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KNK437 The inhibition of CYP activity
2019-07-12

The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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Khan et al investigatedAnomalin a pyranocoumarin
2019-07-11

Khan et al. investigatedAnomalin 44, a pyranocoumarin constituent of S. divaricata, which exhibits potent anti-inflammatory activity. The anomalin 44 dose-dependently inhibited inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) mRNA and protein expression in LPS-stimulated RAW 264.7
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Yet the standards fall back on the development process with
2019-07-11

Yet, the standards fall back on the development process with justification. As shown by Littlewood and Strigini (1993), the extent to which the reliability of software (both OTS and bespoke) can be proved by testing is severely limited––not because appropriate tests cannot be devised, but because a
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It has been reported that cAMP also acts via Epac
2019-07-11

It has been reported that cAMP also acts via Epac and Epac to attenuate CREB. However, in human monocytes ONO-AE1-329 (the EP4 receptor agonist used in this study) worked entirely through the cAMP-PKA pathway and not vis Epac [12]. Our data suggests that the cAMP-PKA-CREB pathway predominates for MU
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br Early developments Historically the advent of
2019-07-11

Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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In summary this is the first report describing the
2019-07-11

In summary, this is the first report describing the enzymatic characteristics, binding activity and localization of T. solium enolase. Here we demonstrate that Tseno gene possesses classical features of enolase family with highly conserved active sites, Mg2+ binding and plasminogen-binding motifs. T
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br Competing interests br Acknowledgments This work was
2019-07-11

Competing interests Acknowledgments This work was supported by grants from Fujian Fujian Provincial Natural Science Foundation (2016J01612). Introduction Cancer is still one of the most serious diseases in the world. According to the World Health Organization (WHO), cancer is the second mo
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As mentioned above EBI and its ligand show some similarities
2019-07-11

As mentioned above, EBI2 and its ligand show some similarities to the sphingosine 1-phosphate (S1P)/S1P-receptor system, which mediates T cell egress from lymph nodes. Blockade of this system yielded in the first oral drug for MS patients named fingolimod. Therefore, the hope that EBI2 deficiency wo
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In this context we initiated a
2019-07-11

In this context, we initiated a program to develop new antiviral chemotypes towards a host factor implicated in Paxilline replication: the host (human) dihydrofolate reductase (DHFR) [21]. We recently identified this enzyme as the molecular target of 1-aryl-4,6-diamino-1,2-dihydrotriazines, structu
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br Introduction The dopaminergic system and its projections
2019-07-11

Introduction The dopaminergic system and its projections including both the prefrontal bcr-abl inhibitor (PFC) and striatum are known as being crucial to synaptic plasticity, skill acquisition and higher order functions (e.g., working memory and cognitive control; Matsumoto et al., 2003). Variat
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br Menopausal hormone therapy from the
2019-07-11

Menopausal hormone therapy, from the beginning to WHI Estrogen products have been used since the 1940s, with increasing prescription through the 1960s. First concerns appeared in the 1970s when oral treatment was linked to uterine cancer. Oral estrogens have traditionally been coupled with proges
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A limitation of this study is the
2019-07-11

A limitation of this study is the between-study heterogeneity of the datasets analyzed. To address this heterogeneity, we used a random-effects model in our analysis. Also, only 2 of the databases provided information on sex, and as a result, the sex-specific analyses were performed with a smaller c
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It is now well accepted
2019-07-11

It is now well accepted that increased local estrogen levels are associated with both the onset and growth of breast cancer. Tissue concentrations of estradiol (E2) in breast cancer are 10 times higher than that found in plasma [12]. Breast cancer tissues also contain increased activity and expressi
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br In order to determine the physiological roles
2019-07-11

In order to determine the physiological roles of WT (wild type) EWSR1, Dr. Lee\'s group established a conventional Ewsr1 KO mouse [38]. Since then, the Ewsr1 KO (−/−) mouse model has successfully been utilized to decipher many important in vivo roles of EWSR1 (Fig. 1). EWSR1 deficiency alters m
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Biocytin The growth inhibitory effect of PGE has
2019-07-11

The growth inhibitory effect of PGE2 has been linked to the ability of Gs coupled PGE2 receptors EP2 and EP4 to mediate elevation of cAMP [22], [23]. Evidence suggests that this mechanism may not be the key cause of growth inhibition [24]. In various cell types, EP4 receptor has been shown to utiliz
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