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Another important new result that has
2019-11-11
Another important new result that has expanded the range of functions of iPLA2-VIA in physiology and pathophysiology is its implication in macrophage polarization under stimulation conditions. Ashley et al. [129] described in peritoneal macrophages from Pla2g6−/− mice that the absence of iPLA2-VIA f
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It is believed that emphysema in smokers is mediated
2019-11-11
It is believed that emphysema in smokers is mediated by proteases released from inflammatory chloride channels that cause destruction of the extracellular matrix in alveolar septa [1]. Metalloprotease-12 is mainly released by macrophages and is considered the enzyme responsible for emphysematous les
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Pursuant to our in vitro
2019-11-11
Pursuant to our in vitro data that neutrophilic elastase activated the elastase-dependent oncolytic virus, we initially hypothesized that tumor-infiltrating neutrophils could be the source for elastase in tumor tissue. However, we did not detect neutrophils in the PANC-1 tumor tissue where we observ
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br Patients and Methods Patients who had been
2019-11-11
Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl)
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apelin receptor Testosterone is inactivated through hydroxyl
2019-11-11
Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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The in vitro cytotoxicity of the prodrugs was assessed in
2019-11-11
The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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br Materials and methods br Results br Discussion We initial
2019-11-11
Materials and methods Results Discussion We initially found that ISL, a natural product with a linear scaffold (2-propenone), is able to inhibit CK2 (IC50 = 17.3 μM). Then we have investigated the inhibitory potential of a novel series of compounds with linear scaffolds by combining fragmen
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In summary synthetic routes with moderate to
2019-11-11
In summary, synthetic routes with moderate to high yields have been developed to produce difluoro-dioxolo-benzoimidazol-benzamides including reference standards and , and -desmethylated precursors and , and carbon-11-labeled difluoro-dioxolo-benzoimidazol-benzamides target tracers [C] and [C]. The
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To further verify the effect of BBR on
2019-11-11
To further verify the effect of BBR on ACAT2 protein expression, we have conducted an in vitro permeability assay using Caco-2 monolayer. This assay has long been used to predict the in vivo porcn and bioavailability of a compound. It was observed that the amount of cholesterol esters in the medium
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The isomeric phenyloxazole not only exhibited
2019-11-11
The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand VU 0155069 (as seen in compound pairs – and –) decreased AC
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Boulares group has demonstrated that the NF B p
2019-11-08
Boulares group [82] has demonstrated that the NF-κB1/p50 NF-κB, a family member of type I NF-κB, is an excellent substrate for DNA-PK, which-dependent phosphorylation of NF-κB1 at serine 20 appears to enhance its binding to DNA as either a homodimer or a heterodimer with p65 NF-κB and the ability of
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br Acknowledgments Grant support was provided by the Leading
2019-11-08
Acknowledgments Grant support was provided by the Leading Academic Discipline Projects of Shanghai Municipal Education Commission (J5028) (J50201) to Dr. Mi, the China National Science Foundation Project (81072076) to Dr. Mi, the China National Science Foundation Project (31000349) to Dr. Shen, a
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minocycline hydrochloride As a functional ETC is required fo
2019-11-08
As a functional ETC is required for DHODH catalysis (Loffler, Jockel, Schuster, & Becker, 1997; Rawls, Knecht, Diekert, Lill, & Loffler, 2000; Zameitat, Freymark, Dietz, Loffler, & Bolker, 2007), DHODH depends on the mitochondrial ETC to generate adequate concentrations of ubiquinone (Fig. 2). Cells
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In order to assess quantitatively the contribution
2019-11-08
In order to assess quantitatively the contribution of the ung, dug and dut u0126 to uracil-DNA accumulation in E. coli, we have developed a novel method for measuring uracil residues in DNA that is based on the approach of Kow and co-workers [33] for measuring AP-sites in DNA. The method, which we
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In summary in the present study we found that CysLT
2019-11-08
In summary, in the present study we found that CysLT1 receptor attenuates while CysLT2 receptor facilitates OGD-induced PC12 cell death as confirmed by receptor over-expression and antagonism. However, we cannot explain why their roles are distinct and why the cell size is increased in the CysLT2 re
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