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Pharmacologic approaches of inhibiting GSNOR activity have r
2022-04-02
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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In plants NO production is
2022-04-02
In plants, NO production is one of the early responses to stress (Tossi, Lamattina, & Cassia, 2009). Usually, NO signal transduction requires the involvement of downstream signaling compounds. We further investigated the effects of cGMP on GSK-3 expression. The data showed that LY83583 (a cGMP inhib
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Introduction Non alcoholic hepatic steatosis is characterize
2022-04-02
Introduction Non-alcoholic hepatic steatosis is characterized by the presence of steatosis in hepatocytes [1], which leads to the development of fatty liver [2]. It is strongly associated with obesity, insulin resistance, and type II diabetes [3]. They are major risk factors of non-alcoholic hepati
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br GPR is a class A
2022-04-02
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine pac 1 which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell signa
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Fig summarizes the underlying mechanism of SB on
2022-04-02
Fig. 7 summarizes the underlying mechanism of SB on inhibiting inflammation and maintaining epithelium barrier integrity in the TNBS-induced colitis model. Our findings not only explained the protective effect of SB on colon health, but also provided evidence that GPR109A likely constitutes a valid
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Finally we investigated if calpain
2022-04-01
Finally, we investigated if calpain truncation affects GlyT1 turnover and trafficking. To simulate calpain cleavage at the T602/T603 and G626/S627 sites we constructed GlyT1 transporters missing the last 12 and 36 amino acids. Since the 36 amino LX7101 HCL truncation also removes all C-terminal ant
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TXA has been shown to be a competitive
2022-04-01
TXA has been shown to be a competitive antagonist on the GABAA receptor and potentially also the glycine [7], [12], [15] receptor. Furtmuller et al. showed that TXA right-shifted the GABA CRC by one order of magnitude [7], while in our study TXA similarly right-shifted the GABA EC50 value from 0.33
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With taurine or other molecules that might be
2022-04-01
With taurine, or other molecules that might be transported by Eaat2, an important area of research will be how such a chemical regulates sleep. Indeed, taurine has been described to act on the nervous system in disparate ways — it can act as an inhibitory neurotransmitter, but also has a well-charac
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br Methods br Results and
2022-04-01
Methods Results and discussion Protein analysis of commonly used cell lines (C6, D54-MG, U87, U251 and STTG1) reveals high AS1842856 of SXC (Cho and Bannai, 1990, Ye et al., 1999, de Groot et al., 2005, Lyons et al., 2007, Savaskan et al., 2008). Since protein expression can be altered over t
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The role of the ER EK variant which is associated
2022-04-01
The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of protein phosphatase inhibitor levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism mi
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br During cardiac ischaemia a decrease in
2022-04-01
During cardiac ischaemia, a decrease in GJ coupling is observed, which results in slower conduction of electrical impulses and a higher risk of arrhythmias.[13], [20] In Huntington’s disease an increase in the x gal of 5 Cxs was observed in the astrocytes in the brain, suggesting an adaptive prot
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br Materials and methods br Results br Discussion The curren
2022-04-01
Materials and methods Results Discussion The current study validates a key role for GAL3 receptors in consummatory drive for sucrose, saccharin, and most notably ethanol intake in mice. We show that alcohol preferring mice drink less ethanol compared to wildtype mice when treated with the G
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br Introduction Farnesoid X receptor FXR is a
2022-04-01
Introduction Farnesoid X receptor (FXR) is a bile Silvestrol regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that are
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The overall very satisfactory potency profile of compounds a
2022-04-01
The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic CCK Octapeptide, non-sulfated core in order to improve affinity to FFA1. The agonist activity in this series appears to
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To understand the impact of alterations in brain zinc
2022-04-01
To understand the impact of alterations in CBiPES hydrochloride synthesis zinc homeostasis, the role of Zn2+ as a neurotransmitter has to be appreciated. Certain regions of the brain including the neocortex and hippocampus harbour so-called “zincergic” (or “gluzinergic”) neurons, where Zn2+ is co-re
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