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The findings in mice were echoed in the
2021-11-05
The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit
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A group of small molecule with
2021-11-05
A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-s
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br Introduction Migraine is a chronic neurological disorder
2021-11-05
Introduction Migraine is a chronic neurological disorder characterized by recurrent episodes of headache. It affects more than 10% of the population worldwide, resulting in a staggering amount of episodic disability, a substantial decrease in the quality of life and a concomitant loss in producti
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GSK1070916 synthesis Tyr phosphorylation of AnxA was first r
2021-11-05
Tyr23 phosphorylation of AnxA2 was first reported to be involved in endocytosis, particularly in the internalisation of the insulin receptor [20]. Phosphorylated Tyr23 seems to be necessary for the stable association of AnxA2 with endosomes, and for their early-stage transport [14]. The role of AnxA
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To our knowledge the putative
2021-11-05
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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br Results br Discussion The present findings outline a nove
2021-11-05
Results Discussion The present findings outline a novel regulatory mechanism for fasting-induced ketogenesis, which involves histamine release from mast Cy3 carboxylic acid (non-sulfonated) receptor into the hepatic portal system, H1 receptor-mediated stimulation of liver OEA biosynthesis, and
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Among the isoforms of heme oxygenases HO
2021-11-05
Among the 3 isoforms of heme oxygenases (HO-1, HO-2, and HO-3), HO-1 expression is inducible, and it catalyzes the degradation of heme to biliverdin, carbon monoxide (CO) and free Fe. The Fe is then stored in ferritin, limiting its ability to participate as a catalyst through the Fenton reaction and
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br Materials and methods br
2021-11-05
Materials and methods Results Discussion Dex has been shown to induce apoptosis in osteoblastic cell lines (MC3T3-E1, UAMS-32 cell) [24], [25]. Consistent with previous reports, we find high-dose Dex (1 or 5 μM) can induce apoptosis of MC3T3-E1 EPZ-6438 within 24 h as evidenced by Annexin
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Recent evidence suggests that HCA
2021-11-04
Recent evidence suggests that HCA2 can also mediate antineuroinflammatory effects [63]. Studies in this field were initiated when monomethyl fumarate, the metabolite of DMF, was shown to be an agonist of HCA2[5]. DMF at the same time was shown to not only have beneficial effects in the treatment of
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br Materials and methods br
2021-11-04
Materials and methods Results Discussion Nervous system disease is an important signal of AIDS deterioration (Rosca et al., 2012, Yilmaz et al., 2012). It is possible that HIV crosses the blood PFK-015 sale barrier or blood cerebrospinal fluid barrier into the central nervous system freely
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Recently several dual GLP GIP receptor
2021-11-04
Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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Pamidronate Disodium Moreover the ubiquitous expression of t
2021-11-04
Moreover, the ubiquitous Pamidronate Disodium of the OTR and GHSR was also observed in hippocampal and hypothalamic primary culture, indicating that this expression pattern is likely due to basal activity of these receptors. GPCR trafficking under control conditions has been linked to biased signal
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br Discussion According to the generally accepted notion whi
2021-11-04
Discussion According to the generally accepted notion which originated from the study of ATP-depleted cftr the changes in Ca2+ homeostasis induced by ATP depletion and leading to the activation of the Gárdos effect are due to the inhibition of Ca2+ pumping, and the subsequent entry of Ca2+ throu
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all-trans Retinal The advent of the genomic era
2021-11-04
The advent of the genomic era has allowed greater detailed investigation of enzymatic properties and has shown that specific enzyme activity is linked to the substrate utilization profiles of the isoenzymes [30], [31]. Not surprisingly, the functional four β-galactosidases from A. niger F0215 shared
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br Conclusion In summary a series
2021-11-04
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic cp-690550 motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent
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