• br Materials and methods br Results br

  2022-01-04

  

  Materials and methods Results Discussion Our liver-specific Gck (−/−) mice and another line of liver-specific mice [13] exhibited impaired glucose tolerance. Furthermore, both knockout mice showed decreased hepatic glycogen content and reduced Pklr and Fas gene Cyclopiazonic acid in the li

• Attempting to further elucidate the role

  2022-01-04

  

  Attempting to further elucidate the role of androgen receptor and activation of the Gcgr without the influence of GLP-1, we used DT-Gcg mice with acute knockdown of all proglucagon products. This mouse model has previously been shown previously to have a normal total islet area as well as β cell are

• To directly address whether pharmacological attenuation of p

  2022-01-04

  

  To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N

• In the liver ghrelin has opposite effects to insulin

  2022-01-04

  

  In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty L-817,818 synthesis oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-in

• br Acknowledgments The research leading to these

  2022-01-04

  

  Acknowledgments The research leading to these results was funded by European Community’s Seventh Framework Programme (FP7/2007-2013) under grant agreement No. 222719 – LIFECYCLE and by the Foundation for Science and Technology of Portugal (FCT), through projects PTDC/MAR-BIO/3890/2012 and PEst-C/

• FPR ligands comprise structurally very

  2022-01-04

  

  FPR ligands comprise structurally very diverse glycogen phosphorylase of compounds, ranging from naturally occurring peptides/proteins or “danger signals” such as PAMPs and DAMPs (see 1.1), respectively, to endogenous lipids and even various synthetic non-peptides, such as benzimidazoles, pyrazolon

• Hardy et al had demonstrated the role

  2022-01-04

  

  Hardy et al. had demonstrated the role of GPR40 in mediating the proliferative effect of the FFA oleate's in breast cancer cells, and found that such effect can be reversed by silencing of GPR40 [14]. Similarly we have observed that inhibition of GPR40 function by its antagonist GW1100 inhibited cel

• The anti platelet functions of ZGR were confirmed

  2022-01-04

  

  The anti-platelet functions of ZGR were confirmed by the mechanistic studies such as the activation of PKC, intracellular Ca2+ mobilization, and the expressions of P-selectin and PAC-1. Further, rivaroxaban prolonged the generation of thrombin and reduced the thrombin burst produced in the propagati

• In conclusion a series of new carboxamido

  2022-01-04

  

  In conclusion, a series of new 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and screened for their inhibitory potency against FAAH. Their cytotoxicity was determined and their lipophilicity was calculated. Compounds bearing a 3-substituted biphenyl moiety with high Log values displayed

• br Materials and methods br Results br Discussion The

  2022-01-04

  

  Materials and methods Results Discussion The roles of EZH2 during oocyte maturation, early embryogenesis, and somatic cell nucleus transfer (SCNT) have been studied extensively in mouse [12,30]. How it functions during porcine preimplantation development, especially the maternal effect, how

• On the basis of the

  2022-01-03

  

  On the basis of the foregoing set of considerations, L1 could exert three possible actions on sGC determining its deactivation, schematically depicted in Fig. 6: i) oxidation of Fe2+ to Fe3+; ii) coordination to sGC, conjecturably, via the pyridyl nitrogen of the canthin-6-one; iii) coordinating and

• br Acknowledgments We thank Dr Kathleen Sullivan of Merck

  2022-01-03

  

  Acknowledgments We thank Dr Kathleen Sullivan of Merck Research Laboratories for providing the CHO-K1 HU 308 expressing an NFAT-β-lactamase reporter and the Gα subunit Gqi5, Dr. Chen Liaw (Arena Pharmaceutical), Ms. Rebecca Kaplan, Mr. Frank Xiaodong Gan for technical assistance, Dr. Andrew Howar

• Since KYNA concentrations are increased by aerobic

  2022-01-03

  

  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

• Compounds and were tested for pharmacodynamic effects in a

  2022-01-03

  

  Compounds , and were tested for pharmacodynamic effects in a mouse oral glucose tolerance test (oGTT) in wild-type and GPR120 deficient mice, and each compound demonstrated GPR120 mechanism-based effects. Data for compound is shown in , indicating mechanism-based reduction in glucose excursion a

• A general synthetic pathway to these

  2022-01-03

  

  A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy

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