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The present study also showed that EP
2020-05-05

The present study also showed that EP2 deficiency and EP4 antagonism significantly suppressed psoriatic LY3039478 in an imiquimod model. Notably, however, the combined EP2 deficiency and EP4 antagonism did not completely suppress ear swelling in this model, possibly because there is the IL-17–indep
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Dual inhibition of ACE and NEP as a strategy for
2020-05-05

Dual inhibition of ACE and NEP as a strategy for treating hypertension has been extensively investigated, including contributions from these laboratories through the discovery of Sampatrilat . Given that both targets are related zinc metalloproteinases, dual enzyme inhibition can be achieved within
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Among the Ub interactions observed in
2020-05-05

Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati
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Wu et al explored the anti inflammatory mechanisms by
2020-05-05

Wu et al. explored the anti-inflammatory mechanisms by which osthole 35 acted on HepG2 cells cultured in a differentiated medium from cultured 3T3-L1 preadipocyte cells. HepG2 cells, a human liver cell line, were treated with various concentrations of osthole 35 in differentiated media from cultured
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Although the analysis described above goes
2020-05-05

Although the analysis described above goes far to explain the mechanism of Concanamycin A perturbations through CHK1 inhibition, it raises important questions about the mechanism by which WT RAS isoforms promote CHK1 S280 phosphorylation. Previous reports have shown that both the MAPK-RSK and PI3K-
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The major concern of PDE
2020-05-05

The major concern of PDE-5-I use in liver cirrhosis is the potentially harmful effect on systemic blood pressure. Data of clinical studies are conflicting [27], [30], [31], [32], but available patient details suggest that in advanced liver cirrhosis, PDE-5-Is lower systemic blood pressure to a great
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Our results are the first to demonstrate that
2020-05-05

Our results are the first to demonstrate that ERRγ acts as a catabolic regulator of cartilage degeneration and OA pathogenesis, and collectively support the idea that ERRγ could be a therapeutic target for OA Introduction DNA cytosine-5-methyltransferases (Dnmts) catalyze the methyl transfer fr
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br Disclosures br Acknowledgements This work
2020-05-05

Disclosures Acknowledgements This work was supported in part by grants from the Ministerio de Ciencia e Innovación, Spain (SAF2010-22051) and Xunta de Galicia, Spain (INCITE08PXIB203092PR). Introduction Ca is a key element in cardiac excitation–contraction (EC) coupling. In each heartbeat,
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More and more studies are focused on the
2020-05-05

More and more studies are focused on the function role of EPAC1 in cancer proliferation, apoptosis and migration. Recently, it was reported that the EPAC-ERK and AKT signaling pathways promote the B cell antigen receptor (BCR) mediated growth arrest and apoptosis in the B lymphoma cell line WEHI-231
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Apart from its high affinity the selection of GW
2020-04-30

Apart from its high affinity, the selection of GW2580 as Chlorogenic acid lead in our radiotracer development program was motivated by its exceptional selectivity. The observed profound impact of small structural modifications on the selected panel of four kinases tested prompted us to conduct compr
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It remains unclear how LINE RNA
2020-04-30

It remains unclear how LINE1 RNA-Nucleolin-Kap1 are targeted to the Dux cluster. LINE1-Nucleolin-Kap1 may have other interacting partners with DNA binding specificity. For example, YY1 has been implicated in targeting a repressive complex containing Nucleolin to the human DUX4 cluster (Gabellini et
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br Cytochrome P monooxygenases Cytochrome P
2020-04-30

Cytochrome P450 monooxygenases Cytochrome P450 monooxygenases (P450s) belong to one of Nature’s most versatile group of enzymes for C–H functionalization and are able to perform challenging regioselective and stereoselective activations of remote, unactivated C(sp3)–H bonds, for which there are o
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br Acknowledgements This study was financially supported by
2020-04-30

Acknowledgements This study was financially supported by the National Special Research Programs for Non-Profit Trades (Agriculture) (Grant No. 201303045) and the Basic Foundation for Scientific Research of the State-level Public Welfare Institutes of China (Grant No. 2013JB10). Introduction L
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In summary we elucidated the in vitro activities
2020-04-30

In summary, we elucidated the in vitro activities of KDM1B in regulation of PC cell proliferation and apoptosis. These studies provided a novel insight into the previously unrecognized roles of KDM1B in human PC cells. We showed for the first time that KDM1B knockdown attenuated proliferation and in
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br Results and discussion br Conclusion A new
2020-04-30

Results and discussion Conclusion A new series of 2-mercapto-quinazolin-4-one analogues is designed and synthesized to possess electron withdrawing or donating functional groups (Cl or CH3O) at position 6- or 7-, 4-methoxyphenyl function at position 3. The 2-mercapto function is used to connec
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