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EBI remains an orphan GPCR and the identity and
2020-02-07
EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et
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DDR expression is upregulated in the glomeruli and tubules o
2020-02-06
DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident SLx-2119 is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In favor to
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One of the critical functions of
2020-02-06
One of the critical functions of the product of the AR gene is to activate the expression of target genes. This transactivation activity resides in the N-terminal domain of the protein encoded in exon 1, which contains polymorphic repeats. These trinucleotide repeats, (CAG) and (GGC), encode polyglu
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Although the implication of DA
2020-02-06
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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DA neurons are capable of somatodendritic and
2020-02-05
DA neurons are capable of somatodendritic and axonal DA release, which may occur at synapses, as well as non-synaptic or asynaptic sites (Trudeau et al., 2014). DA may also be released at different timescales and in response to different DA neuron firing patterns (Grace et al., 2007). Furthermore, s
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Analysis of Table shows that compound b in which
2020-02-05
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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Cucurbitacin B The defining molecular feature of Ewing sarco
2020-02-05
The defining molecular feature of Ewing sarcoma is the characteristic EWSR1/ETS fusion protein, most commonly involving EWSR1 and FLI1 (Delattre et al., 1992, May et al., 1993). EWS–FLI1 causes global changes in gene expression both by directly regulating gene expression and by causing changes in ch
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We found all cases to show at least
2020-02-05
We found all cases to show at least some IGF-1R expression by immunohistochemistry. This is consistent with its ubiquity at the mRNA or protein level in ES/PNET cell lines or clinical samples as shown by others.12, 14 Evidence that IGF-1R expression is required for EWS-FLI1 transformation of mouse f
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Upon assembly of HLA tetramers loaded with either of the
2020-02-05
Upon assembly of HLA tetramers loaded with either of the two peptide versions, we could query the T cell repertoires of RA subjects and healthy individuals for the presence of cognate T pmsf recognizing the respective peptide-HLA complexes. We found no significant difference in frequencies of T cell
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EC barrier dysfunction triggered by inflammatory mediators i
2020-02-04
EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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The optimization of the lead compound
2020-02-04
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic cp-690550 moiety with other functional groups led to loss of functional activity against EP4 receptor. Al
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Using the juxtarenal PPE the
2020-02-04
Using the juxtarenal PPE, the induction of juxta- and suprarenal aneurysms is described herein (Fig. 3A). The infra-/suprarenal part of the all trans retinal receptor can now be investigated separately, taking into account different embryological backgrounds and varying reactivity to differing stim
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Several limitations of this study need
2020-02-04
Several limitations of this study need to be acknowledged. First, although 200 patients were recruited into this study and completed assessments at baseline, only 89 patients completed the cognitive tests after 8weeks of treatment. The relatively long study period (8weeks) was the main reason for th
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The involvement of FOXO and
2020-02-04
The involvement of FOXO3 and STAT5 in DNA-PKcs and Microcystin-LR IV has not been reported before, and the search by the ECR browser (http://ecrbrowser.decode.org) revealed that 1kb of the 5′ promoter of DNA-PKcs possesses 4 STAT (−908bp to −901bp, −676bp to −656bp, −533bp to −526bp and −66bp to −5
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Heparin AMD is equally active against a broad
2020-02-04
AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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