• In addition to the ESIs identified that target

  2021-05-24

  

  In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1

• br Results br Discussion br Materials and

  2021-05-24

  

  Results Discussion Materials and Methods Acknowledgment This work was funded by the Collaborative Research Centre (SFB) 807 of the German Research Foundation (DFG) and supported by the state of Hessen (Center for Biomolecular Magnetic Resonance) and the German Research Foundation (DO545/

• To further define the importance of CYP A for

  2021-05-24

  

  To further define the importance of CYP3A for OSC metabolism in vivo, a strong CYP3A inhibitor ketoconazole was used to test whether CYP3A would affect its metabolism. As expected, the biotransformation of OSC to SC was significantly decreased by ketoconazole at all three substrate concentrations.

• br Transparency document br Main Text The centrosome is

  2021-05-24

  

  Transparency document Main Text The centrosome is a non-membrane-bound organelle found in most animal cells. It has several important functions, including control of cilia formation, microtubule organization and nucleation, spindle assembly and transport of organelles and vesicles. Centrosomes

• DUBs are involved in cell cycle regulation and

  2021-05-24

  

  DUBs are involved in calcium channel blockers regulation and DNA damage pathways and since, in cancer and different stress conditions all the proteins which regulate cell cycle and DNA damage/repair are either up/down regulated (Singh et al., 2013, Singh et al., 2011, Kumar and de Massy, 2010, Gupt

• The authors identified inhibitors of SUMOylation using two a

  2021-05-24

  

  The authors identified inhibitors of SUMOylation using two assays to monitor the conjugation of SUMO1 to RanGAP1 by E1 and E2 enzymes: a fluorescence resonance energy transfer (FRET) primary screen that evaluated over 250,000 compounds and a chemiluminescence secondary screen. A counter screen was u

• AMPHs facilitate dopamine release which further triggers

  2021-05-24

  

  AMPHs facilitate dopamine release, which further triggers dopamine depletion [72]. Indeed, we observed that repeated treatment of MPA significantly inhibited TH-, DAT-, and VMAT-2 levels. Since DAT and VMAT-2 are important for dopaminergic terminal markers [10], their decreases suggest that MPA-indu

• This study had some limitations First a

  2021-05-24

  

  This study had some limitations. First, a small number of HP patients were enrolled because of the extreme rarity of this disease, which may have caused some selection bias. Yokoseki et al., found no increase in Th2 cytokines, such as IL-4, in IHP patients (Yokoseki et al., 2014). The sensitivity of

• Experiment Blunted fear potentiated startle due

  2021-05-24

  

  Experiment 2: Blunted fear-potentiated startle due to deficient fear acquisition. SERT+/+ and SERT+/− showed significant acquisition of the cue-shock association, whereas SERT−/− did not (trial×genotype interaction: F2,50=3.3, pand dpni australia of fear-potentiated startle. Acquisition: Followin

• Previous studies have shown the harmful effects of NEFA

  2021-05-24

  

  Previous studies have shown the harmful effects of NEFA on ovarian functionality, such as inhibition of bovine granulosa cell survival and proliferation, steroidogenesis, and follicular development and alteration in oocyte development [36,45,46]. Therefore, the higher levels of NEFA found in the fol

• The data correlations from Multiflash and

  2021-05-24

  

  The data correlations from Multiflash™ [43] and DIPPR [44] were used for the liquid volume and heat of vaporization. For vapour pressure the curves were regressed from the experimental data present on both the DIPPR [44] and TRC [45] databases. As for liquid heat capacities both the latter databases

• In humans individual differences in prefrontal dopamine are

  2021-05-24

  

  In humans, individual differences in prefrontal dopamine are partially caused by the Val158Met single-nucleotide polymorphism on the catechol-O-methyltransferase gene (COMT). This gene controls activity of the COMT enzyme, which degrades extracellular catecholamines including dopamine. The Val varia

• Among the Ub interactions observed in

  2021-05-22

  

  Among the ~Ub interactions observed in the HOIP structure is one that involves a RING2 domain (from the non-cognate HOIP) [47]. A similar binding interaction was defined between HHARI RING2 and the hydrophobic patch on Ub by NMR [54]. HHARI RING2 mutations that ablate the interaction inhibit formati

• br Patients and Methods Patients who

  2021-05-22

  

  Patients and Methods Patients who had been initiated on a DPP-4 inhibitor (see in the online version at doi:10.1016/j.clinthera.2018.06.002) between April 2012 and June 2017, when the common threshold for dose adjustment for all non-linagliptin DPP-4 inhibitors was a creatinine clearance (CrCl) l

• br Results The AR genotype frequencies are

  2021-05-22

  

  Results The AR genotype frequencies are shown in Table 1. Alleles at the two loci are in linkage disequilibrium, as expected for such closely linked loci and consistent with previous findings (Kittles et al., 2001). The genotype frequency for the DBH 1021 polymorphism is similar to previous find

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