• br Acknowledgements This work was supported by grants

  2021-10-09

  

  Acknowledgements This work was supported by grants from la Ligue Nationale Française Contre le Cancer « Equipe LNCC 2016 » and Electricité de France RB 2016-17 (to M.S.), NU ORAU (http://www.nu.edu.kz) and Ministry of Education and Science of the Republic of Kazakhstan, program 0115RK03029 (to B.

• In terms of stimulation oxytocin

  2021-10-08

  

  In terms of stimulation, oxytocin, dopamine, noradrenaline, adrenaline and glucagon have all been reported to increase ghrelin secretion (Mundinger et al., 2006, Iwakura et al., 2011, de la Cour et al., 2007, Gagnon and Anini, 2013). Stimulatory effects on ghrelin secretion have also been observed w

• Immunohistochemistry using anti FFAR antibodies

  2021-10-08

  

  Immunohistochemistry using anti-FFAR1 antibodies revealed immunoreactivity for FFAR1 in association with the cell membrane of the hepatocytes (Figure 2). However, the anti-FFAR2 antibody was not suitable for immunohistochemistry under the tested conditions (data not shown). Fatty liver is an import

• Murine models of AML were used to identify

  2021-10-08

  

  Murine models of AML were used to identify differentially expressed proteins following treatment with the EZH2 inhibitor, DZnep. Sandow and coworkers demonstrated that inhibition of EZH2 induces leukemia annexin v arrest through regulation of cyclin-dependent kinases and increased expression of p53

• Some studies using RNAi have recently been invalidated by CR

  2021-10-08

  

  Some studies using RNAi have recently been invalidated by CRISPR/Cas9 [25] due to significant off-target effects of RNAi [26]. In this study, we have used both RNAi and CRISPR/Cas9 techniques and have observed consistent and similar phenotypes thus; knockdown or knockout of PATZ1 resulted in reducti

• It appears that different agonists for

  2021-10-08

  

  It appears that different agonists for GPR55 activate different signalling pathways [25]. GPR55 activation through LPI has been shown to trigger ERK 1/2 phosphorylation 22, 23, 25, 33. Conversely, endogenous cannabinoid compounds AEA and 2-AG have been shown to have no effect on ERK 1/2 signalling 2

• Starting from commercially available dioxaspiro decan

  2021-10-08

  

  Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an imidazoline receptors catalyzed deprotection efficiently gave . A - enriched mixture of (/=∼

• GPR A a G protein coupled receptor

  2021-10-08

  

  GPR109A, a G-protein-coupled receptor located mainly on adipocyte cell membranes, has been identified as the molecular target for nicotinic flt3 [[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 inhi

• In vitro studies have shown that some antidepressant drugs b

  2021-10-08

  

  In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th

• The eradication of agonist activity in compound was also con

  2021-10-08

  

  The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary INO-1001 as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize th

• The overall very satisfactory potency

  2021-10-07

  

  The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic Senegenin core in order to improve affinity to FFA1. The agonist activity in this series appears to be particularly sens

• Amphotericin B Conclusions br Author information The obtaine

  2021-10-07

  

  Conclusions Author information The obtained models of complexes of FPR2 with most of the described compounds are freely available at the author’s web site: http://www.biomodellab.eu/models/. Acknowledgements This work was partly done at the Interdisciplinary Centre for Mathematical and Compu

• PK profiles of were evaluated and found to

  2021-10-07

  

  PK profiles of were evaluated and found to be improved compared to compound presumably due to interruption of β-oxidation. Low clearance and high plasma exposure were considered to be suitable profiles as an oral agent (). We first examined in vitro insulinotropic effects of compound from MIN6 cell

• EHop-016 In Kdm c germline and forebrain conditional

  2021-10-07

  

  In Kdm5c germline and forebrain conditional knockout mice, RNA sequencing showed the upregulation of a large set of genes, suggesting that Kdm5c functions primarily as a transcriptional repressor [,]. While no changes in global H3K4me3 levels were observed in the knockout neurons, there were thousan

• Pharmacologic approaches of inhibiting GSNOR

  2021-10-07

  

  Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications

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