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In recent years many studies
2021-11-30

In recent years, many studies have demonstrated that the release of endogenous FPR ligands can influence severe diseases associated with inflammation, including systemic inflammatory response syndrome (SIRS)20, 21 and cancers, such as glioblastoma as well as gastric and colorectal cancer 22, 23, 24.
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Type II diabetes is characterized
2021-11-30

Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty AZD6738 australia receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptors and
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br Materials and methods br
2021-11-30

Materials and methods Results and discussion Conclusion The as-designed system was based on the assembly of MSN-Cy and TPGS, which was dominated by π-π stacking interactions. By the strong mutual force, Cypate and TPGS formed a compact layer around the MSN core, which blocked the drug leaka
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Interestingly the rabbit cornea exhibited a more
2021-11-30

Interestingly, the rabbit cornea exhibited a more than two-fold higher level of total GST activity compared with that of the porcine cornea, whereas their levels of GSTO1‐1 and GSTP1‐1 activity were similar (Fig. 4). Because members of the GST Alpha, Mu, Pi and Omega Cathepsin K Activity Fluorometri
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Thyroid hormone triiodothyronine T and its precursor thyroxi
2021-11-29

Thyroid hormone 3,5,3′-triiodothyronine (T3) and its precursor, thyroxine (T4), are iodinated compounds, which are known to regulate the expression of genes involved in various biological processes, such as development, growth and metabolic control. The iodothyronine deiodinase types I, II and III (
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br Conclusion In conclusion SHP was demonstrated as a
2021-11-29

Conclusion In conclusion, SHP289-04 was demonstrated as a potent glucokinase activator. It could normalize the blood glucose level and lipid level in spontaneous type 2 diabetes model KKAy mice. At the same time, it ameliorated the function of islets and liver in KKAy mice. It had been proved to
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cAMP is a key secondary messenger which transduces
2021-11-29

cAMP is a key secondary messenger which transduces extracellular signals at glucagon receptors to intracellular effector molecules. cAMP-protein kinase A (PKA) pathway increases the gene expression of enzymes including phosphoenolpyruvate carboxykinase (PEPCK) and glucose 6-phosphatase (G6Pase) whic
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In our reporter assay system C H T Gli Luc
2021-11-29

In our reporter assay system, C3H10T1/2-Gli1-Luc cells were incubated with Shh CM to induce Gli1-mediated luciferase activity (Fig. 1B). Z-Ajoene inhibited Shh CM-induced luciferase activity in a concentration-dependent manner as seen in Fig. 1C. Z-Ajoene also inhibited SAG (a Smo activator)-induced
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In the a first in vitro indication of modulation
2021-11-29

In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio
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Fmoc-Phe-OH To investigate the potential molecular mechanism
2021-11-29

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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The rationale for developing HDACi as anticancer agents was
2021-11-29

The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and integrin signaling pathway arrest of cancer cells 1, 2, 3. HDACi have been used in the treatm
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Initial structural and biochemical work showed that Get
2021-11-29

Initial structural and biochemical work showed that Get3 forms an obligate dimer whose conformation is regulated by the bound nucleotide. Analogous to SRP and SR, Get3 contains a P-loop nucleotide hydrolase domain in which the bound ATPs face one another at the dimer interface (Figure 3A, top right
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The cytoprotective effects of glyRs have been reported to as
2021-11-29

The cytoprotective effects of glyRs have been reported to associate with the MAPK (JNK, ERK1/2 and p38) signaling pathways [47], [48]. The present study reveals that suppressive phosphorylation of cRaf-MEK1/2-ERK1/2 is initiated by glycine – glyR α2 interactions in cardiomyocytes. As a central regul
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Several observations about structure activity relationships
2021-11-26

Several observations about structure–activity relationships can be made from this series, including that: (1) all lead compounds are NSAIDs of the 2-arylpropionic STA-21 class, (2) analogues with -oriented aryl substituents showed the best inhibition of FAAH, and (3) replacing the ether linkage of
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Accumulating evidence suggests an important role for
2021-11-26

Accumulating evidence suggests an important role for endothelin ETB receptors in renal homeostasis. ETB receptors promote vasodilation, natriuresis, and diuresis (Davenport and Maguire, 2011) and maintain renal perfusion via counterbalancing the effects of vasoconstrictors and regulation of water re
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