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The endothelin receptor type B EDNRB belongs to
2020-05-19
The endothelin receptor type B (EDNRB) belongs to the family of G protein-coupled receptors, which functions as a vital regulatory factor in signal transduction in cells, locating on human chromosome 13q22.3 (Ayala-Valdovinos et al., 2016; Bregar et al., 2018; Morimoto et al., 2018; Widowati et al.,
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In some cases more than one CYP enzyme may
2020-05-19
In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple p-Cresyl sulfate (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape to determin
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Considering these reports and with
2020-05-18
Considering these reports, and with the aim of further investigating the mechanism by which the cAMP-Epac/PKA pathway activates eNOS, we have performed imaging experiments evaluating the effect of drugs that increase cAMP or modify its signalling pathways (PKA or Epac activators and inhibitors) on b
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To understand the behavior of
2020-05-18
To understand the behavior of enzymes in ILs at a molecular level, it is first desirable to dissolve enzymes in the solvents. For soluble catalysts, there are many relatively simple spectroscopic and other techniques for obtaining accurate information at a molecular level. Parker et al. [9] reported
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br Acknowledgements br Introduction In Arabidopsis thaliana
2020-05-18
Acknowledgements Introduction In Arabidopsis thaliana (L.) Heynh, there are at least four copies of the caseine kinase-like gene Ck1, which is involved in peptide phosphorylation in mammals [1]. These genes are distributed on dig this 1, 2, 4, and 5. A similar number of copies for Ck1 have be
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Recently roflumilast has been approved as the first selectiv
2020-05-16
Recently, roflumilast has been approved as the first selective PDE4 inhibitor for the treatment of chronic obstructive pulmonary disease (COPD) [2]. Roflumilast has been suggested to target several different pathogenetic mechanisms, including inflammation, fibrotic, emphysematous and vascular remode
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The nitrophenols b d were prepared
2020-05-16
The nitrophenols 34b–d were prepared as described in Scheme 3b. Nitration of phenols 39b–d with 1equiv of sodium nitrate in the presence of hydrochloric Safingol gave an inseparable mixture of 34b–d and 40b–d (1:1). This synthetic problem was successfully avoided as described below. Nitration of 39b
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It is noteworthy that little is known as
2020-05-16
It is noteworthy that little is known as to the role of autophagy in regulation of eNOS phosphorylation and eNOS uncoupling. eNOS monomers, but not eNOS dimers could be degraded by ubiquitination [39], harbingering the existence of protein degradation pathways in modulation of eNOS turnover and acti
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Aminothiazole derivatives have been reported
2020-05-16
2-Aminothiazole derivatives have been reported to contain antiviral [17], anti-inflammatory [18], and antimicrobial [19] activities. The in vitro anticancer studies showed that different 2-aminothiazole derivatives possess selective and potent inhibitory effect against wide-ranging human cancerous c
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In general cellular senescence is considered a programmed
2020-05-16
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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Possibly there are similarities among euphorb plant species
2020-05-16
Possibly there are similarities among euphorb plant species but extraction of the rgd peptide present in the microsomal fraction is needed for testing their preferences for substrates. Although R. communis, E. lathyris and E. lagascae belong to the same family, the DGAT activity of their microsomal
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Previous studies showed that many steroidogenic enzymes act
2020-05-16
Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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br Conclusion The results of the present
2020-05-16
Conclusion The results of the present study demonstrate that cysteinyl leukotrienes LTC4, LTD4 and LTE4 cause moderate to marked whereas the dihydroxy leukotriene LTB4 causes small muscle contraction in the stomach in vitro. The LTD4-induced contraction is mediated by CysLT1 in fundus but by CysL
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Almost of drugs in the market undergo
2020-05-16
Almost 75% of drugs in the market undergo deactivation though oxidation, reduction or hydrolysis by cytochrome P450 (CYP) enzymes, and then, either directly or by facilitated excretion from the body (Guengerich, 2008). The CYP3A subfamily is of particular interest because of its broad substrate spec
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br Introduction The dorsal periaqueductal gray matter dPAG
2020-05-15
Introduction The dorsal periaqueductal gray matter (dPAG) is a midbrain site markedly involved in fear/anxiety-evoked responses as well as in nociception (see, for example, Bandler and Carrive, 1988, Deakin and Graeff, 1991, Fardin et al., 1984a, Fardin et al., 1984b, Litvin et al., 2007). Chemic
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