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br Acknowledgments br The design of
2019-12-26

Acknowledgments The design of polyaromatic molecules able to bind to DNA is of significant importance for the development of anticancer and fluorescent imaging agents. Among them, 1,8-naphthalimide derivatives have received significant attention and have been extensively investigated for their
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The following is the supplementary data
2019-12-26

The following is the supplementary data related to this article. Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) to produce phosphatidic CID 2745687 (PA) (Baldanzi, 2014, Goto et al., 2006, Merida et al., 2008, Sakane et al., 2007, Topham and Epand, 2009). To date, t
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br Endothelial mechanotransduction br Apoptosis br Death ass
2019-12-24

Endothelial mechanotransduction Apoptosis Death associated protein kinase Conclusion DAPK is localized to the UNC2025 synthesis network, and promotes actomyosin contractility. DAPK stabilizes stress fibers by phosphorylation of MLC (Bialik et al., 2004, Kuo et al., 2003). In endothelial
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To better understand Wolbachia s
2019-12-24

To better understand Wolbachia’s dependence on these enzymes, RNAi experiments targeting these transcripts will be required to examine the consequences of their down-regulation on Wolbachia in the different tissues of the parasite. Initial studies have shown that decreases in Bm-cpl-3 and Bm-cpl-6 t
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Acidic substituents showed moderate biochemical activity
2019-12-24

Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic biotin-LC-LC-tyramide were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their bi
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We performed three baseline scans in
2019-12-24

We performed three baseline scans in two baboons and one blocking study by administering 1 mg/kg (i.v) meloxicam 30 min prior to [C]TMI injection (injected activity 175.75 ± 18.5 MBq, mass of unlabeled TMI blood phenylephrine hydrochloride barrier (BBB) and retained in brain with a somewhat heterog
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The collagen field undoubtedly regains attractiveness with
2019-12-24

The collagen field undoubtedly regains attractiveness with the emergence of new concepts (cell niche, regulation of growth factor bioavailability, mechanotransduction, cell microenvironment sensing) and new tools to investigate their in vivo functions (atomic force microscopy (AFM), second harmonic
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Prostaglandin E receptor subtype EP is a transmembrane G
2019-12-24

Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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In conclusion we designed novel E inhibitors based on the
2019-12-24

In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and , we f
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br Materials and methods br
2019-12-24

Materials and methods Results Discussion In addition, the responses of CYP450s induced by metalaxyl are species-specific in the four cells. For example, metalaxyl lead to induction of CYP1A1, CYP1A2, and CYP2B1 in HepG2 cells, CYP1A2 and CYP2B1 in H4IIE cells, CYP1A1 and CYP2B1 in LMH cells
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br Results br Discussion The process by which
2019-12-24

Results Discussion The process by which MBCs differentiate from GC B cell precursors remains mostly uncharacterized, in large part because of the uncertainty surrounding the nature of the precursor 740 Y-P within the GC. The identification here of a distinct subset of GC B cells, CCR6+ LZ B c
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Nocodazole Several main strategies for targeting E s describ
2019-12-24

Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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The best characterized APC C substrates are recruited via va
2019-12-24

The best-characterized APC/C substrates are recruited via various linear motifs (e.g., D boxes, KEN boxes, and ABBA motifs) that serve as degrons, binding to distinct regions of the β-propeller domain of a coactivator (Figure 1, Figure 3B) (reviewed in [44]). In addition, D boxes also simultaneously
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br Introduction O Methylguanine DNA
2019-12-24

Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic
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Here we explored the relative
2019-12-24

Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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