• br Introduction The development and plasticity

  2023-09-18

  

  Introduction The development and plasticity of synapses involve the timely recruitment of a plethora of proteins on both pre- and postsynaptic sides through ill-defined mechanisms. At excitatory synapses, two of the major proteins that are dynamically recruited postsynaptically are the Ca2+/calmo

• br Conclusion We have identified three non competitive

  2023-09-18

  

  Conclusion We have identified three non-competitive inhibitors of the human and porcine APN with Ki values in the μM range, by combining virtual screening and kinetic assays. Molecular docking simulations suggest these novel inhibitors block APN activity by an alternative mechanism to Zn coordina

• br Discussion The patient presented initially only with pari

  2023-09-18

  

  Discussion The patient presented initially only with parietal symptoms in the form of acalculia, visuo-spatial deficits, and visuo-perceptual deficits and dressing apraxia. He also had simultognosia as early symptoms. Later when the disease progressed he had recent memory deficits and language in

• The ORR obtained with crizotinib on

  2023-09-18

  

  The ORR obtained with crizotinib on our cohort was low compared to other studies, such as the prospective studies of A. Shaw et al. (ORR = 65% in second line), B. Solomon et al. (ORR = 74% in first line) and the more comparable large retrospective study of M. Duruisseaux et al. on the French CLINALK

• Ketogenic diets are more effective in promoting weight loss

  2023-09-18

  

  Ketogenic diets are more effective in promoting weight loss than conventional caloric restriction [26] however, their effect on hepatic glucose and lipid metabolism remains inconclusive. Blood glucose homeostasis is tightly regulated. In both mice and humans consuming KD, baseline blood glucose decr

• Ambient levels of ppm ozone

  2023-09-18

  

  Ambient levels of 0.2ppm ozone were recorded during a recent 2017 weather event in Texas, United States (EPA, 2007). This concentration or higher levels have been used in several human clinical studies during intermittent exercise (Miller et al., 2016c). Although ozone concentration of 0.8ppm used i

• Our previous work fails to show

  2023-09-18

  

  Our previous work fails to show any maternal effect with blockade of 5-HT2A receptor, as acute and repeated treatment of MDL100907 does not alter maternal behavior at the behaviorally active doses (Chen et al., 2014). In the present study, MDL100907 pretreatment attenuated the maternal disruptive ef

• The fact that the BPloopAsn regains its Btx binding

  2023-09-18

  

  The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li

• The extent to which GPCR oligomerization is a regulated

  2023-09-18

  

  The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or

• Application of the broad acting HTR

  2023-09-18

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• Introduction hydroxytryptamine HT is found throughout the bo

  2023-09-18

  

  Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary 4E1RCat (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current classificati

• We conducted the largest drug

  2023-09-18

  

  We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst

• Here we report discovery of highly selective pan

  2023-09-18

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of A-317491 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To i

• br Conclusions In summary the

  2023-09-18

  

  Conclusions In summary, the present results showed that ageing diminished arginase activity only in clearance tissues and that l-arginine supplementation did not induce major changes in arginase activity thus refuting a role of arginase in the potential deleterious effects of l-arginine supplemen

• br Concluding remarks and future perspectives While the

  2023-09-18

  

  Concluding remarks and future perspectives While the rational engineering of protein-based switches has yet to be fully developed, emerging empirical rules facilitate the construction of tailor-engineered Tankyrase Inhibitors 22 with custom input and output parameters. Both in the context of mole

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