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In addition we assessed the viability of tetrahydroquinoline
2022-07-12

In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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To our knowledge the putative role of ET and ETB
2022-07-12

To our knowledge, the putative role of ET-1 and ETB-R in oligodendroglioma progression was not documented so far. Using primary cultures of grade B oligodendroglial tumor cells, we have here assessed the functionality of ETB-R expression in these tumors. Confocal microscopy analysis confirmed the st
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Literature review suggests a strong presence of central hist
2022-07-12

Literature review suggests a strong presence of central histaminergic transmission in the PNU-120596 sale areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine in th
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Allergic rhinitis characterized by inflammation of
2022-07-12

Allergic rhinitis, characterized by inflammation of the nasal membrane, results from an over-activated immune system exposed to Istaroxime hydrochloride synthesis in sensitized individuals, and is associated with nasal congestion, rhinorrhea, sneezing, and pruritus. As histamine is a key mediator i
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The cytotoxicity of these compounds against
2022-07-12

The cytotoxicity of these compounds against Hep3B cells was assessed using the MTT assay. As shown in , compounds in series and (except ), which retained the carboxyl at C-17, showed no appreciable cytotoxic activity (IC > 100 μM), whereas compounds in series (except ,) were modestly cytotoxic, i
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Human epidermal growth factor receptor HER neu also
2022-07-12

Human epidermal growth factor receptor 2 (HER2/neu, also known as CerbB-2, or ERBB-2) is a proto-oncogene located on chromosome 17q21, which encodes a transmembrane protein with tyrosine kinase activity, and belongs to the HER receptor family (EGFR, named also HER1, HER3, and HER4) [6]. HER2 is invo
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Over the last few years
2022-07-12

Over the last few years, experimental evidence for the involvement of Epac1 in cancer progression is beginning to emerge (Almahariq et al., 2015, Banerjee and Cheng, 2015, Parnell et al., 2015, Parnell et al., 2015, Schmidt et al., 2013). For example in melanoma cells, silencing of Epac1 attenuates
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Our results show furthermore that higher concentrations of
2022-07-12

Our results show furthermore, that higher concentrations of butyric ACSF additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GSTP1 expression remai
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br Materials and methods br Results
2022-07-11

Materials and methods Results Discussion All the UDG superfamily glycosylases examined here, UDG, SMUG1, TDGFL, and TDG82−308, are capable of completely converting U-containing duplex substrates to product, though at different rates. Under STO conditions, kobs reflects the slowest kinetic s
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Finally the results in this article indicate
2022-07-11

Finally, the results in this article indicate that atomistic MD in conjunction with computational electrophysiology and ion-permeation simulations provide a useful tool for the functional annotation of ion-channel structures. In particular, they exemplify how MD simulations in native lipid membranes
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In summary activated A AR exacerbated the reverse
2022-07-11

In summary, activated A2AR exacerbated the reverse transport function of endothelial EAATs through a direct or indirect pathway depending on PKA and glutamate levels in response to OGD in vitro, but A2AR inhibition quickly restored the normal transport function. Moreover, the key mechanisms by which
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NPE-caged-proton mg In this study for the first time the
2022-07-11

In this study, for the first time: 1) the electrochemical glutamate oxidase-based biosensor was optimized for the determination of low micromolar glutamate concentrations; 2) the algorithm of the analysis of exocytotic and transporter–mediated glutamate release was developed; 3) the comparative anal
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A high fat maternal diet during the pregestation
2022-07-11

A high-fat maternal diet during the pregestation period and extending throughout gestation (including the period of conception) has the propensity of affecting early embryonic development and placentation. Previous investigations have revealed that the preimplantation embryos are generally exposed t
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br Funding sources This work was
2022-07-11

Funding sources This work was supported, in part, by NIH GM115388 to BGM. Acknowledgements Introduction Glucokinase (GCK) plays a central role in the regulation of glucose metabolism. Its activity is restricted to mtep mg with important roles in whole-body glucose homeostasis [1]. In panc
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The glucocorticoid GR complex exerts wide
2022-07-11

The glucocorticoid-GR complex exerts wide-spread cellular effects through two distinct mechanisms categorized as genomic and non-genomic pathways [3,39]. Most non-genomic pathways originate from activation of mGR [40]. These actions of the GR appear to all play an important role in the regulation of
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