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Several highly selective COX inhibitors
2020-08-13
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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br Materials and methods br Results br Discussion br
2020-08-12
Materials and methods Results Discussion Conflict of interest Introduction Dopamine-β-hydroxylase (DβH) deficiency is a rare autosomal recessive disorder characterized by the congenital absence of DβH, the enzyme converting dopamine to noradrenaline in sympathetic nerve terminals and
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br Introduction Lung cancer is the leading cause of cancer
2020-08-12
Introduction Lung cancer is the leading cause of cancer-related death worldwide, accounting for more than 1.5 million deaths in 2012. Non–small-cell lung cancers represent approximately 85% of lung neoplasms; among these, squamous cell carcinomas (SCC) account for approximately 30% of cases. The
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br Role of cysLT signaling on various
2020-08-12
Role of cysLT signaling on various neurological complications which are associated with Alzheimer’s disease Alzheimer’s disease, first described in 1906 by Alois Alzheimer, is a neurodegenerative disease and a very common cause of dementia progressively leading to death. Even though years of rese
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The substitution of serine by an
2020-08-12
The substitution of serine 185 by an alanine led to an increase of EGF-R stabilization along with a better binding of PRK1, a RhoB effector described to be involved in EGF-R intracellular traffic. Overall these data indicated that the phosphate group on serine 185 impaired its binding to the effecto
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Further modifications on the position of compound
2020-08-12
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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br Acknowledgements br Introduction Endothelial cells consti
2020-08-12
Acknowledgements Introduction Endothelial BIBW2992 receptor constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile rol
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br Are incretins the only mediators of the anti
2020-08-11
Are incretins the only mediators of the anti-hyperglycaemic effects of DPP-4 inhibitors? Even though both GLP-1 and GIP were identified as substrates for DPP-4 early on [17], [19], [20], [22], and DPP-4 inhibition in vivo raises levels of the intact endogenous forms of both of them [43], [44], fr
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The performance of the qCPA approaches
2020-08-11
The performance of the qCPA approaches is similar with regards to the derivative properties of CO2 and for mixtures of CO2+self-associating compounds. For CO2+n-alkanes the four-parameter versions of qCPA both perform somewhat better than the three-parameter version. Nevertheless this modest improve
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The P H activity and the large number of
2020-08-11
The P4H activity and the large number of 4-Hyp residues that are formed, amounting to half of all the Pro residues or 10% of all residues, have been identified as having a clear role in the structure and chemistry of the triple helix [3]. The role of the rare 3-Hyp residues is less clear and is stil
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br Materials and methods br Results and discussion
2020-08-11
Materials and methods Results and discussion Conclusions Acknowledgments This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korean government (MEST) (No. 2011-0030635) and the MarineBio Research Program (NRF-C1ABA001-2011-0018561). The Fonta
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Spinal cord injury leads to an extensive inflammatory
2020-08-11
Spinal cord injury leads to an extensive inflammatory cascade on spinal cord and the release of pro-inflammatory cytokines can sensitize neurons, activating signaling pathways that will result in thermal and mechanical hypersensitivity [39]. In this regard, Guo and collaborators (2014) demonstrated
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isoprenaline Many DNA repair pathways are candidates for
2020-08-10
Many DNA repair pathways are candidates for DPC repair. Nucleotide excision repair (NER) is widely involved in both bacteria and eukaryotes in removing cross-linked protein with low molecular weights (11kDa) (Ide et al., 2011). The predominant pathway chosen by isoprenaline may also depend on the t
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br Conclusions Present work comprehensively
2020-08-10
Conclusions Present work comprehensively characterizes the inhibitory activity of Yersinia enterocolitica against cysteine proteases. All tested strains, regardless of their bioserotype, genotype and the presence of virulence markers, synthesized the high-molecular-weight inhibitors of papain and
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For human health risk assessment of chemicals a default unce
2020-08-10
For human health risk assessment of chemicals, a default uncertainty factor (UF) of 3.16 is used to capture inter individual variation in toxicokinetics (Dorne and Renwick, 2005). However, the scientific background for this default UF remains unsatisfactory., Several studies have reported that a fac
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