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Finally considering the encouraging inhibitory and selectivi
2021-03-12

Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of exp
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Currently phosphodiesterase type PDE inhibitors are
2021-03-12

Currently, phosphodiesterase type 5 (PDE-5) inhibitors are used widely as the first- line oral treatment for erectile dysfunction of varying causes. Radical prostatectomy for the treatment of prostate cancer is frequently associated with erectile dysfunction, and this type of erectile dysfunction is
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The ESC update emphasizes the need for implementing strategi
2021-03-12

The 2017 ESC update emphasizes the need for implementing strategies to minimize PCI-related complications, including risk stratification for ischemia and bleeding, keeping triple antithrombotic therapy to the shortest possible duration with dual antithrombotic therapy as an alternative, using non–vi
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br Materials and Methods br Results br Discussion
2021-03-12

Materials and Methods Results Discussion Viral infection of eukaryotic Tirapazamine activate signaling pathways both via specific interaction with pattern recognition receptors (TLRs, RIG-I, MDA5) and more nonspecific mechanisms such as accumulation of newly synthesized viral glycoproteins
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It was reported that the expressions of
2021-03-12

It was reported that the expressions of DPP-4 and SDF-1α increase through HIF-1α [27], [28]. Myocardial ischemia by MI enhanced the DPP-4 and SDF-1α levels in myocardium in the present study. SDF-1α is released from cardiomyocytes and has beneficial effects on cardiomyocytes through SDF-1α/CXCR4 aft
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For a physiologically relevant interaction ligand and recept
2021-03-12

For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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In addition to an action via
2021-03-11

In addition to an action via P2Y receptors, extracellular UDP activates GPCRs for cysteinyl leukotrienes (CysLT1, CysLT2; Mellor et al., 2001, 2003). GPR17 has been reported to function as a receptor for cysteinyl leukotrienes and uracil nucleotides (Boda et al., 2011; Fumagalli et al., 2011; but se
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br Conclusions Enzyme can be delivered to the tumour by
2021-03-11

Conclusions Enzyme can be delivered to the tumour by using humanised or fully human L-Carnitine inner salt or even loaded into synthetic nanospheres produced from silica [64] or liposomally entrapped [65]. For any future ADEPT developments, a number of basic points need to be considered. As immu
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The strong adsorption of amines to the stationary phase of
2021-03-11

The strong adsorption of amines to the stationary phase of gas chromatography (GC) columns causes issues such as tailing, ghosting and low reproducibility [12], [13]. A common practice to overcome this problem is the chemical derivatisation of amines prior to GC analysis [14]. Comprehensive reviews
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The intestinal cholesterol absorption markers sitosterol and
2021-03-11

The intestinal cholesterol rsv virus markers sitosterol and campesterol to cholesterol levels were significantly lower in Villin-Tgif1 mice compared to wild type mice, irrespective of diet. However, the decrease was less pronounced in Villin-Tgif1 mice fed a chow diet (∼20–30%) compared to mice fed
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By using live imaging of an ERK fluorescence resonance
2021-03-11

By using live imaging of an ERK fluorescence resonance energy transfer (FRET) sensor, the authors show that ERK activity propagates in a stepwise manner from the center to the periphery of the tracheal placode. This row-by-row propagation of ERK activity fits a relay model in which each row activate
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br Conclusion Our study demonstrates that the
2021-03-11

Conclusion Our study demonstrates that the effects of Epac activation are strongly conditioned by the steady-state Ca levels at which the myocyte is functioning. As intracellular Ca increases, the activity of CaMKII enhances and the phosphorylation of its SR substrates acquires different relevanc
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sgk inhibitor I bungarotoxin competes with ACh an endogenous
2021-03-11

[125I] α-bungarotoxin competes with ACh, an endogenous activator of α7-nACh receptors by binding to the ACh binding site on the receptor (Albuquerque et al., 2009). For this reason, the effect of curcumin was investigated on the specific binding of [125I] α-bungarotoxin. Saturation curves for the bi
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br Oxidoreductase like MEM for prodrug activation
2021-03-11

Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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The enantiomeric ratio ER of chiral compounds accumulated
2021-03-11

The enantiomeric ratio (ER) of chiral compounds accumulated in organisms has been found to be different among species (Borga and Bidleman, 2005, Harner et al., 1999, Warner et al., 2005, Wiberg et al., 2000), indicating enantioselective accumulation of chiral compounds are species-specific. The ER o
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