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In the course of our program which was aimed
2021-06-18

In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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In the last and the most challenging
2021-06-18

In the last and the most challenging part, three mixtures were selected to evaluate the reliability of the presented correlation and the CPA model. For Athabasca bitumen, Amani et al. [25] measured the experimental data at very high temperatures compared to the thermal recovery range up to 644 K (ne
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The present study is the first time to investigate the
2021-06-18

The present study is the first time to investigate the effect of piperine on intestinal sterol transporters and enzymes in the small intestine. NPC1L1 is a sterol transporter responsible for taking up cholesterol from the lumen to enterocytes (Davis et al., 2004). ACAT2 is an enzyme, which esterifie
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In modern science and technology
2021-06-18

In modern science and technology, many optimization problems need to be solved in real time, while these classical methods cannot render real-time solutions to these optimization problems, especially large-scale problems. As a new metaheuristic, particle swarm optimization (PSO) [18], [19] has prove
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The mechanisms by which Cav enhances embryonal
2021-06-18

The mechanisms by which Cav-1 enhances embryonal tumor progression are currently unknown. Given the documented ability of Cav-1 to drive increased biogenesis of caveolae and accelerate the flow of nutrients (mostly glucose and fatty acids) across the membrane, as observed in particular in adipocytes
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br Materials and methods br Results br Discussion Cells
2021-06-18

Materials and methods Results Discussion Cells in the human body, especially in the cardiovascular and musculoskeletal systems, undergo a variety of mechanical stimuli. In order to ensure human movement, the strength of stretching muscles acts on cartilage and bone, moving joints through te
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As an endogenous negative modulator CRBN inhibits AMPK s
2021-06-18

As an endogenous negative modulator, CRBN inhibits AMPK’s activation (phosphorylation of Thr172) by directly binding to the α-subunit of AMPK, disrupting γ-subunit recruitment to the AMPK complex (Lee et al., 2011, Lee et al., 2013). In our study, we did not focus on AMPK activation, since only a si
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A growing number of other post translational modifications a
2021-06-18

A growing number of other post-translational modifications are implicated in regulation of the ubiquitin system, including substrate modification by hydroxylation, glycosylation, acetylation, methylation, modification by poly(ADP-ribose) (PAR), and attachment of ubiquitin-like modifiers. The HIF1-α
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Since both the Ub and ISG systems are
2021-06-18

Since both the Ub and ISG15 systems are crucial for the innate immune response, many prokaryotic and viral pathogens have evolved ways to hijack them in order to create a “window-of-opportunity” for efficient replication. Several viral and bacterial proteins have been found to directly target these
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br Results and discussion br Conclusion We have
2021-06-18

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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br Acknowledgements We thank Dr James Ritchie and
2021-06-18

Acknowledgements We thank Dr. James Ritchie and his dedicated staff (Deptartment of Pathology, Emory University) for performing measures of serum VPA levels; Sumitomo Pharmaceuticals (Osaka, Japan) for the generous donation of DOPS, which is required for breeding Dbh −/− mice; Pfizer (Sandwich, K
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Poxviruses have double stranded DNA
2021-06-18

Poxviruses have double-stranded DNA (dsDNA) genomes, yet they replicate within the cytoplasm. Poxviruses that cause human disease include monkeypox virus (Reynolds et al., 2004), molluscum contagiosum virus (Hanson and Diven, 2003) and variola virus (VARV), the cause of smallpox, a disease eradicate
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Recently it has been shown that among the ELR
2021-06-17

Recently, it has been shown that among the ELR (+) chemokines mentioned above, particularly IL-8 induces neutrophil migration via CXCR-1 chemokine receptor. For example, Godaly et al. [18] reported the potent role of CXCR-1 chemokine receptor in the process of neutrophil migration across epithelial
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br Future direction and conclusion
2021-06-17

Future direction and conclusion Conflict of interest References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Introduction Colony stimulating factor-1 (CSF-1; also referred to as the macrophage-colony stimulating
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Introduction The carnitine choline acyltransferase
2021-06-17

Introduction The carnitine/choline acyltransferase family is a family of enzymes that play diverse roles, ranging from (the regulation of) GSK2636771 and fuel metabolism in mitochondria and peroxisomes to the generation of the neurotransmitter acetylcholine. In mammals, this family consists of sev
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