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We neither observed changes in
2021-06-24

We neither observed changes in midazolam eCLmet indicative of significant inhibition of CYP3A4/5 during both experiments, despite the in vitro evidence for CYP3A4/5 inhibition (Theile et al., 2017). The observed increase in CYP3A dependent midazolam clearance after chronic ingestion of clementines/c
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For in vitro expression analysis of CXCL and
2021-06-24

For in vitro expression analysis of CXCL8 and CXCRs by stimulated leucocytes, peripheral blood leucocytes (PBLs) were isolated using Percoll density gradient centrifugation as described earlier . Cell suspensions were adjusted to 5×10/ml. Four milliliters of tissue culture medium were plated per wel
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br Methods Adult male B CRHtklee
2021-06-24

Methods Adult male B6, 129 CRHtklee mice (25–30g at the beginning of the experiments) that were wild-type (CRF1R+/+) and recessive homozygous or knockout (CRF1R−/−) were housed six per cage. Mice were 3–5months old and derived from mating CRF1R+/− breeders (Jackson Laboratory, California). Wild-t
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In order to further evaluate cpt a
2021-06-24

In order to further evaluate cpt1a function, we determined its tissue distribution in large yellow croaker. The mRNA levels of cpt1a were detected in all the tested tissues, but at varying levels. cpt1a mRNA expression was the highest in liver among different tissues, similar to reports in other fis
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BIIE 0246 receptor Next our exploration shifted to modificat
2021-06-24

Next, our exploration shifted to modifications at the lateral chain of the benzoquinone nucleus (SAR 2). Considering that the CK2 inhibitory activity is favoured by the presence of the -Ph-4-NO2 (SAR 1), the subsequent analogues were investigated with this moiety retained. The influence of the side
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Activating GSK signaling to inhibit PK signaling during
2021-06-24

Activating GSK3β signaling to inhibit PK signaling during ischemia/reperfusion (I/R) is protective of WM ischemic injury. Glycogen synthase kinase (GSK3), which was the first substrate identified for AKT [44], is inhibited by AKT phosphorylation at positions S9 and S21 [45]. When GSK3β is active, it
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The phenolic hydroxyl group of ezetimibe tolerated various
2021-06-24

The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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In this study we also
2021-06-24

In this study, we also conducted an analysis comparing the expression profiling of Hh genes among the sarcomas investigated. In these tumors, the IHH gene showed a higher expression level than PTCH1 gene in RMS and SS samples (pbetulinic citco mg in human RMS cell lines as well as mouse NIH-3T3 fib
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Only a few studies have examined the effect of prostanoids
2021-06-24

Only a few studies have examined the effect of prostanoids on cardiac fibroblasts. Therefore, this study examines the effect of PGE2 on cardiac fibroblast proliferation and tests the hypothesis that PGE2 causes cardiac fibroblast proliferation via alterations of calcitonin gene related peptide regul
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I bungarotoxin competes with ACh
2021-06-24

[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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Introduction Obesity constitutes a global healthcare problem
2021-06-24

Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV
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br Materials and methods br Results
2021-06-24

Materials and methods Results Discussion Chronic inflammation is central to COPD and plays a critical role in the disease pathogenesis and progression. Among the various inflammatory cells, neutrophils are the key players in COPD pathogenesis. Their numbers are raised in airspaces and lung
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The attachment of ubiquitin to RTKs
2021-06-24

The attachment of ubiquitin to RTKs, such as EGFR, mediates efficient delivery through the endosome-lysosome system for proteolysis. In this way, RTK degradation enables cessation of signal transduction. A recent siRNA screen identified a number of USPs that can significantly modulate EGFR levels an
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While oxysterols were most extensively studied
2021-06-24

While oxysterols were most extensively studied for its potent ability to mediate feedback regulation of cholesterol biosynthesis, some early investigations showed that the enzymes involved in its syntheses were highly upregulated in macrophages and dendritic cells—an indication of possible roles in
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br Material and methods br Results br Discussion
2021-06-23

Material and methods Results Discussion In vitro evidence indicates that LAS191859 is a potent CRTh2 antagonist as demonstrated in GTPγS binding studies with potency in the low nanomolar range and in addition it demonstrates a long receptor residence time. This potency is also maintained in
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