• In conclusion starting from the weakly potent GSM exploratio

  2021-10-15

  

  In conclusion, starting from the weakly potent GSM , exploration of various spacer groups between the triazole ring and the aromatic Cisatracurium Besylate led to the discovery of a new series of potent gamma secretase modulators, with an improved drug-like profile—compared with the originally repo

• Recently accumulated evidence has revealed a

  2021-10-15

  

  Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu

• Moreover long term treatment of leukemia cells

  2021-10-15

  

  Moreover, long term treatment of leukemia cells with imatinib activates AKT, ERK and STAT5 signaling pathway and induce upregulation of EZH2 protein in patients with CML, Ph + ALL and human eosinophilic leukemia cell line (EOL-1 cells) [142]. So, resistance to tyrosine kinase inhibitor (TKI) imatini

• EZH interaction with HADC and HDAC through the

  2021-10-15

  

  EZH2 interaction with HADC1 and HDAC2 through the EED subunit is known to recruit histone deacetylases [113,114]. Given that PRC2-mediated repression of transcription may be partly dependent on the function of HDACs in specific cell contexts [115], the leukemia cell treatment with hydroxamic GTP-Bin

• Cell cell junction proteins were the

  2021-10-15

  

  Cell-cell junction proteins were the first upstream modules to be characterized as contact sensors through the Hippo pathway. These junctions may be divided in 2 categories: adherens and epithelial polarity junctions. The establishment of intercellular contacts involves the cadherin proteins present

• br References and recommended reading Papers of particular

  2021-10-15

  

  References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Introduction Male sexual maturation includes gonadal maturation, secondary sexual characteristics, and the attainment of reproductive capacity [1]. Male sexual di

• Our results show furthermore that

  2021-10-15

  

  Our results show furthermore, that higher concentrations of butyric Camptothecin additionally affect GSTP1 mRNA stability leading to a strongly reduced half-life. Concentration-dependent effects of butyric acid on RNA stability and cell signaling pathways involved in the regulation of GSTP1 express

• Like tBHQ and DEM treatment of Keap MEFs with

  2021-10-15

  

  Like tBHQ and DEM, treatment of Keap1+/+ MEFs with SFN increased the abundance of Hmox1 and Nqo1 mRNA, and this was blunted by LY294002 and MK-2206 (Figure 2C). However, unlike the situation with tBHQ and DEM, treatment of Keap1−/− MEFs with SFN did not increase further the elevated basal levels of

• GLP is an intestinal peptide hormone

  2021-10-15

  

  GLP-1 is an intestinal peptide hormone that is released by the gut following ingestion of food, particularly Doxorubicin and fats. Following its release, GLP-1 stimulates pancreatic β-cells to secrete insulin (Hirasawa et al., 2005, Covington et al., 2006). Originally, GLP-1 acted in a similar manne

• The compounds described in this paper were

  2021-10-15

  

  The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m

• Over expression of Glo can suppress inflammatory responses M

  2021-10-15

  

  Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial NS 1619 [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen expressi

• br Introduction The glucagon receptor

  2021-10-15

  

  Introduction The glucagon receptor (GCGR) is a G-protein-coupled receptor expressed mainly in the liver and kidney. Upon glucagon binding, it activates the stimulatory G protein (Gs) and increases cAMP level, subsequently transducing glucagon signaling involved in glucose, amino acids and lipid m

• Besides the described effects on gross locomotor function im

  2021-10-15

  

  Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t

• Here we used a designer receptors activated

  2021-10-15

  

  Here, we used a designer receptors activated exclusively by designer drugs (DREADD)-based chemogenetic approach in a novel Ghsr-IRES-Cre knock-in mouse line to test whether the activity of MBH GHSR neurons is required for the normal rebound food intake following fasting. We also used the Ghsr-IRES-C

• Ligand selectivity may directly be related to the

  2021-10-14

  

  Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This

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