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In the a first in vitro indication
2022-03-29

In the 2003, a first in vitro indication of modulation of FXR expression in CRC showed that FXR expression was absent in undifferentiated colon carcinoma cell line SW480, while it was progressively increasing along with the degree of cell differentiation in Caco2 and HT29 cells, and its transcriptio
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br Discussion and concluding remarks FPR is considered
2022-03-29

Discussion and concluding remarks FPR1 is considered to be a promising drug target for treating inflammatory and immunological diseases. Thus, natural compounds that could block and/or regulate FPR1 activity may be an important source of novel therapeutics for modulating inflammatory processes. H
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Canonical and non canonical Wnt signaling
2022-03-29

Canonical and non-canonical Wnt signaling pathways play essential roles in various cellular activities, including cell fate determination, proliferation, migration and gene expression [57]. The canonical Wnt pathway (β-catenin dependent pathway), is activated by the binding of Wnt ligands, leading t
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A common feature of ferroptosis is
2022-03-29

A common feature of ferroptosis is the iron-dependent accumulation of lipid-ROS and the subsequent depletion of polyunsaturated fatty AMN-107 phospholipids (PUFA-PLs) [118]. The PUFA chains of membrane lipids are more susceptible to both enzymatic and non-enzymatic oxidation, which results in PUFA f
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br Drug design Over the past decades
2022-03-28

Drug design Over the past decades, the development of synthetic, direct fXa inhibitors has undergone four phase. Although these fXa inhibitors possess various scaffolds, most of them bind to the active site in a characteristic l-shaped conformation. In other word, they have a three-component syst
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summarizes FAAH inhibition data for a series of benzofuran
2022-03-28

summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibitio
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To enhance the impact of GD as an immune target
2022-03-28

To enhance the impact of GD2 as an immune target in this cancer, we investigated a novel strategy to upregulate expression on the cell surface of EwS cells by an epigenetic agent, based on the following rationale. Biosynthesis of GD2 and other gangliosides during organ development is driven by stage
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insulin signaling br Conflict of interests br Acknowledgemen
2022-03-28

Conflict of interests Acknowledgements This work was supported by the National Institutes of Health grants HD058577 and ES01678 to Kirill Kiselyov. We thank Sreeram Ravi for technical support. We also thank Mike Myers at the University of Pittsburgh Cancer Institute Flow Cytometry Facility.
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br Methods br Results We have previously used
2022-03-28

Methods Results We have previously used ß-hex assays in HeLa N1-Methyl-ATP synthesis to study the role of lysosomal exocytosis on transition metal clearance and the effects of transition metals on lysosomal exocytosis [26], [29], [40]. ß-hex is a lysosomal enzyme, the delivery of which to the
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Additionally to their peripheral effects evidence
2022-03-28

Additionally to their peripheral effects, evidence indicate a role for ETs in the central nervous system (Mosqueda-Garcı́a et al., 1993). Indeed, using Northern blot analysis and in situ hybridization it has been shown the presence of immunoreactive ET of non-vascular origin and of neuronal location
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The more important effect of pitolisant is related to
2022-03-28

The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced WIN 64338 hydrochloride release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcolep
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Recent studies have also identified additional proteins that
2022-03-28

Recent studies have also identified additional proteins that could act as scaffolds and promote the interaction of core Hippo pathway components. APC, which is best known as a key component of the β-catenin destruction complex, was observed in mammalian apexbt calculator to have an additional funct
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br Experimental br Results br Discussion
2022-03-28

Experimental Results Discussion In this study, we performed molecular docking analysis and in vitro studies to determine whether genistein binds to HIF-1α in BC worldwide distributors and identify the residues involved in this interaction. We found that some functional groups (residues) mi
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br Multiple sclerosis MS is an immune mediated
2022-03-28

Multiple sclerosis MS is an immune-mediated disease of the human CNS with a pathological signature featuring immunocyte infiltration, altered cytokine production, oligodendroglial degeneration, astrogliosis, microglial activation, multifocal demyelination and axonal degeneration (Schipper, 2004b
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Based on pharmacophore modeling a good
2022-03-28

Based on pharmacophore modeling, a good HDAC inhibitor has at least three sides/regions: the attachment side of the Zn2+ cofactor/HDAC active site (Zn2+ binding group/ZBG), hydrophobic cap (CAP) and linker containing connecting unit (CU) with electronegative groups (Mohan et al., 2011, Rossi et al.,
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