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br Acknowledgments The financial support from the National N
2022-05-13
Acknowledgments The financial support from the National Natural Science Foundation of China (Nos. 31460422 and 31060210), the Natural Science Foundation of Jiangxi Province, China (20171BAB204029 and 20143ACB20006), the Project of Science and Technology of Jiangxi Provincial Education Department,
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In order to discover novel small molecule compounds with
2022-05-13
In order to discover novel small-molecule compounds with the activity of GLUT4 translocation, we conducted a cell-based phenotype screening in L6-GLUT4-myc myoblasts by measuring appearance of GLUT4 on the plasma membrane (GLUT4 translocation activity). Evaluation of total 183,400 compounds gave sev
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br Materials and methods br Results br Discussion The
2022-05-12
Materials and methods Results Discussion The distribution of FFA1 and FFA4 expressed in normal tissues is distinguishable. FFA1 is expressed in the restricted organ, such as pancreatic beta Xylometazoline HCl [18]. In contrast, FFA4 is highly expressed in the lung, gastrointestinal tract,
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Magtanong et al observed that caspase
2022-05-12
Magtanong et al. (2019) observed that caspase-dependent apoptotic lipotoxicity of saturated fatty acids is suppressed by exogenous MUFAs. This may explain the ability of MUFAs to prevent atherosclerosis, in contrast to the pathogenicity of saturated fatty acids. Moreover, MUFAs may promote while PUF
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We focus here on the historical discoveries that
2022-05-12
We focus here on the historical discoveries that led to the development of the concept of ferroptosis. Ferroptosis is defined as an iron-dependent form of regulated cell death, which occurs through the lethal accumulation of lipid-based reactive oxygen species (ROS) when glutathione (GSH)-dependent
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Recent findings of us suggest that compounds
2022-05-12
Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that
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These agents can be divided
2022-05-12
These agents can be divided into three categories based upon the therapeutic agent conjugated to the antibody; the most frequently explored are ADCs using a cytotoxic agent to be delivered directly to the tumor site. The second class has not been broadly used and consists of radionucleotides (Wong e
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Palomid 529 Compared with the tetrazole derivative the poten
2022-05-12
Compared with the tetrazole derivative , the potency of analogs – was 3- to 17-fold improved. Of the range of heterocycles prepared, 1,2,4-thiadiazol-5(4)-one and 1,3,4-oxadiazol-2(3)-one showed the best potencies of 0.52μM and 0.61μM, respectively. Introduction of a second hydrogen bond donor, su
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br Conclusion Interactions between neurons and astrocytes de
2022-05-12
Conclusion Interactions between neurons and astrocytes depend on the spatial configuration of their contacts. Therefore, changes of astrocyte morphology may impact various physiological mechanisms ranging from glutamate uptake and potassium homeostasis to modulation of synaptic transmission and p
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Introduction Multiple sclerosis MS a neurological autoimmune
2022-05-12
Introduction Multiple sclerosis (MS), a neurological autoimmune disease, is driven by CD4+ AMG232 synthesis of the T helper (TH) cells [1]. There is no curative treatment for MS and the present treatments typically focus on immunomodulation for slowing the progression of the disease. These includes
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Adenosine triphosphate ATP is thought to
2022-05-11
Adenosine triphosphate (ATP) is thought to be a crucial molecule in acute pain signaling in the DRG, as well as in the development and maintenance of chronic pain (Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). Extracellular ATP activates the ionotropic P2X receptors (Bur
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br Conclusion In conclusion SHP
2022-05-11
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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The in vivo biological activity of the four
2022-05-11
The in vivo biological activity of the four novel analogues was then systematically assessed in three animal models including normal control, high fat fed and ob/ob mice. As expected from earlier in vitro studies, all four glucagon receptor antagonists had minor effects on glucose or insulin concent
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br GLP R expression in the
2022-05-11
GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS
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br Declaration of competing interests br Acknowledgements Th
2022-05-11
Declaration of competing interests Acknowledgements The authors wish to thank the Natural Science Foundation of Jiangsu Province (BK20171261), the project of outstanding scientific and technological innovation group of Jiangsu Province, the National Science Fund for Distinguished Young Scholar
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