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Acute effects of FZ were not altered in GluR
2022-04-14
Acute effects of FZ were not altered in GluR-A−/− mice, thus providing a solid basis for comparing the effects of repeated drug administration. In addition, GluR-A subunit deficiency did not affect the basal behavior of saline-treated animals, despite the GluR-A−/− mice having been described as hype
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br Materials and methods br Results In
2022-04-14
Materials and methods Results In order to address the role played by the catalytic and the anticodon-binding domains of E. coli GluRS in cognate and non-cognate aminoacylation, the two domains (NGluRS: 1–314; CGluRS: 318–471) of E. coli were expressed and purified (Fig. 1b). Prior to assessing
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The potential therapeutic actions of GHSR in
2022-04-14
The potential therapeutic actions of GHSR in the central nervous system has been in the limelight lately. Peripheral administration of GHSR agonists have been shown to inhibit oxidative stress, apoptosis, proinflammatory cytokine production, microglia activation, mitochondrial dysfunction, and excit
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Recently accumulated evidence has revealed a close link
2022-04-13
Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu
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Following these discoveries the term ferroptosis
2022-04-13
Following these discoveries, the term ferroptosis was coined in 2012 [25], to describe this iron-dependent, non-apoptotic form cell death induced by erastin and RSL3. This discovery was accompanied by the development of the first small molecule ferroptosis inhibitor, termed ferrostatin-1, and the de
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br Materials and methods This is a retrospective case
2022-04-13
Materials and methods This is a retrospective case-controlled study. The cases were selected based on the presence or absence of preeclampsia. Women enrolled in the study delivered singleton pregnancies at our institution from June 2003 to July 2004. Preeclampsia is defined as elevated blood pres
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1080 6 br Hydroxyfarnesyl diphosphate was synthesised in thr
2022-04-13
12-Hydroxyfarnesyl diphosphate (6) was synthesised in three steps starting from commercially available (E,E)-farnesol (10) (Scheme 5). Chlorination of 10 gave farnesyl chloride (11) in a quantitative yield, which was carried forward without purification. The following step was a selenium dioxide-c
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Cefpodoxime Proxetil It is an exciting time for translationa
2022-04-13
It is an exciting time for translational histamine research, since preclinical studies show potential value for histamine receptor ligands. As reviewed above, there are several concerns for future studies of histamine and its role in the CNS. 1) Because of the availability of HDC-Cre mice (Williams
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Other N substituted carboxamide oxy pyridine derivatives a
2022-04-13
Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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br Modulators of the GUCY C cGMP PDEs
2022-04-13
Modulators of the GUCY2C/cGMP/PDEs signaling pathways for CRC prevention and therapy (pre-clinical and clinical development) Several modulators of the GUCY2C/cGMP/PDEs signaling pathways, including GUCY2C agonists and PDEs inhibitors, have been developed and explored as chemopreventive agents for
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In our studies the EC values for long chain unsaturated
2022-04-12
In our studies, the EC50 values for long-chain unsaturated fatty acids added to the short form of human GPR120 receptor (BC101175), were higher than the EC50 values previously reported (Hirasawa et al., 2005) for the long form of GPR120 (NM_181745), which was co-expressed with Gα16 protein.(Table 2)
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Armed with this knowledge we
2022-04-12
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 simple p
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br Regulation of Glu transporters The pivotal role of Glu
2022-04-12
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino tetraethylammonium synthesis calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These
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br Acknowledgments This work was supported
2022-04-12
Acknowledgments This work was supported by the NIH (R01DK103884 to JMZ, R01DK100659 to JKE, and F32DK104659 and K01DK111644 to CMC), the Diana and Richard C. Strauss Professorship in Biomedical Research, the Mr. and Mrs. Bruce G. Brookshire Professorship in Medicine, the Kent and Jodi Foster Dist
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Pyridone 6 br Introduction Ghrelin is a
2022-04-12
Introduction Ghrelin is a 28-amino Pyridone 6 peptide mainly produced in the stomach and small intestines with the kidneys, placenta, and pancreas contributing to miniscule amounts of circuiting ghrelin [1]. Ghrelin exists in circulation in two major forms: acyl ghrelin (AG) and desacyl ghrelin
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