The development of alendronate (ALN)-coated magnetite thus serves as a rapid initial screen for the ability of targeting ligands to enhance nanoparticle-antiretroviral drug biodistribution, underscoring the value of decorated magnetite particles as a theranostic drug discovery tool for improved drug delivery.”
“In the DNA damage response, c-Abl tyrosine kinase is transiently accumulated in the nucleus and induces apoptosis; however, little is known about the mechanism underlying apoptosis induction via nuclear c-Abl. Here we demonstrate that the

expression of human pituitary homeobox 1 (Pitx1) transcription factor is increased after DNA damage. Notably, c-Abl controls augmentation of Pitx1 at the post-transcriptional level. Overexpression of c-Abl induces tyrosine phosphorylation of Pitx1, either directly or indirectly. We also show that, upon exposure to genotoxic stress, overexpression of Pitx1 is associated with marked induction of apoptosis that is independent of p53 status. Importantly, inhibition of c-Abl kinase activity substantially attenuates Pitx1-mediated apoptosis. These findings provide evidence that c-Abl participates in modulating Pitx1 expression in the apoptotic response to DNA damage.”
“In some psychiatric disorders 5-HT2A receptors play an important role. In order to investigate those in vivo there is an increasing

interest in obtaining a metabolically stable, subtype selective and high affinity radioligand for receptor binding studies using positron emission tomography (PET). PF-04929113 clinical trial AZD5582 Combining the excellent in vivo properties of [C-11]MDL 100907 for PET imaging of 5-HT2A receptors and the more suitable half-life of fluorine-18, MDL 100907 was radiofluorinated in four steps using 1-(2-bromoethyl)-4-[F-18]fluorobenzene as a secondary labelling precursor. The complex reaction required an overall reaction time of 140 min and [+/-)-[F-18]MDL

100907 was obtained with a specific activity of at least 30 GBq/mu mol (EOS) and an overall radiochemical yield of 1-2%. In order to verify its binding to 5-HT2A receptors, in vitro rat brain autoradiography was conducted showing the typical distribution of 5-HT2A receptors and a very low non-specific binding of about 6% in frontal cortex, using ketanserin or spiperone for blocking. Thus, [F-18]MDL 100907 appears to be a promising new 5-HT2A PET ligand.”
“We varied the surface boundary-contour properties of binocular rivalry (BR) stimuli to measure the rivalry percept as a function of stimulus duration. Experiment 1 compared perception from BR stimuli with monocular boundary contour (MBC) and binocular boundary contour (BBC). We found global dominance is achieved with stimulus duration as short as 30 ms for the MBC rivalry stimuli, whereas it takes more than 150 ms for the BBC rivalry stimuli. This shows that global dominance can occur rapidly in the absence of a corresponding boundary contour in one half-image.