• br Acknowledgements This work was

  2022-09-07

  

  Acknowledgements This work was in part supported by the FöFoLe program by Ludwig-Maximilians-Universität München (to T.S.), the Deutsche Forschungsgemeinschaft (DFG) CO 291/5-2, the Human Frontier Science Program (HFSP) RGP0013, the Helmholtz Validation Funds (Helmholtz Association of German Rese

• To discriminate the peripheral and central involvement of FA

  2022-09-07

  

  To discriminate the peripheral and central involvement of FAAH in paracetamol action, we proposed a pharmacological strategy challenging the analgesic action of paracetamol observed in an inflammatory context with either a peripherally-restricted FAAH inhibitor (URB937, Clapper et al., 2010, Moreno-

• Together the epigenetic interplay revealed in this study ena

  2022-09-07

  

  Together, the epigenetic interplay revealed in this study enabled us to expand the therapeutic potential of EZH2is from hematological malignances to solid tumors. In solid tumors, EZH2i-driven transcriptional changes are shown to be dispensable of H3K27me-regulated transcriptional network. Instead,

• KB SRC 4 While considering the molecular pathogenesis of an

  2022-09-07

  

  While considering the molecular pathogenesis of an MPNST, the Ras/Raf/MEK/ERK, mTOR/AKT, p53, and PTEN pathways associated with tumor growth have been described (McCubrey et al., 2012). The involvement of receptor tyrosine kinases such as EGFR and TAM receptor families, and its associated molecular

• Histamine H and H receptor expression

  2022-09-07

  

  Histamine H2 and H3 receptor expression is altered in the Fmoc-Trp-OH sale of Hdc mice (Chepkova et al, 2012, Fitzsimons and et al, 2001). Because these mice lack HA, expression of HA receptors might be thought to be irrelevant. This is not the case in Hdc heterozygotes, however, or in patients with

• It is important to mention that the

  2022-09-07

  

  It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co

• With LML methyl oxo dihydropyridazin yl piperidin yl cyclobu

  2022-09-07

  

  With LML-134 (1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate) containing drug-likeness properties (MW 375.47, five HBA, and MLogP 1.88), Novartis presents an additional drug-candidate to treat excessive sleepiness. A phase I clinical study was perform

• br Although there are growing bodies

  2022-09-07

  

  Although there are growing bodies of research dealing with diverse non-imidazole based compounds, they are not free from obstacles in their development pipeline and hence the design of these compounds is complicated by various factors briefly discussed below. One of the problems in designing H3R a

• br Acknowledgements br Introduction The glutathione S transf

  2022-09-06

  

  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

• br Acknowledgements br Introduction The study methods consis

  2022-09-06

  

  Acknowledgements Introduction The study methods consisted of the review of articles included in the Pubmed and Medline databases and in the clinicaltrials.gov clinical trials register between 2013 and 2016, and of the preliminary results of therapies presented at international trichology confe

• Previously we reported that the inhibition of PKC and PKC

  2022-09-06

  

  Previously, we reported that the inhibition of PKC-ζ and PKC-ε activity in hypertrophic adipocytes had deleterious effects on EPA-induced GPR120-mediated VEGF-A production [12]. However, the activation of PKC-θ, -ζ and -λ can also enhance the phosphorylation of IKK and p65, and facilitate the transl

• NAD+ br Characterization and regional localization of Glu tr

  2022-09-03

  

  Characterization and regional localization of Glu transporters Molecular studies led to the description of five subtypes of plasma membrane Glu transporters termed in accordance to their human or rodent origin (Kanai and Hediger, 1992, Pines et al., 1992, Storck et al., 1992). In humans, these tr

• Pyrogallol is an organic gallic acid converting

  2022-09-03

  

  Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic Cholera Toxin is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to produce pyrogallol (

• Recently unimolecular multi functional peptides that combine

  2022-09-03

  

  Recently, unimolecular, multi-functional peptides that combine GLP-1RA activity with Streptomycin sulfate and/or GIP activity have been suggested as new therapeutic agents for glycaemic and weight control. In rodents, dual GIP and GLP-1 receptor agonists achieve significantly better glucose control

• A relatively independent review of the history of the

  2022-09-03

  

  A relatively independent review of the history of the discovery of GABA (and L-glutamate) as neurotransmitters in the CNS can be found in ‘When and why amino acids?’ in the in 2010 by Kresimir Krnjevic , who spent a post-doc in Canberra in 1956–1958. Introduction The insect RDL GABA receptor is

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