• To develop novel EPAC inhibitors

  2019-12-28

  

  To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock

• br Materials and methods br Results br Discussion

  2019-12-28

  

  Materials and methods Results Discussion Inflammatory signalling and in particular the arachidonic SynaptoRedTM C2 cascade have been suggested as targets for disease modification, optimization of the therapeutic response, and even restoration of pharmacosensitivity (Potschka, 2010). Recent

• In the present study we investigated the deeper

  2019-12-28

  

  In the present study, we investigated the deeper role of eNOS in the pathogenesis of nasal polyps and analyzed the influence of 1,8-cineol on nasal polyp gene and protein expression of eNOS in vitro. Different studies dealt with the localization and expression of eNOS in nasal polyps and nasal mucos

• Neuropsychological studies of adults with problem gambling

  2019-12-27

  

  Neuropsychological studies of adults with problem gambling indicate impairments in many cognitive areas including inhibition, working memory, decision-making, cognitive flexibility, and executive planning (Ledgerwood et al., 2012, Goudriaan et al., 2006). Dopamine is a neurotransmitter that regulate

• br Author contribution br Acknowledgements

  2019-12-27

  

  Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General

• ABH expression is elevated in

  2019-12-27

  

  ABH3 expression is elevated in prostate carcinomas and has been referred to as prostate cancer antigen-1 or PCA-1. ABH3/PCA-1 was proposed as a diagnostic marker for prostate cancers, and suggested as a possible therapeutic target [82]. However, the recent studies of ABH2 and ABH3-null mice indicate

• An AmDH is engineered by mutating two conserved amino acid

  2019-12-27

  

  An AmDH is engineered by mutating two conserved amino hedgehog signaling residues in the active site of an amino acid dehydrogenase (AADH). Starting from the leucine dehydrogenase (LeuDH) from Bacillus stearothermophilus, substituting a serine and leucine at the K68 and N261 positions, respectively,

• We have previously reported DAPK

  2019-12-27

  

  We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure

• The CysLT receptor antagonist BayCysLT RA significantly supp

  2019-12-27

  

  The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear na+/ca2+ exchanger into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding, Bar

• It is worth mentioning that in this

  2019-12-27

  

  It is worth mentioning that, in this study we only observed the responses of CYP450 to the short-term exposure of DSP toxins (12 h). However, the toxic effects of DSP toxins to bivalves appeared to abate with longer exposure (Pinto-Silva et al., 2005; Flórez-Barrós et al., 2011; Prego-Faraldo et al.

• br Clinical trials of CRM

  2019-12-27

  

  Clinical trials of CRM1 inhibitors KPT-330 clinical trials have been initiated with promising very early results. One trial includes patients with advanced solid tumors whose disease has progressed after at least one prior therapy for metastatic disease (NCT01607905). Another trial includes patie

• br Acknowledgements The study was supported by grant

  2019-12-27

  

  Acknowledgements The study was supported by grant no. 501-003-11043 from the Institute of Psychiatry and Neurology in Warsaw. The authors thank Mrs. Ala Biegaj for the excellent technical assistance. Introduction In an effort to identify hIFN receptor molecules encoded by a gene(s) within hum

• Besides the regulation of the stress responses

  2019-12-27

  

  Besides the regulation of the stress responses, CRF and the urocortins have been implicated in drug addiction (Bruijnzeel and Gold, 2005, Sarnyai et al., 2001). For instance nicotine, the addictive substance of tobacco, can activate the HPA axis, just like any other stressor may do, although its imp

• br Selection of ions for

  2019-12-27

  

  Selection of ions for GaN Systems sample test Sample construction analyses has been provided to analyze the beam penetration of several ions of the cocktail in the component. An X-ray and optical view of GaN System devices parts is presented at Fig. 5, Fig. 6 respectively. The drain and source el

• The collagen field undoubtedly regains attractiveness with

  2019-12-27

  

  The collagen field undoubtedly regains attractiveness with the emergence of new concepts (cell niche, regulation of growth factor bioavailability, mechanotransduction, cell microenvironment sensing) and new tools to investigate their in vivo functions (atomic force microscopy (AFM), second harmonic

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