• To develop novel EPAC inhibitors

  2020-05-26

  

  To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock

• To further define the importance of CYP A

  2020-05-26

  

  To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations. H

• Since ET was discovered first and showed

  2020-05-25

  

  Since ET-1 was discovered first and showed a wide variety of actions not only on the cardiovascular system but also on various other tissues, much information has accumulated on ET-1 compared with the two other peptides. The method for measurement of ET-1 levels in plasma or various tissues by means

• Z-IETD-FMK Although CCR expression clearly identifies MBC pr

  2020-05-25

  

  Although CCR6 expression clearly identifies MBC precursors within the GC, we found that the expression of this chemokine receptor by responding Z-IETD-FMK was not required for MBC differentiation and had no detectable impact on the GC subsets analyzed in this study. Although this is in agreement wi

• br Conflicts of interest br Acknowledgements This

  2020-05-25

  

  Conflicts of interest Acknowledgements This work was supported by the Swiss National Science Foundation No 31003A-179400 to AO. We thank Dr. Thierry Langer, University of Vienna and Inte:Ligand GmbH, for providing the LigandScout Software, and Dr. Daniela Schuster, Paracelsus Medical Universit

• br Conformational Activation of APC C

  2020-05-25

  

  Conformational Activation of APC/C Enables Binding to the Coactivator CDC20 APC/C comes to life by binding a coactivator. This is controlled in part by phosphorylation and APC/C conformational changes that expose the Bicalutamide for the C box and IR tail of the coactivator. In interphase when m

• br E E backside interaction The E possesses an important

  2020-05-25

  

  E3–E2 backside interaction The E2 possesses an important regulatory interface which is termed its backside as it is opposite to the catalytic cleft that bears the active-site cysteine forming the thioester with SUMOD. This backside site interacts noncovalently with a scaffold SUMOB and was origin

• In addition to demonstrating the importance of DNMTs we

  2020-05-25

  

  In addition to demonstrating the importance of DNMTs, we show that TGFβ1 differentially regulated DNMTs, and that TGFβ1 is both necessary and sufficient to induce lineage conversion of hepatocytes into MLCs with phenotypes and multipotency resembling MSCs. Upon withdrawal of TGFβ1 on day 28, we obse

• br DAG kinase activity is

  2020-05-25

  

  DAG kinase activity is confined to specific cell compartments A number of reports demonstrating agonist-dependent translocation of DGKs to distinct membrane compartments suggest that DGK activity is restricted to localized DAG pools generated after activation of receptors. Perhaps the best eviden

• The DDR gene located on

  2020-05-25

  

  The DDR1 gene, located on chromosome region 6p21.33, encodes a transmembrane tyrosine kinase receptor involved in melanocyte anchoring through binding to collagen IV (Silva de Castro et al., 2010). So far, only three studies have been conducted on the association between DDR1 polymorphism and the r

• Introduction Tumor necrosis factor TNF is a

  2020-05-25

  

  Introduction Tumor necrosis factor (TNF) is a pro-inflammatory mediator with the capacity to induce apoptosis (Benderska et al., 2012). Recent reports have shown that TNF might trigger cell death, at least in part, by directly affecting the reorganization of the PD173955 cytoskeleton (Campos et al

• Cy5 Firefly Luciferase mRNA These data raised from human tis

  2020-05-22

  

  These data raised from human tissues suggested a potential link between TGF-β1 signaling and linear invadosome machinery that may explain TGF-β involvement in HCC progression and invasion. Using HCC cultured cells, we confirmed that TGF-β1 stimulation increases the production and secretion of collag

• In LPS treated BV cells we found that

  2020-05-22

  

  In LPS-treated BV-2 cells, we found that the upregulated CysLT2R was translocated into the nucleus. The nuclear localization of CysLT2Rs in microglia has not been reported previously. It is known that CysLT1Rs in endothelial 939 translocated to the nucleus in a ligand-independent manner after ische

• br Materials and methods br Results and discussion br Acknow

  2020-05-22

  

  Materials and methods Results and discussion Acknowledgements This study was supported by the Open Project Program of the Key Laboratory of Mariculture & Enhancement of Zhejiang Province (No. 2016KF003), the Key Project of Zhejiang Province (No. 2016C02055-7), and the International Science

• The current study showed that the

  2020-05-22

  

  The current study showed that the tested nonselective COX inhibitors potentiated the neuronal (EFS) and endothelial (ACh)-dependent relaxation of rat corpus cavernosum. Indomethacin was the most effective among them in potentiating EFS-induced relaxation. Diclofenac was the most effective in potenti

15462 records 862/1031 page Previous Next First page 上5页 861862863864865 下5页 Last page