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As an endogenous negative modulator CRBN
2021-02-25
As an endogenous negative modulator, CRBN inhibits AMPK’s activation (phosphorylation of Thr172) by directly binding to the α-subunit of AMPK, disrupting γ-subunit recruitment to the AMPK complex (Lee et al., 2011, Lee et al., 2013). In our study, we did not focus on AMPK activation, since only a si
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br Materials and methods br Results br Discussion Ubiquitina
2021-02-25
Materials and methods Results Discussion Ubiquitination is an important eukaryotic process that defines the fate of proteins and their functionality. It has multiple roles in cell survival, differentiation and development (Glickman and Ciechanover, 2002). Ubiquitination is usually known as
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The second DDR binding partner
2021-02-24
The second DDR1-binding partner identified here, Shp-2, which was not found in the two-hybrid screen but using a bioinformatics approach, is also a mediator of cell migration. Since Shp-2 has two SH2 domains, as well as phosphotyrosine phosphatase enzymatic activity and two C-terminal tyrosines targ
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Ligand independent constitutively active variants have also
2021-02-24
Ligand-independent, constitutively active variants have also been found in receptors with associated tyrosine kinases. In approximately 60% of patients harboring inflammatory hepatocellular adenomas (IHCAs), these adenomas have been caused by small in-frame deletions in the cytokine-binding domain o
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Tacrine amino tetrahydroacridine I Fig was the
2021-02-24
Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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Here we examined whether Intracellular ER may
2021-02-24
Here, we examined whether Intracellular ER may mediate Cd-induced ovarian cancer proliferation. To determine this relationship, we used ICI 182,780 as a general inhibitor of ERα and ERβ. The results suggest a metalloestrogenic effect of Cd in ovarian cancer cell lines. Inconsistency with our results
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We report our experience using conventional cytogenetic anal
2021-02-24
We report our experience using conventional cytogenetic analysis, FISH using EWSR1 break-apart probes, RT-PCR, and Sanger sequencing to detect characteristic translocations in a total of 32 patients with ES diagnosed at Texas Children's Hospital over a 5-year interval. Materials and methods Re
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In summary we have identified a series
2021-02-24
In summary, we have identified a series of amides as ERRγ agonists with suitable potency for further development. Our SAR studies of this chemotype identified SR19881 as the most potent full agonist of ERRγ with an EC=0.39 μM in a binding assay and an EC=4.7 μM in a cell-based assay. SR19881 was als
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Interest in the PGE EP pathway
2021-02-24
Interest in the PGE2/EP4 pathway is increasing given its diverse capability of regulating central nervous system activity [13]. EP4 has a protective function by reducing cerebral injury and improving functional outcome after stroke [14], and in suppressing odanacatib inflammation [15]. The EP4 rece
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Compound was prepared from chloroindole by acylation to
2021-02-24
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole Apoptozole derivative (). Derivatives and were
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The elastase induced injury model has been
2021-02-24
The elastase-induced injury model has been shown to produce airspace enlargement, and increases in lung volume and compliance that are similar to those observed in human patients (Hantos et al., 2008, Hamakawa et al., 2011). Thus, this model, which has been used to study emphysema, should be adequat
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Introduction Proteins play an important role in cellular fun
2021-02-24
Introduction Proteins play an important role in cellular functions; however, being and remaining properly folded is necessary for their function. Understanding the stability of the protein is necessary to investigate the folding of proteins, as well as their conformation, functions and interactions
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Inappropriate heme metabolism has been linked to
2021-02-24
Inappropriate heme metabolism has been linked to several neuropsychiatric disorders. In the hippocampi of Alzheimer's disease (AD) patients, for example, heme was found to binds intracellular amyloid β (Aβ), resulting in reduced heme bioavailability and its functional deficiency (Atamna and Frey, 20
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Despite robust translation of GA only
2021-02-24
Despite robust translation of GA, only small amounts of GR and GP were translated in cultured YO-01027 and chick embryo spinal cord neural cells from the 75 copies of G4C2 in monocistronic constructs. Interestingly, GA is also the most common dipeptide found in autopsy tissue in FALS patients with
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LY3009104 High concentrations of kC may
2021-02-24
High concentrations of 7kC may also arise from dietary intake of processed cholesterol-rich food, likely favoring or worsening inflammatory bowel disease (IBD) [5,13]. Furthermore, IBD has been associated with a dysregulation of colonic 11β-HSD expression, exhibiting increased 11β-HSD1 and decreased
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