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Synthetic progestogens also known as synthetic gestagens syn
2020-03-06

Synthetic progestogens (also known as ‘synthetic gestagens’, ‘synthetic progestins’ or simply ‘progestins’) are designed to mimic the effects of progesterone (P4) and are the active pharmaceutical ingredient in many contraceptives and hormone replacement therapies. Since most progestins are derived
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Table summarizes the literature data available on the occurr
2020-03-06

Table 4 summarizes the literature data available on the occurrence of these two bioactive of steroidal compounds in sludge and sediments. In activated and digested sewage sludge, the concentrations of ethynyl estradiol (17 ng/g), estrone (37 ng/g ), and estradiol (49 ng/g) found in one of the very
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In normal cells the apoptotic stimuli lower the expression
2020-03-06

In normal cells, the apoptotic stimuli lower the expression level of antiapoptotic proteins by increasing turnover rate and preventing the constant degradation of proapoptotic proteins. Thus, the dysregulation of anti-/pro-apoptotic proteins will confer the survival of cancer PF-3845 via enhancing
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Here we investigate in more detail how
2020-03-06

Here we investigate in more detail how Dot1 function contributes to the regulation of DNA damage tolerance. We find that Dot1 modulates the response to the alkylating agent MMS through its catalytic activity on H3K79. In fact, progressively reduced levels of H3K79 tri-methylation result in gradually
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br Introduction Plasmodium falciparum malaria continues to
2020-03-06

Introduction Plasmodium falciparum malaria continues to be a major global cause of mortality and morbidity. Malaria treatment and control has been complicated by the emergence of resistance to widespread antimalarial drug use. The most common method for measuring antimalarial resistance is estima
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As previously reported azole class antifungal drugs
2020-03-06

As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le
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Nile tilapia Oreochromis niloticus is
2020-03-06

Nile tilapia (Oreochromis niloticus) is an important species farmed worldwide (Doan et al., 2018). Lipid-rich diets are commonly used in Nile tilapia aquaculture to reduce feed cost, but impair lipid homeostasis (Huang et al., 2016). Therefore, it is important to determine whether forskolin can stim
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It has been shown that CK phosphorylates and tubulin in
2020-03-06

It has been shown that CK1δ phosphorylates α-, β- and γ-tubulin in vitro and that CK1δ specifically interacts with the trans Golgi network, COPI positive vesicles, and centrosomes in interphase cells [11], [12], [13], [14]. Moreover CK1δ is also associated with granular particles that are associated
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Another layer of CK regulation in the
2020-03-06

Another layer of CK1 regulation in the Hh and Wnt pathways is to employ different CK1 isoforms to phosphorylate distinct pathway components or even distinct sites on the same substrates. In this regard, it has been shown recently that the membrane-associated CK1 isoform CK1γ, but not the cytosolic i
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br Introduction Fibroblast growth factors FGF are a
2020-03-06

Introduction Fibroblast growth factors (FGF) are a family of 18 secreted ligands that bind to four receptor tyrosine kinase (RTK) FGF receptors (FGFR1–4). The interaction of FGFs with their cognate receptors results in the activation of a number of downstream signaling pathways, including the MAP
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br EphB as a therapeutic target in
2020-03-06

EphB4 as a therapeutic target in cancer Eph receptors and ephrins are promising new therapeutic targets in cancer. Various strategies have been employed to evaluate the interference of tumor-promoting effects or the enhancement of tumor suppressive effects. The inhibition of the Eph-ephrin system
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Molecular docking study of compound was performed using the
2020-03-06

Molecular docking study of Azidobutyric acid NHS ester was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg44
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br Perspective and conclusion Collagen Toolkits II
2020-03-05

Perspective and conclusion Collagen Toolkits II and III have been used to determine the TNF-alpha, recombinant murine protein for DDR1 and DDR2, and the main binding site is the GVM-GFO motif [103,108]. The co-crystal structure of the DS domain of human DDR2 bound to a synthetic collagen-like pe
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br Conflicts of interest br Financial support NZ is
2020-03-05

Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818
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In vivo study showed that the CYP
2020-03-05

In vivo study showed that the CYP3A activity was increased, when morroniside (10, 30 and 90 mg/kg, i.g.) was daily for seven consecutive days. Further, RT-PCR analysis showed that the induction of mRNA Dimethyl Fumarate by morroniside (10, 30 and 90 mg/kg, i.g.) was 1.13-, 1.43- and 1.79-fold higher
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