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Recently a sandwich cultured hepatocyte
2020-11-17
Recently, a sandwich-cultured hepatocyte model has been proved to be a valuable in vitro system that maintains specific hepatic cytomorphology and function relevant to drug metabolism, disposition and toxicity, and thus, closely resembles the in vivo setting. This hepatocyte model was recognized as
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Introduction Cytochrome P CYP A
2020-11-17
Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The JLK 6 level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response and toxicity. A multi
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Deregulated Wnt signaling either due
2020-11-17
Deregulated Wnt signaling, either due to pathway mutations or otherwise aberrant pathway activity, is common in CLL [81], [82]. In addition to targets described above, alvocidib also inhibits glycogen synthase kinase 3 (GSK3)-β at higher nanomolar concentrations [37]. Despite intuition and experimen
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br Prostaglandin D PGD is derived from the
2020-11-17
Prostaglandin D (PGD) is derived from the metabolism of arachidonic jw products by cyclooxygenases and downstream PGD synthases. In the immune system, PGD is mainly produced by mast cells but also although at lower levels, by macrophages and Th2 lymphocytes. PGD binds to three different receptors
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PyBOP br Author contribution br Acknowledgements QNRF grant
2020-11-17
Author contribution Acknowledgements QNRF grant number NPRP6-065-3-012, Qatar National Research Fund, Doha Qatar for funding this work with grant number NPRP No.: NPRP6-065-3-012. Introduction Preeclampsia (PE) affects 3–5 % of pregnancies worldwide and is one of the leading causes of mate
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COMT protein expression was investigated as a
2020-11-17
COMT protein isethionate was investigated as a potential mechanism by which tolcapone may differentially affect male and female P and Wistar rats. COMT protein levels in the PFC were lower in P rats compared to Wistars but female P rats expressed greater levels of COMT in the PFC relative to males.
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Phenylbenzofurans are a very important molecule skeleton
2020-11-17
Phenylbenzofurans are a very important molecule skeleton due to their synthetic versatility and their proved pharmacological properties [2]. They are synthetic compounds in which an additional phenyl ring is present in any position of the benzofuran nucleus. This could be easily obtained possible by
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Besides having a remarkable progestogenic effect an
2020-11-17
Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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The selective estrogen receptor modulators
2020-11-17
The selective estrogen receptor modulators (SERMs) are another type of estrogen receptor ligands. The main difference between SERMs and xenoestrogens relies on the fact that SERMs present functional duality and are able to act both as agonists and antagonists of the estrogen receptors in different t
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It has previously been shown that
2020-11-17
It has previously been shown that human melanocytes are responsive to a multiplicity of hormonal triggers [10], particularly to pituitary or ovarian hormones [11]. Studies concerning the effects of Cl-Amidine trifluoroacetate salt on human melanocytes led to inconsistent data [12], [13]. Im et al.
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The role of Epac in the
2020-11-17
The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e
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In mammals neutrophil elastase is a
2020-11-16
In mammals, neutrophil elastase is a trypsin-like serine protease stored in the azurophilic granules of naïve neutrophils [15], [16]. The catalytic activity of neutrophil elastase relies on a His57–Asp102–Ser195 triad (chymotrypsin numbering system) that functions by transfer of electrons from the c
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Cyclosporine NEORAL Oral Solution Novartis is an
2020-11-16
Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na
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Immunomodulation effects of certain oxysterols were previous
2020-11-16
Immunomodulation effects of certain oxysterols were previously shown to depend on activation of oxysterol-binding liver X receptors (LXRs). Recent work from our labs as well as from others has shown additional receptors linking oxysterols and immunity. For example, we found that 7α,25-dihydroxychole
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Generally glycines and other small residues such as alanine
2020-11-16
Generally, glycines (and other small residues such as alanine) present in a helical GxxxG-motif that are facing the same side of the helix form a uniform surface that enables direct contact with a second helix. Crystal structures of multipass membrane proteins have demonstrated that GxxxG-motifs are
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