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The NVC response in the diseased or aging brain may
2022-07-19
The NVC response in the diseased or aging monensin may be altered, including changes in both the chemical mediators of NVC, ion channel behaviour, and the dynamics of the vascular system. For example, in Alzheimer’s disease the production of NO is shown to be inhibited (Lourenço et al., 2014), hyper
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The role of GJs in liver
2022-07-19
The role of GJs in liver fibrogenesis was studied recently. Studies showed a significant decrease in liver fibrosis in Cx32 knockout mice compared to wild-type mice. Although the mechanism underlying this protective effect of Cx32 deletion is not clear, reduced oxidative stress was suggested as a po
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The second patient had a
2022-07-18
The second patient had a homozygous substitution within exon 6 (c.538C>T). The parents were heterozygous and showed no clinical or immunological defect. The mutation has been predicted to alter a potential exonic splicing enhancer (ESE) site. Therefore, exon 6 skipping could be explained by the ESE-
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br Declarations of interest br Founding information This wor
2022-07-18
Declarations of interest Founding information This work was partially supported by the New Energy and Industrial Technology Development Organization (NEDO) Japan [grant number P03043]; and Grants-in-Aid for Scientific Research [grant number 16H00738 to H.M.] from the Japan Society for the Prom
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The different NO stimulated and ODQ inhibited cNMP patterns
2022-07-18
The different NO-stimulated and ODQ-inhibited cNMP patterns in terms of absolute and relative magnitude and time course reported herein suggest distinct functional roles of cGMP, cCMP and cUMP. Therefore, it will be necessary to dissect cellular effects of these cNMPs in numerous cell systems. For t
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GPR has been implicated in neuropathic and inflammatory pain
2022-07-16
GPR55 has been implicated in neuropathic and inflammatory pain (Staton et al., 2008) and bone remodeling (Whyte et al., 2009). Thus delineating the pharmacology of this receptor and the discovery of selective agonists and antagonists merits further study and could lead to new therapeutics. Acknow
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br Materials and methods br Results
2022-07-16
Materials and methods Results Using an 84 gene Th1-Th2-Th3 cytokine profile, 17 genes were significantly up-regulated in PBMC one week post-marathon compared to pre-marathon samples (Table 1). Eight genes were down-regulated among various subjects but none consistently enough to achieve statis
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br Materials and methods br Results br Discussion GPR expres
2022-07-16
Materials and methods Results Discussion GPR35 expression has been identified within discrete regions of the nervous system, including the spinal cord [[43], [44], [45], [46], [47], [48]]. Importantly, GPR35 is expressed not only in neurons but also in spinal glial cells [43]. Unfortunately
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With this goal in mind
2022-07-16
With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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Based on work from our labs with mGlu
2022-07-16
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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A high throughput screening campaign of
2022-07-16
A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co
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Abnormal expression and higher activity
2022-07-16
Abnormal expression and higher activity of GLO I have been detected more in various tumor rvx mg than in normal cell samples., , , , , , , Among cancer cell lines, lung carcinoma cells frequently showed higher GLO1 activity. Human NSCLC cell line NCI-H522 cells possess high activity and expression
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A number of experimental data declare a tight interdependenc
2022-07-16
A number of experimental data declare a tight interdependence between the pathological changes of glutamate transport in Gambogic Acid and consequent alterations in glutamate transport and activity/expression of glutamate metabolizing enzymes in platelets (Aliprandi et al., 2005, Behari and Shrivas
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Rifampicin that is methyl piperazinyl
2022-07-16
Rifampicin, that is 3-[[(4-methyl-1-piperazinyl) imino] methyl]-rifamycin (Fig. 1), is a semisynthetic antibiotic drug. It is one of the most potent and broad drug against bacterial pathogens and tuberculosis [9]. In recent years, rifampicin has also been reported to have inhibitory effects on Taq R
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In summary this study shows that compound d has strong
2022-07-16
In summary, this study shows that compound 4d has strong clinical potential as an efficient GLP-1/GCGR agonist exhibits weight-lowering, lipid-regulation and diabetes-protective effects and plays an important role in the prevention and therapy of diet induced obesity and dyslipidemia. The present st
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