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The possibility of harm with DPP inhibitors in patients
2019-07-18
The possibility of harm with DPP-4 inhibitors in patients with clinically overt heart failure has been recently highlighted by the results of the VIVIDD (Vildagliptin in Ventricular Dysfunction Diabetes) trial (68), the only trial to date that has been designed to evaluate the effects of a DPP-4 inh
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br Conclusion To our knowledge this study is the
2019-07-18
Conclusion To our knowledge, this study is the first to give evidence that the ETA selective antagonist BQ-123 reverses the cisplatin-induced ARF mainly via restoring SOD activity, in addition to other antioxidant parameters, NO, TNF-α and caspase-3 levels. And that this protective effect require
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br Allosteric inhibitors In general candidate drugs that bin
2019-07-18
Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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Quercitrin chemical Replacement of the saturated propoxy gro
2019-07-18
Replacement of the saturated -propoxy group in compound with the unsaturated allyloxy group to obtain compound resulted in 10-fold decrease in ET receptor antagonism and more than 20-fold decrease in ET-selectivity. Analogous unsaturated allyloxy compound in the tetrazole series was found to have
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In conclusion the present study demonstrates that
2019-07-17
In conclusion, the present study demonstrates that E2\'s antiapoptotic effects are significantly reduced by coadministration of progestogens. The combination of E2 and progestogens resulted in diverging effects on the expressions of ERs and PRs, which induced different effects on the cell growth of
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A putative SHBG receptor SHBG
2019-07-17
A putative SHBG concentration calculator (SHBG-R) has been postulated for about thirty years [66], [69], [70]. The characterization of this receptor has been researched by several groups. There are different ideas on how this receptor works. On the one hand Fortunati et al. provide evidence that SHB
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Form the previous literature It was observed that RHA
2019-07-17
Form the previous literature, It was observed that RHA was burnt in the range of 500 °C to 700 °C, with high content of quartzite silica was used is a partial replacement of cement in mortar and in concrete. The results shown an excellent behavior in enhancing the mechanical properties of cement mor
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Here we investigate in more
2019-07-17
Here we investigate in more detail how Dot1 function contributes to the regulation of DNA damage tolerance. We find that Dot1 modulates the response to the alkylating agent MMS through its catalytic activity on H3K79. In fact, progressively reduced levels of H3K79 tri-methylation result in gradually
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wst-1 assay We also discovered important clues to domain bin
2019-07-17
We also discovered important clues to domain wst-1 assay of DGKs and how to exploit these regions for development of DGKα-selective inhibitors. The identification of a probe-modified site at the C1 domain provided the first evidence of a ligand binding site remote from the ATP binding region of DGK
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br Acknowledgements This work was supported by grants
2019-07-17
Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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The annotation is arguably the
2019-07-17
The annotation is arguably the most important part of analysis, as it enables one to evaluate and interpret the content of the transcriptome assembly. In this context, the non-redundant contigs were initially run in BLAST against the Nr database showing that 55% of them displayed high similarity to
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In the pleural exudates which reflect the
2019-07-17
In the pleural exudates, which reflect the in vivo conditions, the concentrations of CysLTs and PGE2 were quite similar. However, when cancer Coumarin were cultured for 24 h, both analyses of cell culture medium and cell incubations with Ca2+ ionophore showed low levels of CysLTs. In contrast, the p
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Recently it has been shown
2019-07-17
Recently, it has been shown that among the ELR (+) chemokines mentioned above, particularly IL-8 induces neutrophil migration via CXCR-1 chemokine receptor. For example, Godaly et al. [18] reported the potent role of CXCR-1 chemokine receptor in the process of neutrophil migration across epithelial
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Under conditions of energy scarcity or nutritional restricti
2019-07-17
Under conditions of energy scarcity or nutritional restriction, AMPK, a critical energy sensor, is activated in response to the increased ratio of AMP to ATP. Various kinases may phosphorylate AMPK, leading to its activation. For example, AMPK phosphorylation by liver kinase B 1 (LKB1) at Thr172 res
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Some pyrimidine analogs are substrate based inhibitors that
2019-07-16
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHOD
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