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One possible explanation for differences
2021-05-31

One possible explanation for differences in the binding ability of monomeric versus dimeric forms of DDR2 ECD to collagen could be that the monomeric form only binds to the primary GVMGFO site, whereas dimeric (and oligomeric) DDR2 ECD binds to additional sites on the collagen triple-helical molecul
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Midazolam oral clearance is used for characterization of bot
2021-05-31

Midazolam oral clearance is used for characterization of both intestinal and hepatic CYP3A activity. However, the identification and subsequent use of metabolic markers of CYP3A activity can eliminate the need for unnecessary administration of probe drugs such as midazolam. Such metabolic markers wo
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br Material and methods br Results br Discussion In
2021-05-31

Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in
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Another breakthrough towards the understanding of the
2021-05-31

Another breakthrough towards the understanding of the mechanisms responsible for stress-induced relapse to drug seeking behaviour is the evidence published by the group of Wise [34] in which they show that the activation of VTA CRF2 and not CRF1 receptors is responsible for stress-mediated relapse t
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The aim of this study was to use molecular
2021-05-28

The aim of this study was to use molecular methods to characterise C. difficile isolates circulating in the Czech Republic from 2013 to 2015. Material and methods Discussion During a three-year period (2013–2015) a total of 32 hospitals voluntarily participated in this project, but only 11 ho
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honokiol Fisetin tetrahydroxyflavone is a flavonol
2021-05-28

Fisetin (3,3′,4′,7-tetrahydroxyflavone) is a flavonol present in several fruits and vegetables such as grape, persimmon, strawberry, apple, and onion at concentrations rangeing from 2 to 160 μg/g. Fisetin is a well–known bioflavonoid with remarkable biological effects including chemopreventive/chemo
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In addition to providing substantial
2021-05-28

In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus
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In conclusion we have identified
2021-05-28

In conclusion, we have identified Ednra as a downstream direct target of Hoxa9 and Meis1. Upregulation of Ednra has a role in the progression of Hoxa9+Meis1-induced leukemia and targeting Ednra together with other chemotherapies may have therapeutic benefits for leukemia [30]. Ednra inhibitors in th
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Since the number of peptides
2021-05-28

Since the number of peptides hydrolized by PEP is quite large, it is not easy to relate the increase of enzymatic activity with the altered changes of a concrete peptide. However, it is noticeable that imbalances of several natural substrates of PEP [6], such as angiotensins, bradykinin, vasopressin
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br Conflicts of interest br Acknowledgements br Introduction
2021-05-28

Conflicts of interest Acknowledgements Introduction Atherosclerosis is the number one cause of death in the United States and among the leading causes of morbidity and mortality globally [1]. Inflammation is critical in all stages of atherosclerosis from the formation of a plaque in the ves
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ICT is a product of
2021-05-28

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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br Materials and methods br Results br Discussion UPP
2021-05-28

Materials and methods Results Discussion UPP components including the proteasome, E1s, E2s, E3s and DUBs may become one the most important NF 449 of therapeutic targets for the pharmaceutical industry in the near future and supersede those which are involved in the phosphorylation system [
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br Four active site residues of KSTD are
2021-05-28

Four active site residues of Δ1-KSTD1 are fully conserved in Δ1-KSTDs from different species (Supplementary Figure S2). These residues are Tyr-119, Tyr-487, and Gly-491 from the FAD-binding domain and Tyr-318 from the catalytic domain. The structure of the Δ1-KSTD1•ADD complex revealed that the hy
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The secondary objective of the present study was to evaluate
2021-05-28

The secondary objective of the present study was to evaluate the pharmacokinetics, safety, and tolerability of multiple oral doses of 450-mg delafloxacin to reach steady state in healthy male and female subjects. After multiple dosing of oral delafloxacin, steady state was reached after 4 days of do
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br Materials and methods br
2021-05-28

Materials and methods Results Discussion We confirmed the published cDNA and protein sequence of feline CSF-1R and stably cloned the cat receptor into the Ba/F3 cell line. Activation of feline CSF-1R by recombinant human CSF-1 was previously tested by Woolford et al. [14]. Expression of onc
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