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To investigate the mechanism of action of trisubstituted
2019-10-18
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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Our results for imidacloprid were unexpected considering
2019-10-18
Our results for imidacloprid were unexpected: considering that imidacloprid (Im) is a neonicotinoid insecticide with a different mode of action (agonist of the nicotinic TC-I 2000 receptor) than OPs, we expected Es-ChE and T-ChE activity to be largely insensitive to changes in Im concentrations. Ho
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The synthetic routes to the substrates based
2019-10-18
The synthetic routes to the substrates based on the 2,3-dihydroxynaphthalene and 6,7-dibromo-2,3-dihydroxynaphthalene cores are depicted in Scheme 3. A Michael-type glycosylation of 2,3-dihydroxynaphthalene 16a gave the acetylated sugar 17a which was deprotected giving the required β-glucosidase sub
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The present study showed evidence that the
2019-10-18
The present study showed evidence that the AT1 and the ETA receptors were not expressed near or on the plasma membrane as monomers, but also as possibly constitutive dimers and tetramers. For both receptors, the proportion of monomers, dimers and tetramers were unaffected by their respective agonist
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Our previous studies indicate that EBI is
2019-10-17
Our previous studies indicate that EBI2 is involved in the regulation of pro-inflammatory responses and inter-cellular communication under pathophysiological conditions such as LPS challenge (Rutkowska et al., 2016b). The data showed that media taken from LPS stimulated astrocytes induces macrophage
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Intriguingly one E residue may serve as a
2019-10-17
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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apexbt molarity GLP signaling mediates important renal funct
2019-10-17
GLP-1 signaling mediates important renal functions [101], as suggested by the expression of both DPP-4 and GLP-1R in the kidney of several species, including humans [102]. However, controversial data exists on the specific expression pattern of these proteins, based on the specificity and sensitivit
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br Competing interests br Acknowledgements br Introduction D
2019-10-17
Competing interests Acknowledgements Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) in biomembranes to produce phosphatidic Dynorphin A (PA) [1], [2], [3], [4], [5], [6]. To date, ten mammalian DGK isozymes (α, β, γ, δ, ε, ζ, η, θ, ι and κ) have been identified.
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Another notable finding in this study is that
2019-10-17
Another notable finding in this study is that Cbl-b-mediated ubiquitination accelerates the degradation of phosphorylated DDR2. Cbl family has been documented to facilitate RTK degradation either in proteasome through K48-linked poly-ubiquitination or in lysosome through mono-, multiple mono- and K6
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DDR expression is upregulated in the glomeruli and
2019-10-17
DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident pgp inhibitors is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In fa
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DDR was originally cloned by the group
2019-10-17
DDR1 was originally cloned by the group of Michele de Luca, at the time named TrkE. The Genoa-based research team identified the skin, and the keratinocytes in particular, as a major site of DDR1-binding activity [20]. DDR1 is also expressed in kidney, liver and lung (Fig. 2). The functional role of
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The following are the supplementary data related to this
2019-10-17
The following are the supplementary data related to this article. Acknowledgments Introduction Drug-resistant epilepsy (DRE) occurs in approximate 30% of patients who suffer from epilepsy [1]. Temporal lobe epilepsy (TLE) is one of the most common partial seizures and the common cause of DRE
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CDK lacks DNA binding domains and
2019-10-17
CDK6 lacks DNA-binding domains and nuclear localization sequences, and therefore will probably be transported to the nucleus by a ‘piggy-back’ mechanism and needs to contact its specific sites indirectly through DNA-binding proteins. Besides NF-κB p65, a further candidate transcription factor is PAX
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A number of immune relevant genes have been
2019-10-17
A number of immune-relevant genes have been studied to explore the immunologic mechanisms in large yellow croakers; however, the chemokine receptor CXCR family has never been studied in this organism. Chemokines are a large superfamily of chemotactic cytokines that are utilized to direct the traffic
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In this study we observed
2019-10-17
In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased moclobemide when the sensitization condition was established. Similarly, CRF2 receptor incr
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