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We have previously disclosed the
2021-06-02
We have previously disclosed the discovery of a 7-azaindole-3-acetic Octyl-α-ketoglutarate CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of
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Park et al expanded their own model
2021-06-02
Park et al. [34] expanded their own model as hydrogen- bonding lattice fluid EOS (NLF-HB) [35] for calculating the activity coefficients of aqueous amino ixabepilone solution. Further, Pazuki et al. [36] extended the perturbed hard chain theory which has been proposed by Beret and Prausnitz [37] fo
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To investigate the mechanism of action of trisubstituted
2021-06-02
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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The evaluation of internal exposure in workers with omethoat
2021-06-02
The evaluation of internal exposure in workers with omethoate is challenging. Unfortunately, OPs are metabolized and excreted quickly in the urine usually within 24–48 h of exposure, and the variation in metabolic rates exists. Many factors influence daily urinary output, such as salt intake, urea a
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ERR is expressed in several adult
2021-06-02
ERRγ is expressed in several adult and embryonic tissues but its biological role is still largely unknown [21]. Overexpression of ERRγ in breast cancer correlates with a favorable outcome [22]. In addition, ERRγ has been reported to inhibit the growth of prostate tumor leonurine [23]. In this study
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The synthetic route chosen for the preparation of the substr
2021-06-02
The synthetic route chosen for the preparation of the substrates 18 is shown in Scheme 3. Commercially available 4-aminobenzyl alcohol 13 was found to be relatively unstable to storage and hence it was prepared immediately before use by reduction of the readily available and inexpensive 4-nitrobenzy
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A number of chemical strategies have been
2021-06-02
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai
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Initially we ascertained that if the dose of
2021-06-01
Initially, we ascertained that if the dose of elastase was sufficient to cause pulmonary emphysema, then pulmonary emphysema could be maintained throughout the study. We found that elastase at 3U was sufficient to cause emphysema that remained over 35 days. In this experimental design of lung disea
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Several studies have demonstrated that Syn
2021-06-01
Several studies have demonstrated that αSyn specifically associates with lipid rafts (Cole et al., 2002), raising the possibility that the perturbation of rafts can affect the aggregation and phosphorylation of αSyn (Fortin et al., 2004). Schneider et al. (2010) described the potential involvement o
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Our studies approached this problem using
2021-06-01
Our studies approached this problem using integrative -omics analysis of human NK-ieILC1s from distinct microenvironments and functional subsets, including helper and adaptive phenotypes. At both the transcriptional and epigenetic levels, we find that the adaptive subset, CD57+ cytotoxic NK cells, s
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In all available E E structures the
2021-06-01
In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin tran
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rifadin mg In all available E E structures the RING type dom
2021-06-01
In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans
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The HEV vaccine developed based
2021-06-01
The HEV vaccine, developed based on p239 particles, is of good efficacy, immunogenicity and safety, and was licensed in China in 2012. p239 (aa 368–606) and E2 (aa 394–606) share a common region of ORF2, referred to as E2s (aa 459–606), which harbors the major antigenic determinants of the HEV vacci
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br Effect of DPP Inhibitors on the Clinical
2021-06-01
Effect of DPP-4 Inhibitors on the Clinical Course of Heart Failure Four large-scale cardiovascular outcomes trials with DPP-4 inhibitors have been completed, and their findings have been published (Table 1) 31, 32, 33, 34. In 2 studies (with saxagliptin and alogliptin), DPP-4 inhibition was accom
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br Conclusion Our objective is to
2021-06-01
Conclusion Our objective is to promote cell activity on biomaterials, especially for use in regenerative medicine, by grafting THPs containing collagen-binding sites onto inert substrates. We have previously reported a methodology to derivatize EDC/NHS crosslinked films with photoreactive THPs. T
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