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Knock out mice of FXR showed
2021-11-04

Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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In addition several other considerations were made for
2021-11-04

In addition, several other considerations were made for the optimization exercise. While the structural features of the endogenous ligands for long-chain fatty Cytochalasin J receptors suggest obtaining orthosteric agonists with drug-like properties may be challenging, the optimization efforts were
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Interestingly systemic circulating levels of NOx were not dr
2021-11-03

Interestingly, systemic circulating levels of NOx were not dramatically increased by treatment with isosorbide mononitrate or sodium nitrite at a dose which exerted beneficial effects on the progression of PH. In line with our results, Mathew et al. [13] demonstrated that the long-acting NO donor mo
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Importantly each conformational state in the SRP SR dimer
2021-11-03

Importantly, each conformational state in the SRP–SR dimer provides a distinct point of regulation at which these GTPases can directly sense and respond to different biological cues in the pathway. For example, assembly of a stable ‘closed’ complex between SRP and SR is intrinsically very slow (kon
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br Introduction br Mitochondrial dysfunction and cancer br
2021-11-03

Introduction Mitochondrial dysfunction and cancer Lactate and succinate as oncometabolites Intracellular actions of lactate and succinate as tumor promoters Cell-surface receptors for lactate and succinate and their role in cancer GPR109A as the receptor for butyrate and β-hydroxybu
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The combination of niacin with a selective PGD
2021-11-03

The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su
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Conjugated BAs via S PR also activate
2021-11-03

Conjugated BAs via S1PR2 also activate ERK1/2- and AKT-signaling pathways leading to the growth and invasion of cholangiocarcinoma cells. The role of conjugated BAs via S1PR2 to regulate apoptosis or cancer progression remains to be dissected. Nevertheless, there is no doubt that the composition of
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br Conclusion We conducted single marker association and hap
2021-11-03

Conclusion We conducted single-marker association and haplotype association analyses of genetic mutations in porcine SLA-DOB and CD4 genes with T-lymphocyte subsets, cytokines, and am580 in pregnant Landrace sows and obtained the SNPs and insertion that significantly affected the immunity traits
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To shed more light on the binding of benzophenanthridine
2021-11-03

To shed more light on the binding of benzophenanthridine to GlyT1, we studied how the replacement of certain residues around the sanguinarine sensitive cysteine 475 previously identified (Jursky et al., 2012) affects GlyT1 inhibition of by these alkaloids. Based on these results we propose a putativ
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Capillary monolithic columns obtained by in situ
2021-11-03

Capillary monolithic columns obtained by in situ polymerization have been developed rapidly as an efficient chromatographic stationary phase, which exhibits excellent reproducibility, reliable stability and fast transfer kinetics [18]. Recently, it has been extensively applied in capillary liquid ch
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br Introduction Given the growing acceptance of
2021-11-03

Introduction Given the growing acceptance of ergothioneine (ET) as a biologically important agent with potential therapeutic applications [[1], [2], [3], [4]] it is increasingly important to clearly establish the role of the organic cation transporter (novel) type 1 (OCTN1). OCTN1 was discovered
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Ghrelin contains an n octanoylation at its
2021-11-03

Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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In the course of an internal
2021-11-03

In the course of an internal FAAH, program,, , , , , , , , , , , , , many very similar compounds were profiled in vivo with particular interest paid to their ability to penetrate the BBB. The compounds profiled were heteroaryl piperazinyl and piperadinyl ureas; a class of compounds, reported on pr
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Enhancer of Zeste Homolog EZH is a core component
2021-11-03

Enhancer of Zeste Homolog 2 (EZH2) is a core component of the Polycomb Repressive Complex2 (PRC2) which also includes SUZ12 and EED. PRC2 represses gene transcription through trimethylation of Lys27 of histone H3 (H3K27), and contribute to the maintenance of cell identity, Gefitinib regulation and o
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In our study we found that
2021-11-02

In our study, we found that HER2-mutant lung cancers occurred commonly in female patients with an advanced stage at time of diagnosis and in a relatively younger age group. Previously, Mazières et al. [8] obtained comparable epidemiological findings, including a median age of 60 years, a high propor
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