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During the past decade it became increasingly clear that
2020-03-12
During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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The presence of a vicious
2020-03-12
The presence of a “vicious cycle” established between tumor proliferation and paratumor osteolysis plays a crucial role in the development of primary bone tumors [53]. Cancer cells produce soluble factors that activate directly or indirectly via osteoblasts, osteoclast differentiation and maturation
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We next turned our attention to the position of
2020-03-12
We next turned our attention to the 6-position of the indole (). It was found that the chlorine atom present in was extremely important. The des-chloro analogue showed nearly 30-fold less affinity for the EP receptor in the binding assay and was nearly 30-fold lower in activity in the functional a
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As with all meta analysis this study certainly has some
2020-03-12
As with all meta-analysis, this study certainly has some limitations. First, our results were derived from unadjusted analyses due to lack of raw data, and lack of further adjusted analyses for age, gender and co-morbidity conditions may impact the reliability of our findings [63]. Second, obvious h
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br Materials and methods br Results br Discussion
2020-03-12
Materials and methods Results Discussion In rodent species, CYP2E1 and CYP2B have been implicated in CCl4 metabolism. In this study, we used expressed human CYP2E1 to show that this enzyme is a high-affinity catalyst responsible for low-dose CCl4 metabolism. Studies employing an inhibitory
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Introduction Infection of cells by
2020-03-12
Introduction Infection of (R)-PFI 2 hydrochloride receptor by microorganisms activates the inflammatory response. The initial sensing of infection is mediated by innate pattern recognition receptors (PRRs)including Toll-like receptors(TLRs) (Kawai and Akira, 2010; O’Neill et al., 2013).Toll-like re
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br Results and discussion br Conclusion We have constructed
2020-03-12
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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The Nile tilapia Oreochromis niloticus is
2020-03-11
The Nile tilapia (Oreochromis niloticus) is an important farmed fish with an XX/XY sex-determining system. The availability of the whole genome sequence of tilapia and tissue transcriptomes (Brawand et al., 2014), together with its gonadal transcriptomes at different developmental stages (Tao et al.
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Enterobacteriaceae are gram negative rods that include the
2020-03-11
Enterobacteriaceae are gram negative rods that include the Escherichia coli and Shigella. There are several DNA ligases posted on the GenBank belong mostly to Enterobacteria phages, such as the T4 bacteriophage [30]. There are several protein markers used to differentiate between T4 phage superfamil
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br Introduction Malaria remains a serious parasitic disease
2020-03-11
Introduction Malaria remains a serious parasitic disease in tropical areas due to its high morbidity and mortality rates. It is estimated that 212 million cases occurred globally in 2015, leading to 429, 000 deaths, most of which were in children aged under 5 years in Africa [1,2]. The protozoans
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In LPS treated BV cells
2020-03-11
In LPS-treated BV-2 cells, we found that the upregulated CysLT2R was translocated into the nucleus. The nuclear localization of CysLT2Rs in microglia has not been reported previously. It is known that CysLT1Rs in endothelial Sotalol translocated to the nucleus in a ligand-independent manner after i
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ESI-09 br User knowledge representation Various representati
2020-03-11
User knowledge representation Various representation approaches of user interests and preferences are proposed. In this work, we advocate a multidimensional semantic approach based on Bouzghoub et al. meta-model (Bouzeghoub and Kostadinov, 2005), depicted in Fig. 6, to model the user profile. The
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In humans individual differences in
2020-03-11
In humans, individual differences in prefrontal dopamine are partially caused by the Val158Met single-nucleotide polymorphism on the catechol-O-methyltransferase gene (COMT). This gene controls activity of the COMT enzyme, which degrades extracellular catecholamines including dopamine. The Val varia
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br Conflict of interest br Acknowledgements This work
2020-03-11
Conflict of interest Acknowledgements This work was partially supported by University of Cagliari. Introduction Organophosphorous pesticides (OPs) are wildly used in the world due to high efficiency, broad spectrum and low residue, which in turn results in environmental pollution and adver
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br Conflicts of interest br Introduction Diacylglycerols DAG
2020-03-11
Conflicts of interest Introduction Diacylglycerols (DAGs) and phosphatidic (E)-2-Decenoic acid australia (PA) play fundamental roles in biology as basic components of membranes, intermediates in lipid metabolism, and secondary messengers in cellular signaling (Carrasco and Merida, 2007, Fang
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