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A cocktail approach can detect the activities of multiple CY
2021-06-02

A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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Numerous small molecule CRF receptor
2021-06-02

Numerous small molecule CRF receptor antagonists have been reported in the literature. Some representative examples are shown in . In preclinical studies (DMP696), , was found to be efficacious in preclinical behavioral models for anxiety and depression. In an open label clinical trial with (R121
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br Author contribution br Acknowledgements
2021-06-02

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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On close inspection the pattern shows large areas of
2021-06-02

On close inspection, the pattern shows large areas of very low point intensity where hardly any trees can be found. Anecdotal knowledge reveals that these regions are covered by a swamp, where the tree species is known to be very unlikely to grow, independent of local soil covariates and topography.
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In order to validate the
2021-06-02

In order to validate the ATP competitive mode of inhibition, compound 12 was selected as a representative inhibitor of this series, and the IC50 values were determined at eight different concentrations of compound 12 ranging from 0.001 to 100 μM, and repeated four times using different ATP concentra
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Introduction We have recently identified that caseinkinase C
2021-06-02

Introduction We have recently identified that caseinkinase 2 (CK2) inhibition protects white matter (WM) from ischemic injury. We focused our research on CK2 because upregulation of CK2 activity is associated with many diseases, including ischemic injury [1,[6], [7], [8]]. This review highlights an
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Assessment of DNA damage by comet assay
2021-06-02

Assessment of DNA damage by comet assay and ChEs activity has been widely used as a biomarker of genotoxicity and exposure to pesticide respectively, to measure the risk related to pesticides in the exposed population [15]. Very few studies have explored the association between DNA damage and worker
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Synthetic progestogens also known as synthetic gestagens syn
2021-06-02

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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In SLO permeabilized human sperm
2021-06-02

In SLO-permeabilized human sperm, the AR elicited by calcium, persistently active Arf6 [41] and Rab3A, 8-pCPT-2′-O-Me-cAMP [8], diacylglycerol and a non-hydrolyzable analog [35], is sensitive to the PLC blocker U73122. Furthermore, 8-pCPT-2′-O-Me-cAMP elicits a calcium signal in non-permeabilized sp
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br Materials and methods br Results br Discussion The
2021-06-02

Materials and methods Results Discussion The EP4 Oxaliplatin for PGE2 is similar to the EP1, EP2 and EP3 receptors in that they all have seven transmembrane segments and are coupled to Gα subunits of heterotrimeric G proteins, with a different Gα subunit for each receptor (Sugimoto and Nar
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Little information is available regarding the expression
2021-06-02

Little information is available regarding the expression of the different EP receptor subtypes on human monocytic cells, particularly those that are involved in downregulating cytokine production. The receptors are controlled by the respective genes for each receptor i.e. PTGER1–PTGER4 for EP1–EP4 r
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The molecular mechanisms regulating the differentiation of T
2021-06-01

The molecular mechanisms regulating the differentiation of Th1 versus Tfh hesperetin from IL-12-stimulated CD4+ T cells remain largely uncharacterized in humans. This topic has been extensively studied in mice (Weinmann, 2014), because IL-12 stimulation promotes mouse naive CD4+ T cells to express
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High concentrations of kC may also arise
2021-06-01

High concentrations of 7kC may also arise from dietary intake of processed cholesterol-rich food, likely favoring or worsening inflammatory bowel disease (IBD) [5,13]. Furthermore, IBD has been associated with a dysregulation of colonic 11β-HSD expression, exhibiting increased 11β-HSD1 and decreased
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Introduction In vitro synthetic biology has received conside
2021-06-01

Introduction In vitro synthetic biology has received considerably less attention than in vivo processes so far (Foster and Church, 2007). However, cell-free biosynthetic production is very likely to become important for many biotechnological challenges for reasons such as (energy) efficiency, syste
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CX-6258 synthesis br Conclusion The present work describes t
2021-06-01

Conclusion The present work describes the synthesis of 18 naphthoquinonolyl-1,2,3-triazole compounds based on natural product modification with antiplasmodial activity. Lapachol derivatives disclosed higher activity than the natural product. Six of these final modified lapachol 1,2,3-triazole com
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