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A structural explanation for how RBR RING s handle their
2020-02-18
A structural explanation for how RBR RING1s handle their bound E2~Ubs differently from canonical RINGs has not been readily apparent. Only a few residue positions are strongly conserved in RING and RING1 domains, most of which are zinc-coordinating Cys and histidine residues. A key position in canon
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The RING domain was previously considered sufficient to conf
2020-02-18
The RING domain was previously considered sufficient to confer ubiquitination by RING-type E3 ligases. However, recent reports have shown that sequences closest to the RING domain are also important in E3 ligase function. Residues like Tyr193 in RNF4 [40], Phe296 and Arg294 in BIRC7 [31], and Lys65
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These studies established IAP proteins as dimeric
2020-02-18
These studies established IAP proteins as dimeric RING E3 ligases, but did not account for the essential role of dimerization. In IAPs and related E3s, such as RNF4 and MDM2, dimerization not only depends on contacts from the core RING domain but also residues N- and C-terminal to the RING domain (B
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Phylogenetically three related CXC chemokines are classified
2020-02-18
Phylogenetically three related CXC chemokines are classified as the possible ligands for the teleost CXCR1 and CXCR2. They are referred to as CXCL8_L1 (CXCL8/IL-8/CXCa), CXCL8_L2 (CXCc) and CXCL8_L3 (Alejo and Tafalla, 2011, Chen et al., 2013, Laing et al., 2002, Laing and Secombes, 2004, Nomiyama
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If the unwanted objects detected by OpenComet are manually
2020-02-17
If the unwanted objects detected by OpenComet are manually deleted, and then the DNA (%) in tail is computed, the performance of the present method can be compared more effectively. Therefore, performance of OpenComet is analysed in two ways as Approach 1 and Approach 2. Approach 1, considers the DN
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A phenylacetic acid derivative discovered in
2020-02-17
A phenylacetic BMS-833923 derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 mediated cel
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It was reported that IVM modulates various ion channels such
2020-02-17
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 dna-pk inhibitor in vertebrates (Adelsberger et al., 2000, Khakh et al., 1999, Krause et al., 1998, Krůšek and Zemková,
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paf receptor It seems plausible that this
2020-02-17
It seems plausible that this ESC-driven effect relies on a paracrine signaling. Numerous studies showed that the Fgf4 (fibroblast growth factor 4)/MAPK (mitogen-activated protein kinase) pathway is involved in PE differentiation in mouse paf receptor (Chazaud et al., 2006), (Frankenberg et al., 2011
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In this study we investigated the role phenyl tinor pt
2020-02-17
In this study we investigated the role 17-phenyl tinor (pt)-PGE2 on endothelial barrier function and the underlying molecular mechanism in HMVEC-Ls as well as in a murine model of LPS-induced acute pulmonary inflammation. We found that 17-pt-PGE2 concentration-dependently enhanced endothelial barrie
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br Conclusions Enzyme prodrug therapy
2020-02-17
Conclusions Enzyme prodrug therapy mediated by implantable biomaterials combines the benefits offered by the site specific drug delivery techniques and the systemic administration of drugs. From the former, SMEPT inherits the localized mode of drug delivery with lower systemic distribution of the
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Pentamidine Lavallee et al reported that PREG could be
2020-02-17
Lavallee et al. [30] reported that PREG could be esterified by lecithin:cholesterol acyltransferase (LCAT). LCAT uses cholesterol and phosphatidyl choline present in the newly formed high-density lipoprotein (HDL) as substrates and convert them into cholesteryl esters and lysophosphatidyl choline. T
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PI K is a lipid kinase and generates phosphatidylinositol tr
2020-02-17
PI3K is a lipid kinase and generates phosphatidylinositol-(3,4,5)-trisphosphate, which is a second messenger critical for the translocation of Akt to the cytoplasmic membrane. The phosphorylation of Ser473 Akt is important in the cell survival by regulating the eNOS among other targets (Dimmeler et
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br Clinical potential of ET receptor biased ligands
2020-02-17
Clinical potential of ET receptor biased ligands Is there a clinical need for ET receptor biased ligands? Evidence is strongest from research in epithelial ovarian cancer demonstrating that ET-1 stimulated ETA-mediated β-arrestin signalling leads to activation of the oncogenic mediator NF-κB [21]
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The secondary objective of the present study was
2020-02-15
The secondary objective of the present study was to evaluate the pharmacokinetics, safety, and tolerability of multiple oral doses of 450-mg delafloxacin to reach steady state in healthy male and female subjects. After multiple dosing of oral delafloxacin, steady state was reached after 4 days of do
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For membrane protected SPE the choice of sorbent
2020-02-15
For membrane protected μ-SPE, the choice of sorbent is crucial because it determines the extraction efficiency. Up to now, many porous materials, such as carbon based sorbents [1,[3], [4], [5], [6]], ethylsilane or octadecylsilane modified silica (C2 or C18) [7,8], polymeric materials [[9], [10], [1
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