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Grapiprant is a selective antagonist for prostaglandin E PGE
2020-02-21

Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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br Conclusions br Declaration of interest
2020-02-21

Conclusions Declaration of interest Acknowledgements Introduction Uncorrected obesity has been a major health problem and the prevalence of obesity is fast rising reaching an epidemic proportion [[1], [2], [3]]. Ample of clinical and experimental evidence has suggested that obesity leads
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br Biological roles of DGK br Summary and future perspective
2020-02-21

Biological roles of DGKϵ Summary and future perspectives The most Phosphatase Inhibitor Cocktail 1 (100X in DMSO) segment of DGKϵ, comprised of residues 20–42, appears to have no role in binding the lipid substrate DAG or in the acyl chain specificity of substrate phosphorylation. Nevertheles
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Finally the identification of predictive
2020-02-21

Finally, the identification of predictive biomarkers of response will also allow the more recently discovered CDK inhibitors to be explored in particular genetically-defined contexts, for example by building on recent observations that KRAS mutant tumors are highly sensitive to CDK1 inhibition, and
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Recent studies have shown that
2020-02-21

Recent studies have shown that some CLC genes participate in plant salt tolerance and have speculated that they function by mediating Cl− transport across the tonoplast. For instance, AtCLCc, a vacuolar anion transporter, is shown to be involved in the regulation of stomatal movement and to contribu
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The discoidin domain receptors DDR and DDR are
2020-02-21

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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Judging from the densitometric analysis of the Western blots
2020-02-21

Judging from the densitometric analysis of the Western blots, CYP2E1 protein was expressed, although at very low levels, by PT cells. This corresponds to previous observations [10], showing that CYP2E1 was expressed in the PT, although expression was higher in the distal tubule. Testosterone 6β-hyd
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br STAR Methods br Acknowledgments We are
2020-02-21

STAR★Methods Acknowledgments We are grateful to Matthias Mayer at ZMBH in Heidelberg for access to his CD-spectrometer and his help in data interpretation. Technical support by Wolfgang Weinig is gratefully acknowledged. This project was financially supported by the European Union as part of t
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CHAPS br Fragment based drug discovery FBDD is
2020-02-21

Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical CHAPS space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It also
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br Results br Discussion SDF
2020-02-21

Results Discussion SDF-1 performs essential roles in cell migration and proliferation, acts as neuromodulator; and is also involved in many pathological processes including human immunodeficiency virus infection, metastatic malignancy, and chronic inflammatory disorders (Feng et al., 1996, Li
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Third we also found negative correlations between TREM mRNA
2020-02-21

Third, we also found negative correlations between TREM2 mRNA expression and the methylation rate of 4 CpG sites in the intron 1 of TREM2. Gene methylation rates are generally associated with gene expression. Thus, heavily methylated areas of genes are usually less active at the transcriptional leve
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Here we report that ILC s sensed
2020-02-20

Here, we report that ILC3s sensed oxysterols through GPR183, which was highly expressed by LTi-like ILC3s. 7α,25-OHC-synthesizing enzymes were produced by fibroblastic stromal gallic acid found in intestinal lymphoid structures, and the GPR183 ligand 7α,25-OHC acted as a chemoattractant for ILC3s.
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ICT is a product of icariin
2020-02-20

ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene
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In this study we examined a possible association
2020-02-20

In this study, we examined a possible association between the 19-bp gtpase and the 9-bp repeat in the DHFR gene and the risk of spina bifida in 121 mothers of a spina bifida affected child, 292 control women, 109 spina bifida patients and 234 pediatric controls using a case-control design. Furthermo
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The first example of a broadly
2020-02-20

The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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