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nkcc inhibitor Generally replacement of the aryl group
2022-05-13

Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations
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br Materials and methods br Results br Discussion DNA repair
2022-05-13

Materials and methods Results Discussion DNA repair pathways have evolved for a long time to act independently of one another. However, over the past decade several overlaps and crosstalks between these pathways were identified, showing that the DNA repair system is more complex than previo
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In response to oxidative stress in DM
2022-05-13

In response to oxidative stress in DM, antioxidant defence systems are activated in β-cells. Glutathione (GSH) is one of the most abundant antioxidants and has been shown to be expressed at lower concentrations in patients with DM [12], [13]. Furthermore, plasma levels of glycine, which is a synthet
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Cy5 TSA Fluorescence System Kit synthesis Introduction Hista
2022-05-13

Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activiti
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Introduction Histamine was generally accepted as
2022-05-13

Introduction Histamine was generally accepted as a neurotransmitter in 1984, when histamine was first identified to be located in tuberomamillary nucleus (TM) of the brain (Watanabe et al., 1984). In mammals, histaminergic neurons play an important role in regulating multiple physiological activiti
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Active compounds and were further tested and EC
2022-05-13

Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of
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br Regulation of GCK by intrinsic conformational dynamics
2022-05-13

Regulation of GCK by intrinsic conformational dynamics GCK is a 465-residue, 52-kDa enzyme comprised of two domains, hereafter referred to as the large domain and the small domain, that are separated by a flexible hinge region. As with other proteins that adopt the hexokinase fold, substrates bin
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br Conflict of interest br Transparency document
2022-05-13

Conflict of interest Transparency document Acknowledgements We acknowledge our funding sources from the American Heart Association (13EIA4480016) and the National Institute of Health/National Heart, Lung, and Blood Institute (RO1 HL094414). We are very grateful to Dr. Shaohua Xiao and Dr. S
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Iodination of commercially available with
2022-05-12

Iodination of commercially available with excess ICl in AcOH gave a quantitative yield of , which was cyclized with benzyl thioamides to give the 2-benzyl-9,10-dihydro-4-1-thia-3,4-diaza-benzo[]azulenes . Coupling of the iodides with heterocycles including imidazoles, triazoles, or zinc cyanide us
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The physicochemical properties of the prodrugs provided impo
2022-05-12

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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br Materials methods br Results
2022-05-12

Materials & methods Results FAS c.-671AA, AG and GG genotypes and A and G kinase inhibitor frequencies were similar in both patients with FMF and healthy control groups, and no significant difference was found (P>0.05, Table 1). The frequency of TC genotype in FASLG in the healthy controls was
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br Application of TIRFM to visualizing exocytosis TIRFM
2022-05-12

Application of TIRFM to visualizing exocytosis TIRFM was first used to visualize exocytosis from large secretory granules from chromaffin AXL1717 (Steyer et al., 1997). Before that, visualization of secretory organelle was strictly limited to a few exceptions, such as mast cell of mutant mice, o
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The combination of HIV antigen and
2022-05-12

The combination of HIV antigen and antibody testing with the fourth generation immunoassays shortens the window AMG 487 for HIV by detecting HIV antigen, which appears in the blood before seroconversion [3,5,11,12]. Analysis of the seroconversion panels indicated the Elecsys® HIV Duo assay has a goo
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Migration chemotaxis and trafficking of leukocytes including
2022-05-12

Migration, chemotaxis and trafficking of leukocytes, including eosinophils from the peripheral blood into the site of inflammation requires their adhesion to endothelial JC-1 (Ley et al., 2007). Despite ongoing research, the histamine effect on eosinophils adhesion to endothelium cells has not been
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Freinkel first reported in the late s
2022-05-12

Freinkel first reported in the late 1960s that maternal hypertriglyceridemia benefits the fetus during starvation by increasing maternal consumption of triglyceride for ketone body synthesis giving the basis for “accelerated starvation” theory [4,5]. This maternal metabolic reprogramming during peri
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