• The combination of niacin with a selective PGD receptor anta

  2021-11-19

  

  The combination of niacin with a selective PGD2 receptor antagonist laropiprant, designed to circumvent the flushing side effect of niacin, has been evaluated in the HPS2-THRIVE study and showed no clinically meaningful benefit when administered in patients on top of statin therapy [41]. Our data su

• GPR A a G protein

  2021-11-19

  

  GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic Silodosin [[5], [6], [7]] and mediator of NEFA reduction [5]. As a mechanism of NEFA-lowering, it is recognized that activation of GPR109A leads to Gi-mediated

• Generally replacement of the aryl group was

  2021-11-19

  

  Generally, replacement of the aryl group was well tolerated, with tetrahydropyran () and hydroxyl () functionality providing potency equivalent to and . These substitutions had no effect on selectivity versus GlyT2 and taurine transporter (TauT)—no activity was observed at micromolar concentrations.

• The findings in mice were

  2021-11-18

  

  The findings in mice were echoed in the human studies, in which the effects of higher doses of LY3298178 caused greater weight loss than the selective GLP-1RA dulaglutide. In patients with T2DM, LY3298176 demonstrated meaningful weight loss after only four weeks of treatment. This was consistent wit

• Ligand selectivity may directly be related to the conformati

  2021-11-18

  

  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

• glucokinase inhibitor The structures of KDM A

  2021-11-18

  

  The structures of KDM4A revealed a Cys-His Zn(II) binding site that is close to the substrate binding spot, which bioinformatic analyses indicated was not present in any other histone demethylase subfamily. Therefore, an alternative method to inhibit the KDM4 family (95) would be to use compounds th

• The H R antagonist cimetidine Tagamet became the

  2021-11-18

  

  The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.

• The analytical approach for the simultaneous determination

  2021-11-18

  

  The analytical approach for the simultaneous determination of HA and its metabolites is complex. There are commercial kits that allow the determination of HA through ELISA and of its metabolites through radioimmunoassay (RIA) techniques. However, these immunological-based techniques do not allow sim

• br Concluding Remarks One of the remarkable features

  2021-11-18

  

  Concluding Remarks One of the remarkable features of Hippo signaling is its sensitivity to the cytoskeleton and mechanical forces. Progress has been made recently in identifying molecular mechanisms by which the cytoskeleton can influence Hippo signaling, but among the many outstanding questions

• Several bacterial functional pathways were

  2021-11-18

  

  Several bacterial functional pathways were observed after DON administration, of which signal transduction, metabolism and genetic information processing displayed the highest levels of enrichment. Importantly, these three pathways were reported to be closely associated with DON's toxicity. Many evi

• RI-1 Starting from the hypothesis that the linker portion

  2021-11-18

  

  Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [

• br Conclusion br Author contributions br

  2021-11-18

  

  Conclusion Author contributions Acknowledgements We thank gap junctions USC Center for Craniofacial Molecular Biology (CCMB) for their extensive guidance and teaching in biochemical techniques. We acknowledge Laurel Fisher, PhD for her contribution to statistical analysis of the data. We ac

• GSTP catalyzed reduction of Prdx enhances its peroxidase

  2021-11-18

  

  GSTP1-1 catalyzed reduction of Prdx6 enhances its peroxidase activity. Using standard NADPH/GR/GSH-coupled assays we used cell lysates from the transiently transfected teniposide to measure the influence of GSTP1 allelic variation on peroxidase activity. Specificity for detection of Prdx6 activity

• To the best of our knowledge this is the first

  2021-11-18

  

  To the best of our knowledge, this is the first study to examine functional GSTO1‐1 activity in the cornea. Therefore, comparative data for human or animals is not available. Moreover, we observed the nonspecific degradation of the GSTO1‐1 substrate 4NPG via an unknown mechanism, which was corrected

• Our last area of exploration was the

  2021-11-17

  

  Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th

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