• Recent findings of us suggest that compounds that inhibit

  2022-03-04

  

  Recent findings of us suggest that compounds that inhibit both FAAH and TRPV1 may be more efficacious in pain relief than those targeting only one such protein. As continuation of our efforts to identify new molecules able to target simultaneously both FAAH and TRPV1 receptors, we hypothesized that

• br Sources of funding This

  2022-03-04

  

  Sources of funding This work was supported by grants from the Canadian Institutes of Health Research (CIHR) (No. MOP-111096) and from the Heart and Stroke Foundation of Canada awarded to Dr. Danielle Jacques. Disclosures Acknowledgments Introduction A large number of epidemiological, hu

• The H R antagonist cimetidine

  2022-03-03

  

  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.

• An isoflavone type secondary metabolite Glabrescione B GlaB

  2022-03-03

  

  An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th

• br Experimental br Acknowledgements This work

  2022-03-03

  

  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 Acknowledgements br Introduction The glutathione S transf

  2022-03-03

  

  Acknowledgements Introduction The glutathione S-transferase (GST, EC 2.5.1.18) family of multifunctional enzymes plays a particularly important role in cellular detoxification [1]. Over-expression of the GSTP1 isoform characterizes many human tumor cell lines derived from stomach, brain and co

• Since KYNA concentrations are increased by aerobic exercise

  2022-03-03

  

  Since KYNA concentrations are increased by aerobic exercise training, we have investigated if it plays a role in peripheral tissue metabolism. Here we show that KYNA regulates adipose tissue energy homeostasis through activation of Gpr35. Activation of this network stimulates the expression of lipid

• Similar to GPR A activation of G protein

  2022-03-03

  

  Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic ibmx receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al., 1963, Houghton

• It is well known that

  2022-03-03

  

  It is well known that the expression of GPR109A is regulated under physiological and pathological conditions. We previously found that GPR109A expression in islet beta-cells increased with age and was up-regulated by interferon-γ (Li et al., 2011). GPR109A levels in Min6 and INS-1E islet beta-cells

• Crystal structure of CD LEL have revealed the

  2022-03-03

  

  Crystal structure of CD81-LEL have revealed the head sub-domain to be implicated in binding to HCV (Kitadokoro et al., 2001). In a study using African green monkey CD81, T163A, F186 L, E188K and D196E mutations disrupted HCV E2 binding (Higginbottom et al., 2000). In our docking studies, T163 and D1

• Since the isoflavone emerged as privileged scaffold in Hh in

  2022-03-02

  

  Since the isoflavone emerged as privileged scaffold in Hh inhibition, based on molecular modeling predictions and prior studies [17,22], here we designed a number of isoflavones able to interact preferentially with the Smo receptor or the Gli protein. Molecules were synthesized by means of a novel s

• Inhibitors of the G rdos effect include the Ca channel

  2022-03-02

  

  Inhibitors of the Gárdos effect include the Ca2+-channel blocker nitrendipine with an IC50 of ∼103nM (Ellory et al., 1992, Ellory et al., 1992); its mode of action is likely to be from direct blockage of K+ flux through the Gárdos channel (Ellory et al., 1992, Ellory et al., 1992), and the peptidic

• Studies regarding secretase nowadays aim at elucidating how

  2022-03-02

  

  Studies regarding γ-secretase nowadays aim at elucidating how APP is recognized and recruited. It has been suggested based on coarse-grained molecular simulation that the recognition and recruitment of substrate can occur on an extended surface covering PS1's TM2/6/9 domains and PAL motif [15]. Tran

• We next determined the selectivity profile of the most poten

  2022-03-02

  

  We next determined the selectivity profile of the most potent GPR40 agonists (4k–n) against other free fatty AS 602801 receptors (FFA3/GPR41, FFA2/GPR43 and FFA4/GPR120). FFA2 and FFA3 agonists have a preference in binding short-chain fatty acids while FFA1 and FFA4 have a higher affinity to medium

• melatonin receptor agonist br Experimental section br Acknow

  2022-03-02

  

  Experimental section Acknowledgements This study was supported by grants from the National Natural Science Foundation of China (Grants 81673299 and 81273376). Introduction Free fatty acids (FFAs) are important metabolic fuels and those that are polyunsaturated are essential components of t

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