A Remote Arene-Binding Site on Prostate Specific Membrane Antigen Revealed by Antibody-Recruiting Small Molecules

Prostate specific membrane antigen (PSMA) is a membrane-bound glutamate carboxypeptidase overexpressed in many forms of prostate cancer. Our laboratory has recently disclosed a class of small molecules, called ARM-Ps (antibody-recruiting molecule targeting prostate cancer) that are capable of enhancing antibody-mediated immune recognition of prostate cancer cells. Interestingly, during the course of these studies, we found ARM-Ps to exhibit extraordinarily high potencies toward PSMA, compared to previously reported inhibitors. Here, we report in-depth biochemical, crystallographic, and computational investigations which elucidate the origin of the observed affinity enhancement. These studies reveal a previously unreported arene-binding site on PSMA, which we believe participates in an aromatic stacking interaction with ARMs. Although this site is composed of only a few amino acid residues, it drastically enhances small molecule binding affinity. These results provide critical insights into the design of PSMA-targeted small molecules for prostate cancer diagnosis and treatment; more broadly, the presence of similar arene-binding sites throughout the proteome could prove widely enabling in the optimization of small-molecule–protein interactions

Mobile and reliable data access to telematics data systems

The perspective of use the Bring Your Own Device (BYOD) model in telematics environment which ensure a reliable access to network resources is presented in the paper. The BYOD model is a future-proof solution which applies in areas related to database systems. It provides the user wireless access with the use of 802.11n/ac/d standard, mobile access via WiMax-2 or LTE-A networks and wired with the use of Gigabit Ethernet technology. The research network which reflects the events representative for the telematics environment was established for the verification of functional capabilities of BYOD model. Services that offer a user the synchronization of files between mobile terminals and data server were implemented in testbed. A detailed set of test scenarios and criteria for assessment of the declared properties model BYOD were also defined. The article presents the results of research that confirm the use of this type of networking solutions for mobile and reliable access to data in a telematics environment

Zmiany w zawartosci wybranych frakcji bialka izolowanego z siewek pszenzyta jarego poddanego dzialaniu niskiej temperatury

The obtained results indicate that in analysed seed leaves of seedlings of spring triticale ‘Kargo’ cultivar exposed to low temperature occurs a statistically significant decrease in total protein content, comparing to the control. Similar results were showed by analysing the concentration of this protein fraction in propagation joints and roots of seedlings of spring triticale ‘Kargo’ (exception propagation joints after 24 h of exposition to low temperature). Simultaneously a statistically significant increase in soluble protein content in seed leaves was found (exception 12 h of exposition to low temperature) and propagation joints after 12 h of their exposition, comparing to the control plants. Moreover, statistical analysis showed a significant increase in concentration of this protein fraction in roots of seedlings exposed to coldness after 1 and 12 h, comparing to the control