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The typical pharmacophore for GPR agonists contains four par
2022-09-16
The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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The third generation cephalosporin antibiotics can cross
2022-09-16
The third-generation cephalosporin bupropion hydrochloride can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when taken
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The mammalian AMPA receptor protein
2022-09-16
The mammalian AMPA receptor protein family comprises four subunits, termed GluR-A through GluR-D (or GluR1 through GluR4), which form hetero-tetrameric receptor complexes Dingledine et al. 1999, Rosenmund et al. 1998. These subunits possess distinctive intracellular C-terminal domains that can be gr
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br Experimental br Acknowledgments This project was generous
2022-09-16
Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t
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Our data suggest that Slc a is important for amino
2022-09-16
Our data suggest that Slc38a5 is important for amino-acid-induced α cell proliferation and expansion of α cell mass following GCGR inhibition, but not for formation and maintenance of α cell mass. This is supported by the finding that Slc38a5−/− mice have normal α cell mass. This is interesting sinc
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br Acknowledgments The authors gratefully acknowledge the su
2022-09-15
Acknowledgments The authors gratefully acknowledge the support provide by National Natural Science Foundation of China (Number 31301415). Introduction β-Galactosidases (EC 3.2.1.23), frequently known as lactases, are widely used in lactose hydrolysis. This disaccharide is present in mammalian
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NMDARs are glutamate gated ionotropic
2022-09-15
NMDARs are glutamate-gated ionotropic receptors that are involved in excitatory neurotransmission and plasticity (Traynelis et al., 2010). There have been several reports showing that neurosteroids acting as negative modulators of NMDARs exert neuroprotective activity in both in vitro and in vivo mo
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1,2-Dimyristoyl-sn-glycerol mg Type II diabetes is character
2022-09-15
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 1,2-Dimyristoyl-sn-glycerol mg receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of re
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The improved glucose tolerance of Ffar R W R
2022-09-15
The improved glucose tolerance of Ffar1R258W/R258W mice on HFD was unexpected. In combination with similar fasting blood glucose levels, the significant lower fasting plasma insulin of mutant mice compared to wild-type mice is indicative of improved insulin sensitivity. However, peripheral insulin r
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Interestingly the subcellular localization of FBPase in
2022-09-15
Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule RI-1 reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the ability of
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Previously we have isolated liver FBPase
2022-09-15
Previously we have isolated liver FBPase from Pelophylax esculentus (former Rana esculenta, Frost et al., 2006) and characterized its kinetic properties (Dziewulska-Szwajkowska and Dzugaj, 1999) on the contrary the muscle FBPase has never been fully characterized. The primary aim of the present pape
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In accordance with our study
2022-09-15
In accordance with our study, the blockage of Fas/FasL pathway and overexpression of miR-204-5p was associated with reduced BUN, Scr, and MDA, as well as elevated SOD and GSH-Px. A recent study has reported the ectopic expression of BUN and Scr in RIRI animals, which marked the dysfunction of kidney
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br Materials and methods br Results To
2022-09-15
Materials and methods Results To examine the apoptosis in FLS in vitro, we measured the number of caspase pathway in early apoptosis (Annexin V+, 7-AAD−) and late apoptosis/necrosis (Annexin V+, 7-AAD+) using flow cytometry after incubation with or without stimulating Fas antibody. In the abs
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Kif15-IN-1 Focal adhesion kinase FAK also known as protein
2022-09-15
Focal adhesion kinase (FAK), also known as protein tyrosine kinase2 (PTK2), is a tyrosine kinase and vital member in integrin-mediated signaling pathways [3]. In response to integrin involvement, FAK would be phosphorylated. It was reported that FAK is involved in cellular adhesion and spreading [4]
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Factor Xa FXa has emerged
2022-09-15
Factor Xa (FXa) has emerged as a particularly promising target for the development of effective anticoagulant drugs because FXa acts at the convergence point of the extrinsic and intrinsic coagulation pathways. It efficiently catalyzes the conversion of prothrombin to thrombin with one molecule of F
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