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br Materials and methods br
2021-10-22

Materials and methods Acknowledgments Introduction Gentiooligosaccharides are novel functional oligosaccharides composed of glucose units linked through β-1,6 glycosidic bonds, examples of which include gentiobiose, gentiotriose and gentiotetraose (Barreteau et al., 2006, Kim et al., 2003,
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protease inhibitor cocktail In order to discover novel small
2021-10-22

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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In conclusion starting from the weakly potent GSM
2021-10-22

In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic PD 169316 synthesis led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally reporte
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Acknowledgements br Introduction Alzheimer s disease AD is a
2021-10-22

Acknowledgements Introduction Alzheimer's disease (AD) is a devastating neurodegenerative disorder and the leading cause of dementia. There is currently no treatment available to slow or halt disease progression. The underlying mechanisms of AD on the cell and molecular levels are still not comp
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Interestingly we have shown that OA required FFAR
2021-10-21

Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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br Acknowledgments We apologize for the omission
2021-10-21

Acknowledgments We apologize for the omission of primary citations owing to space limitations. This work was supported by grants from National Natural Science Foundation of China (81772801 and 81472455 to C.D.), the Key Program of Zhejiang Provincial Natural Science Foundation (LZ17H160002 to C.D
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br The inhibitory effect of ATP B knockdown
2021-10-21

The inhibitory effect of ATP7B knockdown on lysosomal exocytosis is likely mediated by the resulting oxidative stress induced by Cu, as exposure to oxidative stress induced by tert-Butyl hydroperoxide (TBHP) inhibited β-hex exocytosis as well, indicating that oxidative stress inhibits lysosomal ex
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The role of the ER EK variant which is associated
2021-10-21

The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of hedgehog pathway levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protect f
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br The small conductance Ca activated K SKCa SK
2021-10-21

The small conductance Ca-activated K+ (SKCa; SK, SKCa, KCa2) channels are recognized as a subfamily of KCa channels (Bond, Maylie, & Adelman, 1999). The SKCa channel is encoded by three distinct genes, KCNN1, KCNN2, and KCNN3 with different sensitivities toward apamin. Different with BKCa channels
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br Acknowledgments br Introduction Non
2021-10-21

Acknowledgments Introduction Non-steroidal anti-inflammatory drugs (NSAIDs) are a common treatment for a number of disease states involving an inflammatory reaction. This group of drugs mediate their anti-inflammatory effects mainly by inhibition of cyclooxygenase (COX), an enzyme of prime imp
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Recently it has been found that treatment of
2021-10-21

Recently, it has been found that treatment of human phagocytic HATU or microvascular endothelial cells with NO donors inhibited the O2− generating capacity of NADPH oxidase [[8], [9], [10], [11]], which may involve down-regulation or S‑nitrosylation of the p47phox subunit (a cytosolic subunit of NA
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Epigenetic drugs such as HDAC inhibitors regulate gene expre
2021-10-21

Epigenetic drugs, such as HDAC inhibitors, regulate gene expression by affecting the activity of histone or DNA modifying enzymes and their associated transcriptional response [141]. BET bromodomain protein inhibition is another epigenetic approach for blocking the Hedgehog pathway at the downstream
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Recently anti tumor or antiviral strategies
2021-10-21

Recently, anti-tumor or antiviral strategies using RNAi for both gene silencing and innate-receptor activation were designed; one mechanism of these strategies is activating the intracellular retinoic acid–inducible gene I protein (RIG-I). 5′-Triphosphate RNA (3p-small interfering RNA [siRNA]) is th
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Failure of antioxidant defenses to remove
2021-10-21

Failure of antioxidant defenses to remove exogenous ROS produced by redox cycling chemicals either by being inhibited by those compounds or overwhelmed by an excess ROS, will disrupt the balance between antioxidant/prooxidant system within the organisms leading to oxidative damage (Livingstone, 2003
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Recently a G protein coupled receptor GPR a was identified
2021-10-20

Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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