human peripheral monocyte-derived macrophages differentiated for 6 days with 20 ng/ml macrophage colony-stimulating factor (M-CSF) and challenged
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CPG a metalloenzyme derived from sp was
2020-04-28
CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic colony stimulating factor 1 receptor prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond
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Furthermore in silico physicochemical characters
2020-04-28
Furthermore, in silico physicochemical characters and pharmacokinetic parameters for the synthesized compounds were predicted using dedicated computer software [34], [35], [36] to ensure successful in vivo therapeutic activity. Practical logP testing was performed and compared to the theoretical val
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DGK is classified into the type II
2020-04-27
DGKη is classified into the type II DGK subfamily [12], [13], [14], [15]. As described above, DGKη has the splice variants η1 and η2 [10]. DGKs η1 and η2 possess in common a pleckstrin homology domain at the N-terminus and a catalytic domain that is divided into two subdomains (catalytic subdomain-a
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In Senegal malaria remains a
2020-04-27
In Senegal, malaria remains a formidable public health issue, causing significant morbidity and mortality in infants and pregnant women (WHO Malaria Report, 2012). In the absence of an effective vaccine, the National Malaria Control Program has followed WHO recommendations for IPTp-SP since 2003. Th
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br Materials and methods br
2020-04-27
Materials and methods Results Discussion The studies reported here provide a more direct link between conformations of the glycine-rich region of DAPK and enzyme activity. As schematically illustrated in Fig. 3, the various conformations of DAPK with bound substrate or product can be consid
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Kif15-IN-1 br Materials and methods br Results br Discussion
2020-04-27
Materials and methods Results Discussion Chronic inflammation is central to COPD and plays a critical role in the disease pathogenesis and progression. Among the various inflammatory cells, neutrophils are the key players in COPD pathogenesis. Their numbers are raised in airspaces and lung
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The pseudo DUBs KIAA and Abraxas are required for
2020-04-27
The pseudo DUBs KIAA0157 and Abraxas are required for the catalytic function of BRCC36. Comparison of the BRCC36–KIAA0157 heterodimer structure with an inactive BRCC36 homodimer structure provides a model for understanding how this functional interplay is achieved. As shown in schematic form in Figu
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(R,S)-Anatabine receptor Another pathway that requires prope
2020-04-27
Another pathway that requires proper DUB recruitment is the DNA damage response (DDR). After ultraviolet (UV)-induced DNA damage, monoubiquitylated proliferating cell nuclear antigen (PCNA) mediates signaling that leads to repair. The DUB complex USP1/USP1-associated factor 1 (UAF1) deubiquitylates
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Fisetin tetrahydroxyflavone is a flavonol present in several
2020-04-27
Fisetin (3,3′,4′,7-tetrahydroxyflavone) is a flavonol present in several fruits and vegetables such as grape, persimmon, strawberry, apple, and onion at concentrations rangeing from 2 to 160 μg/g. Fisetin is a well–known bioflavonoid with remarkable biological effects including chemopreventive/chemo
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Compounds that interact with MDR can do so by
2020-04-27
Compounds that interact with MDR1 can do so by different mechanisms. Verapamil is known to modulate drug resistance by acting as a competitive MDR1 substrate [36]. Interestingly, NU7441 has similar growth inhibitory activity in the sensitive and resistant CA074 and there was no observed reduction i
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