• (E)-2-Decenoic acid receptor Congenital Gcgr mice exhibit in

  2021-10-28

  

  Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific (E)-2-Decenoic acid receptor impairs glucose control in these mice [6]. In addition, the FGF21 an

• br Materials and methods br Contributors br Acknowledgements

  2021-10-28

  

  Materials and methods Contributors Acknowledgements This work was funded by the Ministry of Human Resources and Social Security, Shanxi Province [(2010)255], by a Shanxi Scholarship Council of China, and supported by a grant from the Alzheimer Society UK. The authors declare no conflict of

• Activation of FXR or TGR inhibits inflammatory

  2021-10-28

  

  Activation of FXR or TGR5 inhibits inflammatory response via repressing NF-κB activity [1]. FXR is not expressed or expressed at a very low level in macrophages [45] (data not shown), but highly expressed in hepatocytes. In contrast, TGR5 is expressed in macrophages but not in hepatocytes. Our data

• In the previous paper we described the design and synthesis

  2021-10-28

  

  In the previous paper, we described the design and synthesis of tricyclic thiazoles as FBPase inhibitors, and a series of SAR studies led to the identification of phosphate 3 and difluoromethylenephosphonate 4 exhibiting potent FBPase inhibitory activities (IC50=13, 47nM, respectively) (Fig. 2). In

• On the other hand Li Zhang et

  2021-10-28

  

  On the other hand, Li+ (Zhang et al., 1996) and Ca2+ (Gizak et al., 2004) cations inhibit FBPases. However, in the case of Ca2+, the inhibition is attributed solely to the muscle isozyme which is over 100 times more susceptible to the cation action than the liver isoform (Gizak et al., 2004). At the

• Next we aimed to investigate if the cardiac apoptosis

  2021-10-28

  

  Next, we aimed to investigate if the cardiac apoptosis induced by CO-HFD, LA, T1DM or hyperglycemia involves up-regulation and activation of Fas/FasL-mediated cell death and if such effects are mediated by ROS and/or Ca+2/calcineurin/NFAT signaling axis. Similar to previous reports, [8], [9], [10],

• Recently results obtained by our group have demonstrated

  2021-10-28

  

  Recently, results obtained by our group have demonstrated that hEECs are able to secrete NPY into the extracellular medium and that this peptide can induce an increase in the [Ca]i of these cells (Jacques et al., 2003b). In light of these results and those obtained in this study, we can speculate th

• Based on the inhibitory potency of C

  2021-10-28

  

  Based on the inhibitory potency of C646 for HDAC6, we monitored α-tubulin acetylation; an HDAC6 substrate. C646 treatment provided pronounced inhibition of α-tubulin acetylation after both 6 and 20h of incubation, which argues against HDAC6 inhibition by C646 in RAW264.7 cells. The observed effect o

• This crosstalk may be responsible for the beneficial effects

  2021-10-27

  

  This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on LXR-623 pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of high-dose ranitidin

• br Experimental br Acknowledgements This work was financiall

  2021-10-27

  

  Experimental Acknowledgements This work was financially supported by Ministry of Knowledge and Economy (10032113) and Ministry of Education, Science and Technology (20100000297). Introduction To ensure accurate chromosome segregation, cohesion between sister chromatids must be maintained u

• br GSK The GSK family

  2021-10-27

  

  GSK-3 The GSK-3 family is highly conserved throughout evolution and is encoded by two genes, GSK-3α and GSK-3β, which are located in chromosomes 19q13.2 and 3q13.3 in human, respectively. Both GSK-3α and GSK-3β proteins exist in a variety of tissues with the highest levels found in Nogo-66 (1-40)

• Because of its role in the cleavage of

  2021-10-27

  

  Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i

• According to its major function as master regulator of

  2021-10-27

  

  According to its major function as master regulator of BA homeostasis, FXR has been shown to have a specific tissue distribution; it is expressed along the entire gastrointestinal tract with a peak in the liver and ileum, as well as in the kidney, and adrenal glands [30], [66], [135]. Low FXR expres

• In order to understand the determinants

  2021-10-27

  

  In order to understand the determinants of high affinity of with amide side chain, an X-ray crystal structure of human liver FBPase in complex with was determined (). The position of phosphonate group and tricyclic scaffold of is similar to those of with no side chain, which suggests the formati

• In addition to indoles two

  2021-10-27

  

  In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic PF-03814735 australia side chain to prepare compound (). The extension of th

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