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Several highly potent CysLT receptor antagonists with large
2020-11-03

Several highly potent CysLT1 receptor antagonists with large structural glucagon like peptide have been developed. Beyond antagonists with structures analogous to cysteinyl leukotrienes, other subclasses comprise: (a) hydroxyacetophenones, (b) indoles and indazoles, (c) quinolines, benzothiazoles,
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To assess which export pathway is used
2020-11-03

To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 raf kinase with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activity as well
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Kaempferol-3-rutinoside synthesis Introduction Globally lung
2020-11-03

Introduction Globally, lung cancer has the highest morbidity and mortality rates of all types of cancer, with 1.5 million patients newly diagnosed annually [1]. Approximately 85% of lung cancer cases are non-small cell lung cancer (NSCLC) [2]. The first-line treatment for NSCLC is surgical resectio
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Partial suppression of the cot ts phenotype by deletion of
2020-11-03

Partial suppression of the cot-1 (ts) phenotype by deletion of gul-1 has been well documented (Seiler et al., 2006). This is now also very clearly evident in the transcriptional profile of the various strains (Fig. 2). Furthermore, the comparative analysis of the single and double mutants revealed,
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Artificial permutations have also been
2020-11-03

Artificial permutations have also been exploited by protein engineering to manipulate protein scaffolds, in order to improve catalytic activity, alter substrate or ligand binding affinity, reduce proteolytic susceptibility, increase stability, generate different aggregation states and improve fluore
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Several recent reviews have appeared covering different
2020-11-03

Several recent reviews have appeared covering different aspects of the sPLA2 family of enzymes, including sPLA2-V, and the interested reader is kindly directed to these for specific details [34,[135], [136], [137]]. It is important to remark here, however, that recent studies on sPLA2-V suggest that
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Berberine Studies have focused on a hydrophobic
2020-11-03

Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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br Experimental Procedures br Author Contributions br Acknow
2020-11-03

Experimental Procedures Author Contributions Acknowledgments Research in the Davis laboratory was supported by grants 4R37NS019904, 5R01NS052351, and 1R35NS097224 from NINDS. Research in the Martemyanov laboratory was supported by grants DA036596 and DA026405 from NIDA, and MH105482 from NI
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br Conclusion The role of DNA PK
2020-11-03

Conclusion The role of DNA-PK target in DNA DSB repair renders this Pradaxa kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for design of p
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Introduction Trichloroacetic acid TCA might enhance
2020-11-03

Introduction Trichloroacetic FK 866 hydrochloride (TCA) might enhance the activation of T cells and disrupt various activities of peripheral T cells [1], which is related to human immune function and reduces human immunity. Trichloroethylene (TCE) has been widely used in many manufacturing industr
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br Introduction Acylglycerol acyltransferases AGATs are pred
2020-11-03

Introduction Acylglycerol acyltransferases (AGATs) are predominantly responsible for triglyceride synthesis in the body, via two major pathways: the glycerol phosphate (GP) pathway (Kennedy, 1957) and the monoacylglycerol (MG) pathway (see Coleman and Lee, 2004, Yen et al., 2008). The final step
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br Subjects and methods br Results br Discussion In
2020-11-03

Subjects and methods Results Discussion In the present study, we found significantly increased CSF levels of IL-4, IL-5, IL-9, IL-10, TNF-α, CXCL8/IL-8, and VEGF-A together with significantly higher detection rates of IL-6, GM-CSF, PDGF-BB and IL-1ra in IHP patients compared with OND patien
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The isolation of a proteinaceous putative inhibitor of
2020-11-03

The isolation of a proteinaceous putative inhibitor of cysteine proteases from the extracts of Y. enterocolitica and E. coli was performed by affinity chromatography on immobilized and inactivated papain (Fig. 7A). Instead of the column variant of this technique (Tsushima et al., 1992), we used a ba
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The ACC receptor family appear to be attractive targets for
2020-11-02

The ACC receptor family appear to be attractive targets for the development of novel anthelmintics. With this in mind we also tested the activity of the anthelmintics levamisole and pyrantel which activate the nematode nAChR (Martin and Robertson, 2007). We found both molecules were partial agonists
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br Acknowledgements Professor Olli A J nne is warmly
2020-11-02

Acknowledgements Professor Olli A. Jänne is warmly thanked for support and for providing excellent research facilities. Professor Patrik Finne is acknowledged for his help with statistical analyses. Drs Ronald Evans, Vincent Giguère, Jorma Palvimo, Malcolm Parker, and Anastasia Kralli are acknowl
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