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Currently ursodeoxycholic acid UDCA is the only recommended
2022-01-27
Currently, ursodeoxycholic Pridinol Methanesulfonate synthesis (UDCA) is the only recommended and widely used drug in the treatment of CFLD. However, the clinical efficacy of UDCA is controversial. The most recent Cochrane review only identified a small number of trials assessing the effectiveness o
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br Computational details and modeling All calculations were
2022-01-27
Computational details and modeling All calculations were performed using the density functional B3LYP [34] method, implemented in Gaussian03 program [35]. The structures of reactants, transition states, intermediates, and products were optimized using the 6-31+G(d) basis set for the H, C, N, O an
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br Introduction The alternative splicing
2022-01-26
Introduction The alternative splicing of pre-mRNA is essential for generating multiple matured mRNAs from a single gene by selectively removing introns. Neural lose your own voice show many examples of regulated alternative splicing events, which produce structural changes in proteins important
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br Conclusion br Conflict of Interest JJH has collaborated w
2022-01-26
Conclusion Conflict-of-Interest JJH has collaborated with several different pharmaceutical companies during the last 30 years; is currently receiving speaker honoraria from NovoNordisk and MSD and is on advisory boards for NovoNordisk. The author is currently supported by an independent grant
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The second patient had a homozygous substitution
2022-01-26
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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The urea derivatives a e were obtained from
2022-01-26
The urea derivatives 7a–e were obtained from 1-(3-phenoxybenzyl)-piperazine (6) by reaction of isocyanate, or triphosgene and subsequent reaction of produced carbamoyl chloride with the amine RH as shown in Scheme 2. The imidazole urea 7g was prepared by reaction of 6 with 1,1′-carbonyldiimidazole.
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Among the various epigenetic mechanisms involved in
2022-01-26
Among the various epigenetic mechanisms involved in EwS pathogenesis, we focused on the PRC enzyme EZH2, since it is a direct target of EWSR1-FLI1 and a critical mediator of malignant cell growth.24, 30 Our observation that the inhibition of EZH2 in GD2neg EwS 87 6 induces GD2 expression leads us to
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The EZH overexpression group exhibited upregulated CEP expre
2022-01-26
The EZH2 overexpression group exhibited upregulated CEP55 expression but downregulated methylation, suggesting that changes in EZH2 expression in lung adenocarcinoma result in differences of CEP55 methylation and expression. Moreover, according to TCGA database and GSE27262 chip data, CEP55 expressi
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br Conclusion In this research
2022-01-26
Conclusion In this research we have successfully formulated a PEGylated liposomal formulation encapsulating IRL-1620. The liposomal nanocarriers loaded with IRL-1620 were characterized for their particle size, PDI, zeta potential, and loading efficiency. We established that the treatment with IRL
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br Drugs approved or in development To date three drugs
2022-01-26
Drugs approved or in development To date, three drugs: RAL (MK-0518), EVG (GS-9137) and DTG (GSK1349572) [104], have been approved by the FDA. Their structures are shown in Fig. 5. DTG is under development by GlaxoSmithKline (GSK), and studies have shown DTG to be effective in patients with resis
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Compounds and were evaluated for their pharmacokinetic prope
2022-01-26
Compounds and were evaluated for their pharmacokinetic properties in rats and the results are summarized in . Following intravenous (IV) administration, both compounds displayed low clearance (CL), short half-lives (t) and low volumes of distribution (V). When dosed orally as a solution, exposure wa
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In various models histamine has been
2022-01-26
In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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Based on our results we propose three possible mechanisms
2022-01-26
Based on our results, we propose three possible mechanisms of HER2 loss after trastuzumab-based therapy (Fig. 3). The first possibility is a result of the differential effects of treatments on clonal subsets. In breast cancer, such selective pressure has been suggested to preferentially eradicate HE
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We demonstrated that bilirubin the product of heme
2022-01-26
We demonstrated that bilirubin, the product of heme metabolism by HO-1, exerted a potent suppression of NADPH oxidase activity (Fig. 2B). Different from the down-regulation of NADPH oxidase subunit by HO-1 induction in macrophages [24], the protein levels of the NADPH oxidase subunits in vascular en
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The rationale for developing HDACi as anticancer agents
2022-01-26
The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and S-Adenosylhomocysteine receptor arrest of cancer cells 1, 2, 3. HDACi have been used in the t
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