• br Conflicts of interest br Financial support NZ

  2020-10-28

  

  Conflicts of interest Financial support NZ is an Established Investigator of the Dutch Heart Foundation (2013T111) and is supported by an ERC Consolidator grant (617376) from the European Research Council and by a Vici grant from the Netherlands Organization for Scientific Research (NWO; 91818

• Stattic synthesis Compound was advanced to a chronic efficac

  2020-10-28

  

  Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, Stattic synthesis 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured

• Besides the assessment of toxicological effects immediately

  2020-10-27

  

  Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c

• br Materials and methods br Results

  2020-10-27

  

  Materials and methods Results We examined the effects of curcumin in Fluo-4 loaded SH-EP1 amg express llc stably transfected with human α7-nACh receptor. Application of curcumin alone in the concentrations up to 100 μM for 30 sec. did not induce any detectable change in intracellular Ca2+ lev

• Artificial permutations have also been exploited by protein

  2020-10-27

  

  Artificial permutations have also been exploited by protein engineering to manipulate protein scaffolds, in order to improve catalytic activity, alter substrate or ligand binding affinity, reduce proteolytic susceptibility, increase stability, generate different aggregation states and improve fluore

• From an industrial perspective the low turnover numbers and

  2020-10-27

  

  From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo

• A major finding to emerge from this study

  2020-10-27

  

  A major finding to emerge from this study is a conserved regulatory scheme deployed by both innate and adaptive lymphocytes, which is coordinated by a cohort of TFs. The scheme functionally compartmentalizes effector ras gtpase that circulate between blood and peripheral tissues from self-renewing

• We propose two different pathways for the

  2020-10-27

  

  We propose two different pathways for the production of this species: either that described by Dooley [24], where the phenol ring is first activated by binding of its oxygen to copper, or one where a copper-peroxo species would directly react with an active site tyrosine residue (Scheme 1B). This se

• In conclusion we have discovered two new derivatives and

  2020-10-27

  

  In conclusion, we have discovered two new derivatives ( and ) that are potent inhibitors of DHODH. H and C NMR spectroscopic data revealed that these compounds undergo ready isomerisation at room temperature in -DMSO, but the docking studies indicate that there is neither conformation nor configurat

• As previously reported azole class antifungal drugs inhibit

  2020-10-27

  

  As previously reported, azole class antifungal drugs inhibit fungal CYP450 14α-demethylase, as this interrupts the conversion of lanosterol to ergosterol, a component of the fungal cell membrane (Hof, 2006). Furthermore, correlation between fluconazole dose, the extent of hepatic hypertrophy, the le

• The consistent anti anxiety effects

  2020-10-26

  

  The consistent anti-anxiety effects obtained with intra-mPFC injections of CP 376395 strongly suggest a tonic role of CRF at CRF1 receptors located within this limbic ribosomal s6 kinase area in the modulation of anxiety in the mouse on the EPM. Intra-mPFC injection of CP 376395 led mice to explore

• br Materials and methods br Results br Discussion Recently i

  2020-10-26

  

  Materials and methods Results Discussion Recently it has been found that prostaglandins play an important role in modulating the host immune system [1,3,22,23], and some parasites produce these eicosanoid mediators to survive into their hosts [6,[10], [11], [12],24,25]. The discovery that p

• This structure guided the variation of the compounds

  2020-10-26

  

  This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis

• The present study intended to characterize the predominant c

  2020-10-26

  

  The present study intended to characterize the predominant cholinesterasic form found in tissues of three tropical fish species, namely Phalloceros harpagos Lucinda, 2008 (common name guaru), Pterygoplichthys pardalis Castelnau, 1855 (common name cascudo) and Astyanax altiparanae Garutti and Britski

• Although in vitro and in vivo immunosuppressive effects of

  2020-10-26

  

  Although, in vitro and in vivo immunosuppressive effects of female steroids have been described in fish (Yamaguchi et al., 2001, Law et al., 2001), their mode of action was not evaluated in detail. Consequently, it is of considerable interest to investigate the intracellular pathways that regulate t

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