• br Methods br Results br

  2021-01-20

  

  Methods Results Discussion MEN91507 is a potent and selective CysLT1 receptor antagonist. Guinea-pig lung membranes have been widely used for the detection and characterization of CysLT1 receptor antagonists: in this assay the high affinity (subnanomolar) binding of [3H[leukotriene D4 or [3

• Alternatively procedural factors may have contributed to the

  2021-01-20

  

  Alternatively, procedural factors may have contributed to the conflicting results. For instance, in order to have a more circumscribed area of drug diffusion, a volume of 0.05μl was injected in experiment 1b, which is four times lower than the one used in the mentioned plus-maze investigation. Besid

• This structure guided the variation of the

  2021-01-20

  

  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

• SID 26681509 Many processes can lead to changes in soil P po

  2021-01-20

  

  Many processes can lead to changes in soil P pools over time. Plant-available P (when measured as DGT P) decreased over time for the INORG-P treatment (Fig. 1a). Orthophosphate can be stabilised with cations such as calcium to produce insoluble phosphates, reducing plant-available P (Bünemann et al.

• EBI and its ligand s EBI was found in

  2021-01-20

  

  EBI2 and its ligand(s) EBI2 was found in a screen of upregulated genes in human B cells upon infection with EBV [1]. EBI2 is a G-protein (Gαi type) coupled receptor [2] but as long as 18 years after its discovery the nature of its ligand remained undisclosed. With the help of transfected cell lines

• The unique property of mutant

  2021-01-19

  

  The unique property of mutant IDH1/2 in producing an oncometabolite that has no known physiological function makes mutant IDH enzymes as obvious potential therapeutic targets for the treatment of IDH-mutated tumors (Rohle et al., 2013, Wang et al., 2013). Clinical studies have also suggested the pre

• A novel series of DHODH inhibitors was developed

  2021-01-19

  

  A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h

• DGK is classified into the type II DGK

  2021-01-19

  

  DGKη is classified into the type II DGK subfamily [12], [13], [14], [15]. As described above, DGKη has the splice variants η1 and η2 [10]. DGKs η1 and η2 possess in common a pleckstrin homology domain at the N-terminus and a catalytic domain that is divided into two subdomains (catalytic subdomain-a

• br Materials and methods br Results br Discussion

  2021-01-19

  

  Materials and methods Results Discussion Conclusions First, we replicated the association of DDR1 with SZ in an independent Spanish sample and demonstrated that a SNP-SNP interaction within DDR1 played a role in the association with the disease. Second, we observed that SZ subjects with

• br Conclusions The present study

  2021-01-19

  

  Conclusions The present study demonstrated that CuE possesses strong hepatotoxicity. CuE is not only a mechanism-based inhibitor of human CYP3A4, but also inhibits P-gp activity in vitro. In whole animal studies, CuE induces CYP3A and P-gp after a long-term treatment but inhibits the activities o

• R co localizes Golgi marker

  2021-01-19

  

  R co-localizes Golgi marker GM130 (Fig. 5). Our metabolic pulse-chase studies carried out in the presence of CSF-1 exposed the newly synthesized CSF-1R to its ligand, which promoted its rapid degradation. While this was clearly seen in control BMDMs, the mature band of CSF-1R remained intact for the

• It is important to note that CRF may be activated

  2021-01-19

  

  It is important to note that CRF1 may be activated during acute stress and early phases of anxiety disorders (Coric et al., 2010, Ising et al., 2007), as well the administration of Astressin 2B into the lateral septum did not have an effect on anxiety-like behavior in low-stress conditions but had a

• Following mutagenesis of the glucarpidase gene of Pseudomona

  2021-01-19

  

  Following mutagenesis of the glucarpidase gene of Pseudomonas sp. strain RS-16 [30], approximately 73% of the clones retained enzyme activity, as indicated by the clear zones and yellow precipitate surrounding their colonies. However, there were very few that had ‘halos’ around colonies that were da

• Yang et al investigatedPsoralidin a coumestan

  2021-01-19

  

  Yang et al. investigatedPsoralidin 39, a coumestan derivative isolated from the seed of Psoralea corylifolia, regarding its effects on IR-induced pulmonary inflammation. Psoralidin 39 inhibited the IR-induced COX- 2 expression and PGE(2) production through regulation of PI3K/Akt and NF-κB pathway. A

• Nowadays it is possible to detect the AChE inhibitors

  2021-01-19

  

  Nowadays it is possible to detect the AChE inhibitors by several methods such as gas chromatography-mass spectrometry [11], ion mobility spectrometry [12] and lab-on-chip devices [13,14]. However, almost all instrumental detection techniques that are able to conclusively determine the presence of th

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