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To investigate the potential molecular mechanism of
2021-12-21

To investigate the potential molecular mechanism of FXR-mediated regulation of liver cancer cell proliferation, gene expression profiles were determined using Agilent arrays in SK-Hep-1-FXR and NC after treatment with the FXR agonist GW4064. The results indicate that mTOR and S6k are involved in div
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Lenvatinib is an orally available multi targeted
2021-12-21

Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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br FREE FATTY ACID RECEPTOR
2021-12-21

FREE FATTY ACID RECEPTOR 1 (GPR40) G-PROTEIN-COUPLED RECEPTOR 120 CONCLUSION Free fatty N6022 receptors whose natural ligands are identified as FFAs having various lengths have been reported. They act as novel nutrient sensing receptors independent of PPARs and FABPs, and they are known to
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Attractively existing reports suggest that cellular ferropto
2021-12-21

Attractively, existing reports suggest that cellular ferroptosis also probably plays vital role in liver fibrosis [[62], [63], [64]]. Carlson BA et al. illuminated that the ferroptosis regulator GPX4 was important for hepatocyte survival and proper liver function [62]. Sun X et al. showed that Nrf2
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br Place in Therapy In the case of
2021-12-21

Place in Therapy In the case of minor bleeding, the anticoagulant effects of all FXa inhibitors except betrixaban, which has a longer half-life, will diminish within 24-48 hours of discontinuation of the drug provided the patient has normal renal function. In these cases stopping the FXa inhibito
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In addition to acting as the gatekeeper for
2021-12-20

In addition to acting as the gatekeeper for the metabolic and antioxidant roles of glucose, HKs have also been found to regulate mPTP opening directly. First described in the cancer field, the high-affinity HK isoforms HK1 and HK2 are strongly anti-apoptotic when bound to the outer mitochondrial mem
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Unfortunately the approved drugs suffer from failure in many
2021-12-20

Unfortunately, the approved drugs suffer from failure in many cases [5,6]. Several mutations occur in the binding site of NS3/4A protease, which affect drug binding and cause drug resistance [13]. It is a big challenge and needs more efforts to be done. This is the reason why research is still conce
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Acute in vivo experiments were performed in normoglycemic
2021-12-20

Acute in vivo experiments were performed in normoglycemic 129SVE mice to confirm GPR119 activation and corresponding Remoxipride hydrochloride control. GIP release was utilized as a biomarker for target receptor engagement and plasma GIP levels were measured 45min after oral dosing (). Both 3 and 1
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Because of its excellent GPR potency
2021-12-20

Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Imiloxan hydrochloride was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extens
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(-)-Lobeline hydrochloride The combination of niacin with a
2021-12-20

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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5-Formyl-UTP receptor Several studies have shown that regula
2021-12-20

Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upregu
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Apoptosis a form of programmed cell
2021-12-20

Apoptosis, a form of programmed cell death, is a critical component in maintaining homeostasis and growth in all tissues and plays a significant role in immunity and cytotoxicity [54,55]. Although GR are expressed in all immune cells, the physiological outcomes of GR activation are highly cell type-
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Next we investigated the transfer of
2021-12-20

Next, we investigated the transfer of peptides and proteins between contacting cells by nano-LC-MS/MS analysis using the fractions corresponding to molecules higher than 3 kDa. The MS data analysis revealed the direct transfer of several labelled peptides between receivers and donors. Labelled pepti
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OCA has recently been approved for
2021-12-20

OCA has recently been approved for the treatment of patients with PBC and is under study for diseases such as NASH, PSC and biliary atresia [30], [49]. Up to now, the beneficial effects of OCA have been related to its anti-cholestatic, anti-inflammatory and anti-fibrotic properties. We have here rep
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br Melanoma cell lines There is suggestive epidemiological e
2021-12-20

Melanoma cell lines There is suggestive epidemiological evidence that omega-3 PUFA can be preventative against melanoma, although the mechanisms of this relationship has not been extensively investigated [65], [66]. A 2014 study demonstrated that DHA inhibited cell proliferation in vitro in A2058
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