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br NO GC pathway and implications
2022-08-12
NO-GC-1 pathway and implications for glaucoma Direct in vivo measurement of NO in the eye is not yet feasible. However, measurement of nitrate and nitrite levels are routinely used as markers for the activity of NOS and the production of NO radicals [98]. Several studies in human glaucoma patient
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Among prostaglandins PG PGD remained the most elusive specie
2022-08-12
Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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Similar to GPR A activation of G protein coupled
2022-08-12
Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic thymidine phosphorylase receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et
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Given that inactivation of GLO by BAB is an
2022-08-12
Given that inactivation of GLO1 by 4BAB is an active site directed mechanism, as the transition state analogue CHG protects GLO1 against inactivation by 4BAB (Figs. 2D and S6b), we next set out to determine the amino SKI-606 that is covalently modified by 4BAB. From the X-ray crystallographic struc
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Conformational changes are observed in the LBDs after
2022-08-12
Conformational changes are observed in the LBDs after ligand binding, including partial cleft closure for GluN2A and complete cleft closure for GluN1. For GluN2A, additional conformational rearrangements in the protein and ligand may be required before the ligand can be accommodated within lobe 2. F
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The plasma levels of glucose and amino acids at day
2022-08-12
The plasma levels of glucose and amino acids at day 0 likely represent the function in utero since the blood was collected within 2h after birth. To elucidate the roles of intestinal transporters as determinants of plasma levels of glucose and amino acids, we analyzed the correlation between the exp
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br Conflict of interest statement br Acknowledgements This
2022-08-12
Conflict of interest statement Acknowledgements This work was supported by the National Health and Medical Research Council of Australia (NHMRC) (project grants [1061044], [1065410] and [1126857], and NHMRC program grant [1055134]); P.M.S. and A.C. are NHMRC Principal and Senior Principal Rese
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br G protein coupled receptor GPR also
2022-08-11
G-protein coupled receptor 40 (GPR40), also known as a free fatty Medetomidine HCl receptor receptor, is dominantly expressed in pancreatic β cells and intestine K, L cells., . Besides, GPR40 is also reported to be expressed in brain, but its function is still unknown. It is well documented that
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br Materials and methods br Results br Discussion Since earl
2022-08-11
Materials and methods Results Discussion Since early times, herbs and their extracted substances have been used as foods and medicinal resources worldwide (Petrovska, 2012). A Ginger is one of the most important and oldest spices, consisting of the prepared and sun-dried rhizomes of Zingibe
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Previous study demonstrated that Hcy elevated organ culture
2022-08-11
Previous study demonstrated that Hcy elevated organ culture-induced up-regulation of ETB receptor in VSMCs (Chen et al., 2016a; Chen et al., 2016b). Many signaling pathways were involved in Hcy-induced up-regulation of ETB receptor in VSMCs, such as ERK1/2/NF-κB signaling pathway, Sirt1/NF-κB signal
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The H R antagonist cimetidine Tagamet became the
2022-08-11
The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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The other possibility for the lack
2022-08-11
The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,
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The inhibitory activities against HDAC and HDAC
2022-08-11
The inhibitory activities against HDAC1 and HDAC6 of title compounds were evaluated in a fluorescent assay using SAHA and ACY-1215 as positive control. The results were displayed in A. Compounds – with linker containing 5–7 carbons showed good inhibitory activities against HDAC6. They also displayed
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Sonidegib is currently under investigation
2022-08-11
Sonidegib is currently under investigation for the treatment of relapsed/refractory acute leukemia (NCT01826214) [76]. All patients experienced at least 1 AE, including anemia, diarrhea, fatigue, nausea, muscle spasms, decreased appetite, and blood creatine phosphokinase increased. The ongoing phas
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A few animal and cell culture
2022-08-11
A few animal and cell culture studies have been reported that the reason of HCV-related hepatic steatosis in CHC infection is mainly HCV core protein (Chang et al., 2007; Perlemuter et al., 2002; Ferré, 2004). HCV core protein inhibits activities of microsomal triglyceride transfer protein (MTP) and
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