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Another milestone in the field is the de novo
2019-10-02
Another milestone in the field is the de novo discovery of EPAC2 and EPAC1 specific inhibitors through fluorescence-based HTS assays. Due to the excellent EPAC/PKA selectivity of PF-CBP1 hydrochloride , it has been widely applied as a useful chemical probe to discriminate EPAC related signaling pat
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To compare the phage of
2019-10-02
To compare the phage of the 4th round results, we conducted isolated single rounds of FGE screening as described above for the 4 individual phage 4(1), 4(2), 4(3), and NC then determined the number of colony forming units afforded by cleavage from the support. Interestingly, we found that the 4(2) s
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EBI remains an orphan GPCR and the identity
2019-10-01
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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Our data supports the conclusion that the exonuclease activi
2019-10-01
Our data supports the conclusion that the exonuclease activity thought to be intrinsic to Artemis is not a component of the Artemis polypeptide. Many possibilities exist to explain the presence of the exonuclease activity in less-pure fractions of Artemis. It is possible that the exonuclease is simp
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It is well established that Shp can function
2019-10-01
It is well established that Shp-2 can function as a substrate for several RTK, such as PDGF or EGFR [23], [36]. To test whether DDR1 recognizes Shp-2 as its substrate, we overexpressed a catalytically inactive Shp-2 mutant together with DDR1b in 293 cells [31]. Immunoprecipitation of Shp-2 followed
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Compounds and administered orally to fasted
2019-10-01
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinical
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In vivo study showed that the
2019-10-01
In vivo study showed that the CYP3A activity was increased, when morroniside (10, 30 and 90 mg/kg, i.g.) was daily for seven consecutive days. Further, RT-PCR analysis showed that the induction of mRNA melk inhibitor by morroniside (10, 30 and 90 mg/kg, i.g.) was 1.13-, 1.43- and 1.79-fold higher,
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br Methods br Results br Discussion The lowest intra
2019-10-01
Methods Results Discussion The lowest intra-CeA dose of R278995/CRA0450 that prevented the elevations in IT-901 reward thresholds associated with nicotine withdrawal was 0.05μg/side (0.1μg total bilateral dose). The total bilateral dose in the present study is 100 times lower than the lowe
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br Materials and methods br Results br
2019-10-01
Materials and methods Results Discussion Intra-BNST injections of NOC-9 (at all doses) were able to produce freezing and anxiogenic-like effects. Freezing was observed immediately after the NO donor injection and lasted about 2–3min (data not shown). When exposed to the EPM 5min after intra
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NVP-AEE788 Analysis of DNA fragmentation We
2019-10-01
Analysis of DNA fragmentation. We followed a modified Hirt extraction procedure for analysis of DNA fragmentation. Cells were suspended in TNE buffer (1M NaCl, 20mM Tris–HCl, pH 7.4, 2mM EDTA, and 0.6% SDS) at a density of 106 cells/ml and incubated overnight on ice. The next day, cellular debris wa
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5\'-Iodoresiniferatoxin kinase br DGKs inhibition and si
2019-10-01
DGKs inhibition and signaling Local DAG levels are strictly controlled by a balance between synthesis and degradation rates. Both receptor controlled PLC-mediated production and DGK-mediated degradation are classically implicated in the control of “signaling” DAG. However, this dogma is starting
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br Conclusion br Competing interests br Authors
2019-10-01
Conclusion Competing interests Authors\' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number
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Phylogenetically three related CXC chemokines are classified
2019-09-30
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 e
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BIRB796 In frame exon skipping of COL A has been
2019-09-30
In frame exon 41 skipping of COL6A3 has been suspected to be responsible for isolated dystonia in several human kindreds without muscular defects [94]. In order to validate their hypothesis, the authors used zebrafish to selectively knock down several exons in col6a3 and found a negative impact on m
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br Experimental br Declaration of interest br Introduction b
2019-09-30
Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR vitamin d receptor library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound was m
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