• In order to evaluate the

  2020-02-12

  

  In order to evaluate the in vivo pharmacology associated with EP receptor antagonism, we wished to discover antagonists presenting a higher degree of selectivity over the other prostanoid receptors. We also wanted to increase the brain–blood ratio since it is probable that centrally mediated EP agon

• To study systemic potential of the selected compounds as

  2020-02-12

  

  To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,

• We further analyzed the transcriptional

  2020-02-11

  

  We further analyzed the transcriptional mechanisms underlying the synergistic action of IL-23 and PGE2 and found that this action is mediated by not only STAT3 but also CREB1 and NF-κB. Involvement of CREB1 is analogous to that in the PGE2-EP2/EP4–mediated Il12rb2 induction during TH1 cell different

• SU 4312 Accumulating evidence suggests that certain abnormal

  2020-02-11

  

  Accumulating evidence suggests that certain abnormal emotional traits, such as impulsive aggression and cluster B personality, are associated with suicidal behaviors (Currier and Mann, 2008, Mann et al., 2009, Rujescu et al., 2007, Turecki, 2005). Impulsive aggression appeared to be associated with

• br Introduction As a strong analgesic morphine is

  2020-02-11

  

  Introduction As a strong analgesic, morphine is often used to treat acute and chronic pain. However, morphine is a substance with low lipid solubility that slowly enters the nerve tissue through the blood–brain barrier and produces neurotoxicity. Morphine-induced neurotoxicity can be produced aft

• The DNA damage response DDR is a cellular mechanism

  2020-02-11

  

  The DNA damage response (DDR) is a cellular mechanism that protects against DNA damage induced by endogenous and exogenous factors, it includes changes in cellular processes such as zilpaterol regulation, DNA damage repair, apoptosis and chromatin remodeling. In recent years, the DDR has been recog

• Molecular modelling studies were performed on the hDHFR

  2020-02-11

  

  Molecular modelling studies were performed on the hDHFR inhibitors identified (1, 11, 13, 14, 16, 25 and 32) to explore the structural basis of the interaction between the mentioned compounds and the human enzyme. The docking studies were performed using the X-ray crystallographic structure of the h

• Supported by the Austrian Science Fund

  2020-02-11

  

  Supported by the Austrian Science Fund FWF (grant P22521-B18 to A.H.) and the Austrian National Bank (grant 14263 to A.H.). K.J. was funded by the PhD Program DK-MOLIN (FWF-W1241). Acknowledgements Introduction Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS), a more se

• Our results show that COX and

  2020-02-11

  

  Our results show that COX-1 and COX-2 inhibition improve cognitive performance and decrease the neuronal insult during HH. However, when a neuroinflammatory response was observed, COX-1 inhibition was more effective than COX-2 inhibition at reducing microglial activation and augmenting pro-inflammat

• The assessment process is even more difficult when

  2020-02-11

  

  The assessment process is even more difficult when Commercial-Off-The-Shelf (COTS) components – whose internals are partially or totally unknown – come into play. COTS are being increasingly used by the industry to reduce costs and to shorten development (and possibly deployment) time. However, sinc

• It is noteworthy that little is known as

  2020-02-11

  

  It is noteworthy that little is known as to the role of autophagy in regulation of eNOS phosphorylation and eNOS uncoupling. eNOS monomers, but not eNOS dimers could be degraded by ubiquitination [39], harbingering the existence of protein degradation pathways in modulation of eNOS turnover and acti

• DGK deficiency caused a significant increase in the SERT

  2020-02-10

  

  DGKδ deficiency caused a significant increase in the SERT protein level, but its mRNA level was not affected (Fig. 1). These results suggest that SERT protein stability is directly reduced by interaction with the DGKδ protein. In contrast, DGKδ deficiency regulated both TPH-2 and MAO-A protein and m

• arginase inhibitor In the preclinical evaluation of CRF rece

  2020-02-10

  

  In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe

• br Conclusion The past few years

  2020-02-10

  

  Conclusion The past few years have witnessed substantial progress in understanding the structural mechanisms of substrate recognition and the reactions catalyzed by the O-GlcNAc-cycling enzymes, but more work remains. In particular, future research will be needed to establish how OGT and OGA inte

• br Concluding remarks and prospective Cardiac proteinopathy

  2020-02-10

  

  Concluding remarks and prospective Cardiac proteinopathy, a more common disease condition and more frequent cause of cardiomyocyte decay than previously thought, is largely neglected and no effective therapy exists yet. Protein quality control and protein degradation via autophagy or the ubiquiti

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