• We recently employed a functional drug screening approach

  2019-12-27

  

  We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito

• To develop novel EPAC inhibitors Zhou and co workers optimiz

  2019-12-27

  

  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). Dockin

• From an industrial perspective the low

  2019-12-27

  

  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

• br Results and discussion The effects of hypoxia a combinati

  2019-12-27

  

  Results and discussion The effects of hypoxia, a combination of shear stress and hyperoxia, and a combination of shear stress and hypoxia in BAECs were assessed at 0, 15, 30, 60, 120, and 180 min. Changes in phosphorylation levels of eNOS at Ser635 were investigated using immunoblotting, and repr

• The hepatic cytochrome P CYP superfamily is essential for

  2019-12-27

  

  The hepatic cytochrome P450 (CYP450) superfamily is essential for metabolising foreign chemicals, fatty acids, vitamins, hormones and other compounds and consists of 18 subfamilies (Uno et al., 2012). The number of discovered CYP genes is increasing as a result of intense work with CYP450 gene struc

• One question relates to our

  2019-12-27

  

  One question relates to our finding that oxysterol-GPR183 signaling is critical for CP and ILF formation in the colon but dispensable in the small intestine. GPR183 and its ligand were expressed in both the small and large intestines. Moreover, 7α,25-OHC was required for ILC3 migration to CPs not on

• Interestingly our analyses of human PBMCs using a monoclonal

  2019-12-27

  

  Interestingly, our analyses of human PBMCs using a monoclonal antibody against EBI2 showed that the expression pattern of human EBI2 is largely overlapping with that in mice. Especially Th17 Malonic acid showed homogeneous high expression of EBI2 compared with Th1 cells, which contained a fraction o

• If the factors needed for A NHEJ are not

  2019-12-26

  

  If the factors needed for A-NHEJ are not completely defined and the A-NHEJ reaction mechanism nebulous, it is also fair to say that the biological role(s) of A-NHEJ is even more poorly understood. Most of the current interest in A-NHEJ, however, stems from its implicated use in the chromosomal trans

• Primary human GBM neurospheres expressed high

  2019-12-26

  

  Primary human GBM neurospheres expressed high levels of the metabolic enzyme fatty acyl-CoA synthetase VL3 (ACSVL3) that were associated with CSCs self-renewal and tumorigenic capacity. ACSVL3 knockdown significantly decreased ALDH levels, indicating its contribution to cell metabolism and maintenan

• Animal studies investigating the role

  2019-12-26

  

  Animal studies investigating the role of D1 dopamine receptors in the PFC have focused on delayed response tasks, which require online maintenance of a previously presented stimulus. Striatal dopamine is thought to be important for flexibility and updating goal representations when new information i

• Key molecules in the EP second messenger signaling cascade t

  2019-12-26

  

  Key molecules in the EP1 second messenger signaling cascade that are necessary for potentiation of GluK2/GluK5 were identified. We also identified three GluK5 serines located in a membrane-proximal C-terminal domain that, when mutated to the phosphomimetic aspartate and expressed with GluK2, rendere

• br Materials and methods br Result and

  2019-12-26

  

  Materials and methods Result and discussion qRT-PCR was utilized to explore the effect of acetamizuril on the mRNA level of enolase. The results were analyzed according to the Livak 2−ΔΔCT method (Schmittgen and Livak, 2008): the mean CT of the enolase in treated and untreated samples was 29.

• br Results br Discussion Oxysterols and EBI have received

  2019-12-26

  

  Results Discussion Oxysterols and EBI2 have received growing attention in the field of immunology, with works highlighting an important role for EBI2 in immune cell migration. However, these studies are mainly limited to animal models (Chalmin et al., 2015, Hannedouche et al., 2011, Kelly et a

• br Results br Discussion In this

  2019-12-26

  

  Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 clodronate via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inhib

• A previous study suggested that

  2019-12-26

  

  A previous study suggested that DARs and octopamine/tyramine receptors (OARs/TARs) have close pharmacological properties (Beggs et al., 2011). Their relationships were also supported by phylogenetic analyses (Balfanz et al., 2005, Hauser et al., 2008, Wu et al., 2014), indicating that some of DAR an

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