• br Non cyclic nucleotide EPAC regulators Despite the

  2021-05-07

  

  Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su

• br Materials and methods br

  2021-05-07

  

  Materials and methods Results Discussion In this study, we employed a liquid chromatography mass spectrometry (LC–MS)-based metabolomic approach to profile GEF metabolism and bioactivation in human and mouse liver microsomes. Metabolomic approaches rendered us readily screen out the GEF-rel

• Historically covalent drugs have had

  2021-05-07

  

  Historically, covalent drugs have had great success (e.g., aspirin and penicillin), and covalent drugs have become a focus in anticancer and antiviral drug discovery (Kalgutkar and Dalvie, 2012, Singh et al., 2011). These compounds contain low reactivity warheads that allow covalent adducts to form

• Acyclovir Approximately of the etamicastat dose was recovere

  2021-05-07

  

  Approximately 50% of the etamicastat dose was recovered in urine, 30% in the form of etamicastat and 20% in the form of BIA 5-961. These data agree with those from a study with [14C]-labeled etamicastat in healthy subjects, which showed that approximately 95% of the administered radioactivity had be

• Given the structural similarity of

  2021-05-07

  

  Given the structural similarity of BMAA to other amino acids, our hypothesis was that N-nitrosation of BMAA might result in a toxic alkylating agent, providing a previously unrecognised mechanism for BMAA action. Materials and methods Results and discussion We first examined whether chemical

• In conclusion our results demonstrated that

  2021-05-06

  

  In conclusion, our results demonstrated that TGF-β1 promotes linear invadosome formation in hepatocellular carcinoma cells, through the regulation of collagen I, its receptor and its cross-linker (Fig. 6). The key role of TGF-β1 in HCC development allow us to suggest that linear invadosomes and thei

• Having generated synthetic cytokines and synthetic cytokine

  2021-05-06

  

  Having generated synthetic cytokines and synthetic cytokine receptors, the logical next step has been to design fully synthetic cytokine/cytokine receptor systems, modifying either cytokine/cytokine receptor binding interfaces or cytokine-unrelated combinations of substances and their binding domain

• Cysteine protease inhibitors representing several chemical

  2021-05-06

  

  Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests

• To elucidate the potential mechanism underlying

  2021-05-06

  

  To elucidate the potential mechanism underlying osteosarcoma cell growth decrease by CDK4 inhibition, flow cytometry analysis was used to determine more helpful hints and apoptosis in human osteosarcoma cells after palbociclib treatment. The results showed that osteosarcoma cells were arrested in G

• The aim of the present study was

  2021-05-06

  

  The aim of the present study was to investigate the acute effects of THC on resting state triapine neurophysiology, and to examine the impact of COMT genotype on these effects. Thirty-nine healthy volunteers participated in a randomised, placebo-controlled, crossover pharmacological MRI study. Acut

• The acetylcholinesterasic activity of exposed animals after

  2021-05-06

  

  The acetylcholinesterasic activity of exposed animals, after treatment with diverse concentrations of uranium and following distinct recovery periods, remained unaltered for all species. This finding suggests that uranium, in spite of being a water-soluble metal, does not exert any effect on the sel

• br Cholesterol handling in the arterial wall cells Foam

  2021-05-06

  

  Cholesterol handling in the arterial wall cells Foam cell formation in the arterial intima is a major hallmark of early-stage atherosclerotic lesions, which is attributed to uncontrolled uptake of modified lipoproteins, excess cholesterol esterification and impaired cholesterol release [44]. As a

• br Materials and methods br

  2021-05-06

  

  Materials and methods Results Discussion In this study, the N&B analysis showed new evidence regarding the proportion and the oligomerization state of the AT1 and the ETA receptors near or on the plasma membrane. Althought, preliminary studies suggest that the AT1 and the ETA receptors occu

• Introduction Penetrator with Enhanced Lateral Effect PELE

  2021-05-06

  

  Introduction Penetrator with Enhanced Lateral Effect (PELE) is a kind of ammunition which consists of a low-density material as the filling and a high-density material as the jacket [1,2]. When PELE impact target, the jacket is radially accelerated, expanded and fractured because of distinctive lat

• The underlying assumption of consolidation

  2021-05-06

  

  The underlying assumption of consolidation/re-consolidation is that the focal adhesion kinase activity initiated during the acquisition trial/re-consolidation trial continues to persist briefly after completion of the trial and it is during this post-trial period that immediate post-trial treatment

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