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Glycine regulates several brain functions
2022-08-18
Glycine regulates several brain functions and glycine transporters significantly contribute in such processes. In previous work we reported calpain sensitive regions in N-terminal domains of GlyT1a and GlyT1b (Baliova and Jursky, 2005). Here we show that distal part of glycine transporter GlyT1C-ter
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Armed with this knowledge we looked at ways to
2022-08-18
Armed with this knowledge, we looked at ways to reduce the log of through nitrogen incorporation while still maintaining potency via installation of ortho substituents such as chloro, methyl, bromo, and thiomethyl (). In general, pyridine analogs were less active ( vs ; vs ; vs ) than their simpl
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br The presence of an active glyoxalase pathway
2022-08-18
The presence of an active glyoxalase pathway in an apicomplexan parasite was first reported in Plasmodium falciparum-infected erythrocytes (Vander Jagt et al., 1990). Some years later, glyoxalase I and both glyoxalase II enzymes were characterized in this parasite (Akoachere et al., 2005, Iozef et
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Capillary monolithic columns obtained by in situ polymerizat
2022-08-18
Capillary monolithic columns obtained by in situ polymerization have been developed rapidly as an efficient chromatographic stationary phase, which exhibits excellent reproducibility, reliable stability and fast transfer kinetics [18]. Recently, it has been extensively applied in capillary liquid ch
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br Experimental Procedures br Acknowledgments This work was
2022-08-18
Experimental Procedures Acknowledgments This work was supported by NIH/National Human Genome Research Institute (NHGRI) R00 HG006922 and NIH/NHGRI R01 HG008974 (to J.G.), the Huntsman Cancer Institute, and the Women’s Cancers Disease-Oriented Team at the Huntsman Cancer Institute. Research rep
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The findings in mice were echoed in the human
2022-08-18
The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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Therefore as it stands presenilin has a secretase independen
2022-08-18
Therefore as it stands, presenilin has a γ-secretase-independent role in regulating protein trafficking, proteolysis and degradation, however given that inhibition of γ-secretase activity can have a negative effect on protein trafficking [69], [98], we cannot exclude the possibility that some of th
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br Secretase modulators a loss
2022-08-18
γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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Target regulated the formation of G quadruplex
2022-08-18
Target-regulated the formation of G-quadruplex was used here to “kill two Acetaminophen synthesis with one stone” for the detection of melamine and I− with one probe DNA. G-quadruplexes are higher-order structures formed from G-rich oligonucleotides through the stacking of planar G-tetrads [43,44].
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Glucose metabolic pathways are well defined but
2022-08-18
Glucose metabolic pathways are well defined but the subcellular organization of these pathways is poorly understood in liver and kidney. Several factors affect the net flux of gluconeogenesis and allow the AK-7 to respond to physiological changes [1]. Ovadi and Srere have suggested that a new regul
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In summary although there are still several important questi
2022-08-18
In summary, although there are still several important questions open on the mechanisms that trigger FAK nuclear localization and FAK-dependent gene regulation, Cardoso et al. (2016) provide important new insights on FAK/MEF2-mediated initiation of cardiac hypertrophy. Acknowledgments The author
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Introduction Ventilator induced lung injury VILI
2022-08-18
Introduction Ventilator-induced lung injury(VILI) is the most common complication in the mechanical ventilation in clinic. Repetitive opening and closing of HOBt at high pressures during artificial ventilation would generate shear stress and then lead to the damage of cell junction and dysregulatio
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br Results br Discussion HIV reservoirs represent
2022-08-18
Results Discussion HIV reservoirs represent a major barrier to HIV eradication (Archin et al., 2014, Kimata et al., 2016), and substantial research efforts are being directed toward the goal of identifying and eliminating this obstacle to cure (Archin and Margolis, 2014, Pitman et al., 2018).
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Ropivacaine HCl The replacement of the P butyl urea
2022-08-17
The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P
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In an effort to further improve the
2022-08-17
In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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