• br TGR Agonists br FXR TGR Dual Agonists

  2022-10-04

  

  TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency

• Finally the results in this article indicate that atomistic

  2022-10-04

  

  Finally, the results in this article indicate that atomistic MD in conjunction with computational electrophysiology and ion-permeation simulations provide a useful tool for the functional annotation of ion-channel structures. In particular, they exemplify how MD simulations in native lipid membranes

• br Conclusions The results of this

  2022-10-04

  

  Conclusions The results of this work showed that β-glucosidase could be efficiently immobilized onto hydroxyapatite nanoparticles in a single adsorption step. The enzyme adsorption was accomplished by coordination bonds between remaining Ca2+ sites of HA and COO− of amino acids. The immobilizatio

• br Ghrelin and energy balance

  2022-10-03

  

  Ghrelin and GW9662 balance To characterize the physiological role of ghrelin in energy homeostasis, ghsr−/− and ghrelin−/− mice were generated [33], [36], [41], [47]. Although ghrelin regulates the amplitude of episodic GH release, ghsr−/− mice were not dwarfs, and in fact appear identical to th

• Moreover studies on subcellular localization of FBPase

  2022-10-02

  

  Moreover, studies on subcellular localization of FBPase in carp heart and smooth muscle revealed nuclear localization of the enzyme. Previously, we have unequivocally demonstrated the presence of FBPase in the nuclei of mammalian cardiomyocytes (Gizak and Dzugaj, 2003) and myocytes (Gizak et al., 20

• Thus far it is reported that the histone methyltransferase a

  2022-10-02

  

  Thus far, it is reported that the histone methyltransferase activity of SUV39H1 is regulated through some posttranslational modifications. For example, deacetylation of SUV39H1 at Lys-266 by SIRT1 deacetylase increases SUV39H1 activity [31], and methylation of SUV39H1 at Lys-105 and Lys-123 by SET7

• To identify structurally novel autophagy inhibitors a medium

  2022-10-01

  

  To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 Clofazimine stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automat

• br Discussion In the present paper it

  2022-10-01

  

  Discussion In the present paper it was shown for the first time that the conjugation of ethacrynic NLG-8189 mg and glutathione catalyzed by GSTP1-1 stereospecifically forms one of the diastereoisomers of the glutathione conjugate (EASG). Chemical conjugation results in formation of a mixture of b

• We also observed a significantly higher SLC A gene

  2022-09-30

  

  We also observed a significantly higher SLC10A1 gene expression and NTCP protein level among metastatic individuals vs. donor livers. Na+/taurocholate co-transporting polypeptide (NTCP), which is expressed on the basolateral membrane of hepatocytes and is primarily responsible for the uptake of bile

• Herein we report the discovery

  2022-09-30

  

  Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to

• Accordingly it is tempting to

  2022-09-30

  

  Accordingly, it is tempting to speculate that the maintenance of a stimulus representation in the A2 state for a short period of time after the presentation of a specific stimulus (i.e. self-generated priming) may rely upon GluR-A-dependent synaptic plasticity. If this were the case, GluR-A GI 25402

• In a previous study M

  2022-09-30

  

  In a previous study (Möykkynen et al., 2003), we reported that ethanol lengthens the time needed for the AMPA receptors to recovery from desensitization in isolated hippocampal neurons. Here, we did not observe any effect of ethanol on recovery from desensitization in recombinant homomeric GluR-D re

• Administration of a fructose rich diet to

  2022-09-30

  

  Administration of a fructose-rich diet to normal rats induces insulin resistance and impaired glucose tolerance or diabetes, depending on treatment duration [23]. We have shown that development of these abnormalities as well as fat deposit in liver, are effectively prevented by co-administration of

• A key limiting factor in the semi quantitative analysis of

  2022-09-30

  

  A key limiting factor in the semi-quantitative analysis of changes in the nuclear-to-cytoplasmic distribution of glucokinase is the large intercellular heterogeneity of Ursodiol of glucokinase in both isolated hepatocytes in vitro and also in liver in vivo[13], [23], [24], [26], [36]. This necessit

• A majority of investigations of the GCK PFK FBPase interacti

  2022-09-30

  

  A majority of investigations of the GCK-PFK-2/FBPase-2 interaction have taken place within cells. Immunofluorescence studies in several fixed cell lines indicate that GCK colocalizes with PFK-2/FBPase-2 in the cytoplasm following overexpression [[68], [69], [70]]. Live cell imaging conducted on Alex

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