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With the narrow SAR of
2020-09-21
With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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br Conflicts of interest br Acknowledgments This
2020-09-19
Conflicts of interest Acknowledgments This research was supported by the Basic Science Research Program through the National Research Foundation of Korea funded by the Ministry of Science, ICT and Future Planning (NRF-2015R1A2A2A01004593). Introduction Resistance to Inhibitors of Cholinest
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Adding MPA or NETA we found
2020-09-19
Adding MPA or NETA we found no impact on the estradiol-induced downregulation of serum-stimulated endothelin synthesis in vitro [40]. Progesterone was also able to inhibit the angiotensin II-induced increase in endothelin production [41]. Several clinical studies on the effect of oral or transdermal
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To our knowledge immunohistochemical analysis
2020-09-19
To our knowledge, immunohistochemical analysis for proGRP was done in 5 cases [9], [10], [17], [18]. Takagi-Takahashi et al. reported that the tumor Kif15-IN-1 australia were positive for proGRP in one case [9]. Yamaguchi et al. also showed that tumor cells in two patients of ES/PNET with elevated
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In the present study we investigated the
2020-09-19
In the present study, we investigated the role of EP1R after ICH and its mechanism of action. We hypothesized that EP1R activation aggravates ICH injury but that its blockade reduces injury through the Src kinases and the MMP-9 signaling pathway. To test this hypothesis, we examined the effects of s
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Glycolysis is important to maintain the
2020-09-19
Glycolysis is important to maintain the vital functions of T. gondi. Extracellular T. gondii shift its Epibrassinolide synthesis metabolism towards glycolysis, based on the observation that a relocation of glycolytic enzymes from the cytosol to the pellicle occurs at the time when tachyzoites egres
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br Materials and methods br Results br Discussion In
2020-09-18
Materials and methods Results Discussion In this study, we employed a liquid chromatography mass spectrometry (LC–MS)-based metabolomic approach to profile GEF metabolism and bioactivation in human and mouse liver microsomes. Metabolomic approaches rendered us readily screen out the GEF-rel
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br Results and discussion In the present study we
2020-09-18
Results and discussion In the present study, we used a set of compounds (Fig. 2) consisting of ATP (a), dATP (b), an ATP analog containing β,γ-nonhydrolyzable hypophosphate P-P bond (c), and three pairs of P-diastereoisomers of α-thio-ATP analogs (d,e,f) containing a sulfur A 77-01 synthesis ins
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br Development of a liquid chromatography
2020-09-18
Development of a liquid chromatography-mass spectrometry method to improve detection of PA species detection Liquid chromatography-mass spectrometry (LC-MS) is a powerful tool to detect different molecular species of phospholipids in AZ20 (Houjou et al., 2005, Pulfer and Murphy, 2003). However,
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The presence of H PPases in parasitic protists
2020-09-18
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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br Acknowledgements br Introduction Chemokines are a superfa
2020-09-18
Acknowledgements Introduction Chemokines are a superfamily of chemotactic cytokines that play important roles in regulating cell migration and activation under inflammatory conditions (Nomiyama et al., 2008; Peatman and Liu, 2007; Zlotnik and Yoshie, 2000), such as angiogenesis (Arenberg et al
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Various domains of the HSA molecule
2020-09-17
Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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chemokine receptor antagonist Although the presence of at le
2020-09-17
Although the presence of at least one triple helix domain is typically the collagen signature, collagens are modular proteins composed of a succession of collagenous (COL) and non-collagenous domains (NC) that are both involved in collagen functions and in receptor binding. COL domains are linked by
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Conventional assays rely on a
2020-09-17
Conventional assays rely on a comparable transformation of the target analytes and the structurally similar (but not identical) proxy substrates and are commonly used to measure individual enzyme activities in (pre-treated) intact sludge flocs (Burgess and Pletschke, 2008a, Gessesse et al., 2003, Yu
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On the opposite side sPLA
2020-09-17
On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer hesperetin and promotes their survival during nutrient stress. It acts through the products of its enzyma
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