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Recently several groups reported that four orphan receptors
2021-10-01
Recently, several groups reported that four orphan receptors, GPR40, GPR41, GPR43, and GPR120, can be activated by free fatty acids. Short-chain fatty acids are specific agonists for GPR41 and GPR43 . Medium and long-chain fatty acids can activate GPR40 and GPR120 . Our previous report showed that
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In the brain hydrolysis of AG by MGL is the
2021-10-01
In the brain, hydrolysis of 2-AG by MGL is the primary source of AA for conversion to PGs by cyclooxygenase (Nomura et al., 2011). PGE2 production is required for IL-1β-evoked synapse loss (Mishra et al., 2012). Here, we tested whether decreased PG levels contributed to the synapse protective effect
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Studies of human and mouse GPR as
2021-10-01
Studies of human and mouse GPR84, as ascertained by mRNA levels in various tissues, have determined that GPR84 is highly expressed on bone marrow cells, splenic T and B cells, and circulating granulocytes/monocytes/macrophages. In the latter cells, mRNA expression of is up-regulated only under infl
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At the second step blind docking simulation of
2021-10-01
At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se
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Extending time action is another strategy to increase in viv
2021-10-01
Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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FAK Inhibitor 14 Cx is the major molecule involved in
2021-10-01
Cx43 is the major molecule involved in the dynamic life cycle of GJIC (Cusato et al., 2006). Initially generated Cx43 exist in the cytoplasm and correctly transfer it to the plasma membrane during its life cycle (Ji et al., 2018). To understand the toxic effects of MC-LR on GJIC, Cx43 localization w
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The anti platelet functions of ZGR were confirmed by the
2021-09-30
The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagati
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Treatment with histamine had no effect on histamine H recept
2021-09-30
Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 PS-341 (Fig. 1), while knockdown of histamine H1 receptor expression prevented histamine from repressing apo A-I gene expression (Fig. 2). Overexpression of the histamine H1 receptor regulated apo A-I promoter activ
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br Acknowledgments We thank Drs Yasuhiro Saito
2021-09-30
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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br Hippo Signaling in Autoimmunity An
2021-09-30
Hippo Signaling in Autoimmunity An imbalance of T cell subsets, such as immunosuppressive regulatory T Pemetrexed (Treg) and inflammatory TH17, has a key role in autoimmune diseases. Recently, investigations found that TAZ but not YAP enhances TH17 differentiation but attenuates Treg differentia
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The mechanisms of action of MMF and DMF are
2021-09-30
The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio
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Attempting to further elucidate the role of glucagon
2021-09-30
Attempting to further elucidate the role of Mirin and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well as β cell area compared
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The role of GJs in liver fibrogenesis was studied
2021-09-30
The role of GJs in liver fibrogenesis was studied recently. Studies showed a significant decrease in liver fibrosis in Cx32 knockout mice compared to wild-type mice. Although the mechanism underlying this protective effect of Cx32 deletion is not clear, reduced oxidative stress was suggested as a po
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Several small molecules such as erastin and RSL
2021-09-29
Several small molecules, such as erastin and RSL3, are reported to induce ferroptosis in both normal and cancer glibenclamide [21,22]. We confirmed that erastin-induced growth inhibition is an ideal ferroptosis model for cardiomyocytes. The erastin inhibits the growth of H9c2 cells in a Fe-dependen
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br The signal of ferroptosis
2021-09-29
The signal of ferroptosis ROS generated by extracellular or intracellular stimuli play a fundamental role in cell and tissue injury in a variety of disease states [47]. Ferroptosis is generally considered as a type of ROS-dependent regulated necrosis [48]. Intracellular iron accumulation and lipi
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