Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine

The histone methyltransferase SET7/9 methylates not only histone but also non‐histone proteins as substrates, and therefore, SET7/9 inhibitors are considered candidates for the treatment of diseases. Previously, our group identified cyproheptadine, used clinically as a serotonin receptor antagonist and histamine receptor (H1) antagonist, as a novel scaffold of the SET7/9 inhibitor. In this work, we focused on dibenzosuberene as a substructure of cyproheptadine and synthesized derivatives with various functional groups. Among them, the compound bearing a 2‐hydroxy group showed the most potent activity. On the other hand, a 3‐hydroxy group or another hydrophilic functional group such as acetamide decreased the activity. Structural analysis clarified a rationale for the improved potency only by tightly restricted location and type of the hydrophilic group. In addition, a SET7/9 loop, which was only partially visible in the complex with cyproheptadine, became more clearly visible in the complex with 2‐hydroxycyproheptadine. These results are expected to be helpful for further structure‐based development of SET7/9 inhibitors.     

The effect of lutein supplementation on visual fatigue: A psychophysiological analysis

We used psychophysiological technology to examine the effect of an oral supplement, a combination of lutein, zeaxanthin and blackcurrant extract (LUT), on visual fatigue, within the context of a randomized, double-blind, placebo-controlled cross-over trial. The LUT supplement and placebo samples were randomly assigned to thirteen participants, who took the samples for two LUT (and vice versa) for another 2 week. Each participant completed visual proof reading tasks for 2 h during each of four testing sessions. Saccade tests were administered before and after the proof reading task, during which the participants moved their eyes back and forth between two targets positioned in the center of two checkerboards. We recorded EEG, EOG, heart rate, and facial muscle potential/performance during the saccade tests. Blood pressure was measured and subjective fatigue and stress scores were collected before and after the proof reading task. We averaged EEG starting at saccade offset in order to analyze eye fixation related potentials (EFRP). Our results suggested that the proof reading task induced visual fatigue. An analysis of EFRP and other psychophysiological data revealed significant differences between the LUT and placebo conditions. These results suggest that supplementation with LUT could help to reduce symptoms of visual fatigue.     

Polyurea thin film ultrasonic transducers for nondestructive testing and medical imaging

Ultrasonic transducers using polyurea piezoelectric thin film are studied in this paper. Aromatic polyurea thin films, prepared by vapor deposition polymerization, have useful characteristics for use as an ultrasonic transducer. This paper presents the fabrication and experimental evaluation of ultrasonic transducers formed using polyurea films. First, the vapor deposition polymerization process using two monomers is briefly reviewed, and the temperature conditions for higher piezoelectric constants are explored. Second, in order to test the fundamental characteristics of this material as a high-frequency, ultrasonic transducer, a polyurea film of 2.5 microm thickness was deposited on a silicon substrate. In the pulse/echo experiment results, a resonant frequency of about 100 MHz was observed. Third, we fabricated a concave point focus transducer and a cylindrical line focus transducer. To examine the performances of the focus transducers, two-dimensional images of a coin and V(z) curve measurements for an aluminum surface were demonstrated.     

Preparation of porous membranes by selective decomposition of adamantane unit in ABA‐type triblock copolymer

The mechanism of pore formation by selective decomposition of adamantane unit in an ABA‐type triblock copolymer derived from 4,4‐(hexafluoroisopropylidene)diphthalic anhydride‐2,3,5,6‐tetramethyl‐1,4‐phenylenediamine (6FDA‐TeMPD) and poly(2‐methyl‐2‐adamantylmethacrylate) (PMAdMA) was investigated on this basis. This study aims to developing a novel method of material design for high‐precision gas separation membranes and application to electric devices by improving dielectric constant. Scanning electron microscopy images showed that the membrane structure changed considerably after heating; the difference increased with the increase in adamantane content. Interestingly, the internal structure of Block(36 mol%6FDA‐TeMPD/64 mol%PMAdMA) membrane was almost unchanged although its surface structure was changed. These results suggest that the mechanism of formation of porous membrane involves the decomposition of adamantane unit from surface. In addition, more adamantane units inside the membrane were discharged to the surface of the membrane through a path formed by decomposed adamantane units. POLYM. ENG. SCI., 56:1191–1200, 2016. © 2016 Society of Plastics Engineers     

Refinement of inverter model considering dead‐time for performance improvement in predictive instantaneous current control

Model predictive instantaneous‐current control (MPIC), which was proposed in our earlier works, enables us to achieve better instantaneous current control using mathematical models of an inverter and permanent magnet synchronous motors (PMSMs). However, dead‐time to avoid short breakdown in the inverter is not usually considered in a general inverter model. Such an unmodeled part in the inverter model prevents accurate prediction of current evolution in motor systems based on the model predictive control. Therefore, in this paper, we analyze current response resulting from the dead‐time in the MPIC, and propose a refined inverter model considering the dead‐time so that control performance is improved. The effectiveness of the proposed method is verified through simulation and experiments. © 2013 Institute of Electrical Engineers of Japan. Published by John Wiley & Sons, Inc.     

Molecular Thermal Phenomena in an Ultrathin Lubrication Liquid Film of Linear Molecules Between Solid Surfaces

Molecular dynamics simulation has been performed on an ultra-thin lubrication liquid film, where the liquid film of diatomic molecules having a thickness of molecular scale (several nanometers) is sheared by two parallel solid walls moving at different speeds. The Couette-like flow is generated and energy conversion from the macroscopic flow energy to thermal energy, which is the viscous heating in a macroscopic sense, occurs in the liquid film. It was observed in the present simulations that the thermal phenomena in the liquid film are far from the macroscopically expected ones; thermal energy is not distributed evenly to each degree of freedom of molecular motion, and energy transfer in the liquid adjacent to the solid surface is contributed by molecular motion in a manner different from those in a bulk liquid.     

Swarm robotic network using Lévy flight in target detection problem

One approach in swarm robotics is homogeneous system which is embedded with sensing, computing, mobile and communication components. In this study, a target detection problem, which is one of navigation problems, was employed. Once a robot detects a target, robots immediately communicate with a base station via intermediate relay robots due to the multi-hop transmission of wireless communication. Therefore, this control task is completed with connectivity of the network. In a target detection problem, we must improve the performance of exploration as well as connectivity of the network. This study investigates the performances of the two types of random walk algorithm in navigation while loosely ensuring connectivity of the robotic network based on our previous study.     

Influencing factors for diamond formation from several starting carbons

The possible influencing factors for diamond formation which prevent non-graphitic carbons from transforming to diamond in the presence of nickel as solvent-catalyst were pursued. The relative amount of nickel to carbon did not affect the behaviour of each starting carbon on diamond formation. The existence of a graphitic structure in the starting carbon was not the major prerequisite for diamond formation. Adsorbed gases on the starting carbon and atmospheric gases in the high pressure cell were found to be the most important influencing factors for diamond formation. Hydrogen and chemical species containing hydrogen atoms were the most harmful.