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In conclusion we designed novel E inhibitors based on
2021-06-09
In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and , we f
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Enolase as a plasminogen receptor and activator localized on
2021-06-09
Enolase, as a plasminogen receptor and activator localized on the surface of several helminths, can interact with the host fibrinolytic system (Yang et al., 2010, Du et al., 2009, de la Torre-Escudero et al., 2010). The enzyme is also one of excretory/secretory (ES) products in some helminths, such
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The purpose of this study is to investigate KDM B
2021-06-09
The purpose of this study is to investigate KDM1B expression and its functional significance in PC. We used lentivirus-mediated shRNA to down-regulate KDM1B expression in PC cell lines in vitro and detected the changes of cell proliferation and apoptosis. These studies provided a novel insight into
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What are the molecular signals that guide Tfh cells
2021-06-09
What are the molecular signals that guide Tfh cells as they navigate around the lymph node in the course of the immune response? It was recently reported that Tfh cells inside GCs have high expression of SIPR2, which acts to repel them from the S1P-rich lymph in the SCS and promote their retention i
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Introduction Cognitive impairment is a core stable
2021-06-08
Introduction Cognitive impairment is a core, stable feature of schizophrenia that limits patient functioning and well-being (Keefe and Harvey, 2012) and associates with poor functional outcome (Fervaha et al., 2014, Kontaxaki et al., 2014). Studies also indicate that cognitive deficits occur prior
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A An optimized BEI SEIscore
2021-06-08
(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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The presence of H PPases in parasitic protists raises
2021-06-08
The presence of H+-PPases in parasitic protists raises the question of the physiological role of these proteins. So far, they had been extensively characterized mainly in higher plants, and some prokaryotes [1], [2], [3], [4], [5], [6], [7], [16], [20]. A common feature to all these organisms is tha
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There are numerous resources clinicians may use
2021-06-08
There are numerous resources clinicians may use to gather information on the strength of evidence related to pharmacogenetic-based dosing and treatment decisions, as well as specific dosing guidelines, some of which are summarized in this review. These include resources from CPIC, which provides pe
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br Conclusions The present study
2021-06-08
Conclusions The present study demonstrated that CuE possesses strong hepatotoxicity. CuE is not only a mechanism-based inhibitor of human CYP3A4, but also inhibits P-gp activity in vitro. In whole animal studies, CuE induces CYP3A and P-gp after a long-term treatment but inhibits the activities o
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The COMT gene is involved in
2021-06-08
The COMT gene is involved in numerous psychological and physiologic processes, including modulation of pain. Polymorphisms in this gene have also been associated with many painful conditions, including pain sensitivity in children. Bivariate analysis demonstrated that individuals with heterozygous C
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Recently several Pt IV complexes
2021-06-08
Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with
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br Conclusions In the present study decreased AChE and incre
2021-06-08
Conclusions In the present study, decreased AChE and increased BuChE and BeChE activities were observed in greenhouse workers relative to control subjects; however, these changes cannot be related to OP exposure but likely to pesticide-induced oxidative stress or a mild inflammatory state. The in
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NT157 The cholinergic system has been shown to play
2021-06-08
The cholinergic system has been shown to play a role in regulation of the inflammatory response [13] as well as in the influence of the metabolism of PCa cells [14]. The reduced activity of cholinesterase (ChoE) and the consequent increased amount of NT157 has been shown to lead to a cholinergic ov
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It was reported that IVM modulates
2021-06-08
It was reported that IVM modulates various ion channels, such as type-A GABACls, α7 acetylcholine-gated cation channels, P2X4 ATP-gated cation channels, and glycine-gated chloride Famprofazone in vertebrates (Adelsberger et al., 2000, Khakh et al., 1999, Krause et al., 1998, Krůšek and Zemková, 199
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Udenafil also has shown the
2021-06-08
Udenafil also has shown the ability to significantly inhibit the decrease of vascular endothelial cell function and inhibit the decrease in endothelial cell and smooth muscle contents, thus preventing their fibrosis within the penile corpus cavernosum in diabetic or hyperlipidemic animal models when
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