Archives
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br Evasion strategies for enhanced therapeutic outcomes In
2021-09-14
Evasion strategies for enhanced therapeutic outcomes In order to increase AED penetration into the CNS, several strategies have been developed over the years to overcome the activity of efflux transporters, by inhibiting their function or by regulating their expression. Due to the high relevance
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br Conflict of interest br Funding
2021-09-14
Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino torin mg derivatives into cells throughout the body. Disrupting neurotransmitter SLC6-mediated t
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In addition to the increase of extracellular glutamate ICH
2021-09-14
In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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One way to approach this unifying hypothesis will be
2021-09-14
One way to approach this unifying hypothesis will be to compare the effects of the PBR/VDAC ligands on these processes. Recent studies have demonstrated that the three ligands of peripheral-type benzodiazepine receptor, i.e. PK 11195, Ro5-4864 and diazepam reduce membrane transport and conductance i
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Our own search towards aryl imidazole derived GSMs led
2021-09-14
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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The orientation of the immobilized enzyme
2021-09-14
The orientation of the immobilized enzyme may affect its activity and stability and therefore the final biocatalyst performance. Since proteins present areas more prone to unfolding in their surface or near to it [36], the immobilization through these areas may improve the final biocatalyst stabilit
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To investigate an involvement of
2021-09-14
To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) dihydrofolate reductase inhibitor were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in
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Many extracellular matrix ECM proteins are ligands and regul
2021-09-14
Many extracellular matrix (ECM) proteins are ligands and regulators of integrin/FAK signaling and are involved in various aspects of cancer progression, including growth, survival, invasion, and metastasis (Lu et al., 2012). Tubulointerstitial nephritis antigen-like 1 (Tinagl1), a secreted extracell
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br Application of TIRFM to visualizing exocytosis TIRFM
2021-09-14
Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin hippo signaling (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of mutant
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Acetylation of histones by histone acetyltransferases stimul
2021-09-14
Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing Ellipticine synthesis structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Re
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Recent studies in our laboratory demonstrated that several
2021-09-14
Recent studies in our laboratory demonstrated that several histamine H1 receptor antagonists induce apo A-I gene expression while histamine itself represses it [20]. In humans, there are three histamine receptor genes (H1, H2, and H3) that code for G-protein-coupled receptors (GPCR's) which bind his
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The inhibition of NSAIDs towards GLOI provides a
2021-09-14
The inhibition of NSAIDs towards GLOI provides a direction for the development of novel effective GLOI inhibitors. Although the inhibitory activity of indomethacin was determined and the interactions between it SBI-0206965 receptor and GLOI were probed by NMR titration experiments, no detailed inhi
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Acknowledgements This work is partially
2021-09-14
Acknowledgements This work is partially supported by the Natural Science Foundation of China(81273353), and the National Science & Technology Key Projects of China (2009ZX09103-085). Glyoxalase I (GLO I) is a key enzyme in the pathways leading to glutathione (GSH)-mediated detoxification of meth
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Fatty acids have been repeatedly shown to
2021-09-13
Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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br Materials and Methods A human skin SCC
2021-09-13
Materials and Methods A431 (human skin SCC) and HT-297.T (human AK) cell lines were purchased from ATCC (Manassas, VA) and were maintained in DMEM supplemented with 10% fetal calf serum, 4 mM L-Gln, 1 mM sodium pyruvate, 100 U/mL penicillin, and 1 μg/mL streptomycin. Human HK1 and HK2 plasmids we