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Consistent with previous simulations on the DFG Asp out in
2019-07-24
Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event
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Our recent discovery M P H R A S of
2019-07-24
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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The availabilities of serotonin and dopamine are
2019-07-24
The availabilities of serotonin and dopamine are modulated by the serotonin transporter and catechol-O-methyltransferase enzyme. The serotonin transporter (5-HTT) is a key protein that reuptakes serotonin from the synaptic cleft back into synaptic boutons (Coleman et al., 2016; Talvenheimo et al., 1
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br Material and methods br
2019-07-23
Material and methods Results and discussion Conclusions Acknowledgements S. De thanks DST, New Delhi for generous grant of the SERC Fast Track Scheme No. SR/FT/CS-057/2008. R. Kundu thanks the University of Kalyani for financial assistance. We are grateful to Prof. K. Bhattacharyya of IA
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Interferon IFN induces formation of a heterotetrameric
2019-07-23
Interferon (IFN)-γ induces formation of a heterotetrameric, IFN-gamma-activated inhibitor of translation (GAIT) complex in human monocytic cp-690550 (Mazumder et al., 2003a, Sampath et al., 2004). The complex binds a bipartite stem-loop element in the 3′UTR of vascular endothelial growth factor (VEG
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IL is not expressed in tissues constitutively because
2019-07-23
IL-8 is not expressed in tissues constitutively because of its strong chemoattractant, proinflammatory, and angiogenic activities. Rather, it is an inducible factor, produced by a variety of cell types, including leukocytes, fibroblasts, endothelial and epithelial cells, in response to proinflammato
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The present review also summarizes the efforts that have bee
2019-07-23
The present review also summarizes the efforts that have been made to find new c-FMS inhibitors under clinical trial as given in the Table 1. These inhibitors may reduce the burdens of potency and side effects that have faced the scientists globally. ABT-869 41 was manufactured in Abbott laboratorie
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To estimate the nonparametric regression we
2019-07-23
To estimate the nonparametric regression, we use a B-spline basis. Let be the space of polynomial splines of degree and denote a normalized B-spline basis with and , where is the supremum norm. For any and , we have for some coefficients . Here we allow to increase with and differ for differ
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The observed increase in Bdnf mRNA occurred h
2019-07-23
The observed increase in Bdnf1 mRNA occurred 1 h after treatment indicates participation of BDNF in early plasticity and subsequently mnemonic processes. Most of the evidence regarding the importance of BDNF for memory formation derived from electrophysiological studies that utilized the molecular
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It was reported that IVM modulates various ion channels
2019-07-23
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 OICR-9429 in vertebrates (Adelsberger et al., 2000, Khakh et al., 1999, Krause et al., 1998, Krůšek and Zemková, 1994,
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Several studies have shown that independently of body weight
2019-07-23
Several studies have shown that, independently of body-weight control, the central actions of leptin improve glycemic control in obese diabetic rat and mouse models [62]. For instance, restoration of OB-Rb expression in OB-Rb-deficient mice, and in particular in POMC neurons, was sufficient to norma
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In the horse oviduct the
2019-07-23
In the horse oviduct, the EP2 receptor was most strongly expressed in epithelial flap inhibitor particularly in nonciliated (secretory) epithelial cells as evidenced by IHC. Furthermore, relative amount of EP2 mRNA was greater in the ampulla than in the isthmus, although this likely reflects differe
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br Results br Discussion The origin
2019-07-23
Results Discussion The origin and fate of Tfh cells has been intensely studied since their first description 14 years ago (Breitfeld et al., 2000, Schaerli et al., 2000). Although mice engineered to report BCL6 (Kitano et al., 2011, Liu et al., 2012) and interleukin-21 (IL-21) (Lüthje et al.,
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Early tubular differentiation in WT lacks lumen formation an
2019-07-22
Early tubular differentiation in WT lacks lumen formation and, therefore, sometimes can be confused with rosettes of ES/PNET or neuroblastoma. However, tubular structure usually has 5 alpha reductase neatly aligned to form a single layer around the future lumen, whereas neuroblastic rosettes are arr
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In mammals neutrophil elastase is a trypsin like serine
2019-07-22
In mammals, neutrophil elastase is a trypsin-like serine protease stored in the azurophilic granules of naïve neutrophils [15], [16]. The catalytic activity of neutrophil elastase relies on a His57–Asp102–Ser195 triad (chymotrypsin numbering system) that functions by transfer of electrons from the c
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