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In conclusion this is the first description
2022-10-12

In conclusion, this is the first description of a GPR81 agonist with an ability to exert in vivo efficacy without causing flushing. These results demonstrate that GPR81 small-molecule agonists may be effective for treating dyslipidemia. In addition, targeting GPR81 could prevent the unwanted side ef
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To characterize the binding receptor for HIV gp in
2022-10-12

To characterize the binding receptor for HIV-1 gp120 in autophagy, we used the CXCR4 inhibitor AMD3100 and NMDA receptor inhibitor MK801 along with gp120 to treat the cardiomyocytes. Our data demonstrated that inhibition of the NMDA receptor significantly blocked the increase of gp120 induced autoph
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Capillary monolithic columns obtained by in situ polymerizat
2022-10-12

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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Next we investigated the accumulation of H ribavirin
2022-10-12

Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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Previous studies have suggested that GPR protects from bone
2022-10-12

Previous studies have suggested that GPR40 protects from bone loss via inhibition of osteoclasts. Wittrant et al. used GPR40 knock-out mice and primary osteoclasts to investigate the role of GPR40 on bone remodelling. Their results in primary osteoclast cultures and the RAW264.7 cell line showed tha
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dmh express receptor br Materials and methods br Results Ana
2022-10-12

Materials and methods Results Analysis of the post-mortem human prefrontal cortex by western blotting indicated that GLAST expression was increased 1.6-fold in the extracts of alcoholic brains relative to controls (Fig. 1A and B). To resolve the distinct sub-pools of GLAST within our samples w
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Methoxyflavone and methoxyflavanone Fig both
2022-10-11

6-Methoxyflavone and 6-methoxyflavanone (Fig. 2) both act as flumazenil-insensitive positive allosteric modulators of GABA responses at human recombinant α1β2γ2L and α2β2γ2L GABAA receptors. However, unlike 6-methoxyflavone, 6-methoxyflavanone was relatively inactive at α1β2 GABAA receptors. Both fl
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To improve the performance of
2022-10-11

To improve the performance of the immunoassay, various nanomaterials including carbon nanospheres [9], gold nanoparticles [10] and transition metal compounds [11] were used to immobilize natural enzymes as the label. Natural enzymes, such as horseradish peroxidase (HRP) [12] and glucose oxidase (GOD
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In terms of cytotoxicity studies under two dimensional cell
2022-10-11

In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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DAMPs are endogenous danger signals
2022-10-11

DAMPs are endogenous danger signals that can initiate and perpetuate a noninfectious β-Sitosterol receptor during cell death [23]. HMGB1 is a well-studied nuclear DAMP in various types of regulated necrosis and has been implicated in the pathogenesis of infection and sterile inflammation. Our curre
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br Introduction A great many isoprenoids with varieties of
2022-10-11

Introduction A great many isoprenoids with varieties of structural diversity, such as steroids, carotenoids, prenyl quinones, and natural rubber, occur in nature. All of these biosynthetic precursors are constructed by the action of prenyl chain elongating enzymes [1], [2], [3], [4]. These enzyme
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Next to their indirect effect on ASBT expression microbiota
2022-10-10

Next to their indirect effect on ASBT expression, microbiota are also directly involved in BA homeostasis and FXR-FGF15/19 signaling. Different species of intestinal microbiota have the ability to biotransform BAs mainly by deconjugation and subsequent de-hydroxylation, the latter resulting in more
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Although we showed that RBL H Sc cells took
2022-10-10

Although we showed that RBL-2H3 Sc98 calcium sensing receptor took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family,
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In conclusion we demonstrated that the atypical high basal a
2022-10-10

In conclusion, we demonstrated that the atypical high-basal activity of the mGlu3 Quetiapine results mostly from its activation by low ambient glutamate concentrations. This is due to a unique interaction network located in the extracellular domain of the mGlu3 receptor. This network acts as “Cl− l
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Glucose uptake a critical metabolic control point in glycoly
2022-10-09

Glucose uptake, a critical metabolic control point in glycolysis, is mediated by the GLUT (SLC2) family of integral membrane transporters (Mueckler and Thorens, 2013). GLUT1 (SLC2A1), one of the most well-studied members of the SLC2 family, exhibits a wide tissue distribution; cell surface expressio
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