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Lipid sensing GPCRs as therapeutic targets G protein coupled
2021-10-13

Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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Some biguanides can cross the mitochondrial membrane
2021-10-13

Some biguanides can cross the mitochondrial membrane and increase L-lactate formation by inhibiting oxidative Decanoyl-RVKR-CMK [34]. On the other hand, it has also been reported that levels of fasting plasma lactate in T2DM patients are similar regardless of whether or not metformin is administere
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In conclusion we have designed and characterized a
2021-10-13

In conclusion, we have designed and characterized a novel series of EAAT-blockers, exemplified by (-[4-(2-bromo-4,5-difluorophenoxy)phenyl]--asparagine)—a potent, selective, competitive non-substrate inhibitor of EAAT-2. As one of the most potent and selective EAAT-2 inhibitors identified to date,
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In order to elucidate the reasons of
2021-10-13

In order to elucidate the reasons of high efficacy of , we evaluated the BOC group itself and the linkage between the BOC group and the benzene ring of A-part. Urea moiety (), the replacement of an oxygen filgotinib synthesis of the BOC group to a nitrogen atom, decreased the activity (EC = 0.12 μM)
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Animal studies have shown that various antidepressant treatm
2021-10-13

Animal studies have shown that various antidepressant treatment are capable of upregulating GR protein and mRNA in key Imeglimin synthesis regions including the hippocampus and decreasing basal and/or stress-induced glucocorticoid secretion [37]. Changes in the level or function of GR regulate the n
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Azidobutyric acid NHS ester sale When PKC was applied alone
2021-10-13

When PKC19–31 was applied alone, it attenuated the activity run-down following excision. Furthermore, the activity induced by addition of PKC19–31 during PMA treatment in many cases was higher than in controls. Accordingly, in our experimental conditions, the mechanism which underlays channel inhibi
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Based on the previous report that
2021-10-12

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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Recent research has focused on identifying key
2021-10-12

Recent research has focused on identifying key agonists and receptors mediating nutrient-induced GLP-1 and insulin secretion. The long-chain fatty phenethyl receptor receptor GPR40 is the most abundant GPCR expressed in islet β cells and is also expressed on intestinal L-cells, where it contributes
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By measuring the accumulation of unprenylated Rap a as a
2021-10-12

By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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Colorectal cancer CRC is the
2021-10-12

Colorectal cancer (CRC) is the leading cause of cancer deaths in Taiwan and is also a most common cancer in the world (Huang et al., 2012, Jemal et al., 2011). With early detection and treatment in the initial stage, CRC can be recognized as curable in comparison with other malignant tumors (Levin e
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TLRs were originally identified as pathogen associated molec
2021-10-12

TLRs were originally identified as pathogen-associated molecular pattern recognition receptors that recognized exogenous ligands in response to infection [31]. In cirrhotic mice or patients, the gastrointestinal tract produces and absorbs considerable bacterial LPS with increased permeability of the
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br Acknowledgments We thank Drs Yasuhiro Saito and Mitsuru
2021-10-12

Acknowledgments We thank Drs. Yasuhiro Saito and Mitsuru Futakuchi for helpful discussion. We also thank Drs. Kohei Miyazono and Tadashi Matsuda for cells. This work was supported by Grant-in-Aids for Scientific Research on Innovative Area (16H06373; 16K15273) from MEXT, Japan (to M.H.) and by Pr
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In this study we present the first data
2021-10-12

In this study, we present the first data on the kinetic properties of the hexokinase of T. equiperdum, which we compare with similar data available for pleomorphic T. brucei (Seed and Baquero, 1965, Nwagwu and Opperdoes, 1982, Hara et al., 1997, Morris et al., 2006, Chambers et al., 2008b, Chambers
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An important aspect of macrophage biology
2021-10-12

An important aspect of macrophage biology, highly influenced by HO-1 activity, is macrophage polarization. The broadest classification, based on the in vitro stimulation, surface marker expression, and inflammatory cytokines production, describes macrophages as classically activated, proinflammatory
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The relationship between increased GPR expression
2021-10-12

The relationship between increased GPR120 expression in the EDL skeletal muscle and systemic glucose control is yet to be investigated. However, if the increased expression of GPR120 correlates with enhanced insulin-stimulated glucose uptake in skeletal muscle, particularly the EDL muscle, this migh
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