• In summary we have identified a series of

  2021-03-11

  

  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

• EPAC activation in VSMCs and ECs reverses

  2021-03-11

  

  EPAC activation in VSMCs and ECs reverses several processes involved in the development of in-stent restenosis. Of particular relevance is the ability of EPAC1 to induce SOCS3 gene expression, as SOCS3 exerts multiple protective effects in both cell types, while immunohistochemical studies have show

• br Conclusions Nanoparticles can be used to modulate the

  2021-03-11

  

  Conclusions Nanoparticles can be used to modulate the catalytic activity of various industrially and clinically useful enzymes, as well as pH, temperature and storage stabilities, which will enable the process to occur more efficiently and less costly. The interaction between an enzyme and nanopa

• Two GPCR subtypes of interest in the myocardium

  2021-03-11

  

  Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy

• br Results br Discussion PKR is activated

  2021-03-11

  

  Results Discussion PKR is activated by viral dsRNA and exerts its antiviral effect through phosphorylation of eIF2a. Because eIF2a phosphorylation leads to attenuation of protein synthesis, many viruses have evolved mechanisms to block or suppress PKR activation. Some viruses use alternative t

• An important role for the precursor molecule of the

  2021-03-11

  

  An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener

• br Substoichiometric substrate modification E ligases cataly

  2021-03-11

  

  Substoichiometric substrate modification E3 ligases catalyze the rapid transfer of the SUMOD from the E2 enzyme to the substrate. By definition, enzymes are recycled in the reaction, allowing multiple rounds of substrate modification by a single enzyme. Thus, enzymes function at substoichiometric

• We also observed reduced insulinotropic effects after intrav

  2021-03-11

  

  We also observed reduced insulinotropic effects after intravenous administration of both GLP-1 and GIP with atropine, whereas no inhibition was observed by atropine of the direct effects of GLP-1 and GIP action on beta-cells in the islet experiments. This suggests that the reduction in circulating i

• br Development of the double strand break repair model for

  2021-03-11

  

  Development of the double strand break repair model for meiotic recombination Meiotic recombination was first described by Frans Alfons Janssens using GW9662 in the salamander Batracoseps attenuatus in 1909 [21] and then further elaborated at the genetic level in Drosophila by Thomas H. Morgan [

• br Enzymes repairing alkylated DNA br Induction

  2021-03-11

  

  Enzymes repairing alkylated DNA Induction of the Ada regulon Methylated Ada is a strong activator for ada and alkA promoters. Although much weaker than the methylated form, unmethylated Ada acts alone as an activator for ada and alkA promoters. In contrast, the unmethylated protein present in

• We also found a significantly inverse correlation

  2021-03-10

  

  We also found a significantly inverse correlation of OPRM1 CpG2-4 methylation level with HDL-C in Han male controls. Lipids are known to involve the inflammation pathway, Aβ formation and stability of neuron, whereby their abnormalities have been shown to increase the risk of AD [39], [40], [41]. HD

• Yang et al investigatedPsoralidin a coumestan derivative

  2021-03-10

  

  Yang et al. investigatedPsoralidin 39, a coumestan derivative isolated from the seed of Psoralea corylifolia, regarding its effects on IR-induced pulmonary inflammation. Psoralidin 39 inhibited the IR-induced COX- 2 expression and PGE(2) production through regulation of PI3K/Akt and NF-κB pathway. A

• As the communications interface was developed

  2021-03-10

  

  As the communications interface was developed by two separate organisations with differing software processes and tools, a modular approach to the safety case was deemed appropriate. The modular approach related the communications interface safety argument to the safety arguments for both the ACS an

• br Introduction The cys loop ligand gated

  2021-03-10

  

  Introduction The cys-loop ligand gated ion channels (LGICs) are membrane-bound proteins mediating fast transduction from chemical to electrical signals at neuronal synapses and neuromuscular junctions [1], [2]. Each subunit that makes up the pentameric LGIC architecture possesses a dicysteine bri

• The same reservoir of genes is involved in

  2021-03-10

  

  The same reservoir of Olcegepant receptor is involved in fusions in all types of cancers, which predominantly encode kinases and transcriptional factors [102]. This makes fusion genes potential pan-cancer targets, and renders tumor categorization based on genetic profiling therapeutically reasonabl

14159 records 659/944 page Previous Next First page 上5页 656657658659660 下5页 Last page