Design,Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders

Lysine demethylase 5 C (KDM5C) controls epigenetic gene expression and is attracting great interest in the field of chemical epigenetics. KDM5C has emerged as a therapeutic target for anti-prostate cancer agents, and recently we identified triazole 1 as an inhibitor of KDM5C. Compound 1 exhibited highly potent KDM5C-inhibitory activity in in vitro enzyme assays, but did not show strong anticancer effects. Therefore, a different approach is needed for the development of anticancer agents targeting KDM5C. Here, we attempted to identify KDM5C degraders by focusing on a protein-knockdown strategy. Compound 3 b , which was designed based on compound 1 , degraded KDM5C and inhibited the growth of prostate cancer PC-3 cells more strongly than compound 1 . These findings suggest that KDM5C degraders are more effective as anticancer agents than compounds that only inhibit the catalytic activity of KDM5C.     

Fundamental Evaluation of Power Supply and Rectifiers for Wireless Power Transfer Using Magnetic Resonant Coupling

This paper provides a fundamental analysis of a power supply and rectifiers for wireless power transfer using magnetic resonant coupling (MRC). MRC enables efficient wireless power transfer over middle‐range transfer distances. MRC for wireless power transfer should operate at a high frequency in the industry science medical band, such as 13.56 MHz, because the size of the transfer device decreases at higher transfer frequencies. Therefore, the output frequency of the power supply on the transmitting side should be 13.56 MHz. In addition, the rectifier on the receiving side is operated at a high frequency. This paper focuses on the reflected power in the power supply and rectifiers. Thus, the parametric design method is clarified for the power supply, including a low‐pass filter to match the output, the impedance of the power supply with the characteristic impedance of the transmission line. In addition, the effects on the rectifiers of silicon carbide and gallium nitride diodes are confirmed by performing an experiment and a loss analysis.     

Catalytic Aerobic Photo‐oxidation of a Methyl Group on a Heterocycle to Produce an Aldehyde via Homolytic C?I Bond Cleavage caused by Irradiation with Visible Light

A new catalytic method was developed for photo‐oxidizing the methyl group on aromatic heterocycles such as benzothiazole, benzoxazole, and quinoline to produce the corresponding aldehyde. This is the first report of the metal‐free catalytic synthesis of benzothiazole‐2‐carboxaldehydes using molecular oxygen as the terminal oxidant.

     

Precipitation recovery of boron from wastewater by hydrothermal mineralization

It is well known that boric acid exhibits various toxic effects on plant, animal and human beings even at very low concentrations. Thus, the development of boron-removal technique from wastewater has been intensively investigated. In this study, a new hydrothermal treatment technique was developed to recover boron as recyclable precipitate Ca(2)B(2)O(5).H(2)O from aqueous solutions. As a result, it was found that the hydrothermal treatment using calcium hydroxide as a mineralizer converted boron in the aqueous media effectively into calcium borate, Ca(2)B(2)O(5).H(2)O. In the optimal hydrothermal condition, more than 99% of boron was collected from the synthetic wastewater of 500 ppm. Thus, the present hydrothermal treatment in the presence of calcium hydroxide is recommended as one of the effective techniques to recover boron from aqueous media.     

Effect of weld line direction and paint orientation on corrosion and paint deterioration characteristics of welded part of steel

One thousand two hundred cycles of accelerated exposure experiment with combined salt water spray simulating atmospheric corrosion was performed for investigating the effect of weld line direction and paint orientation on the corrosion and paint deterioration characteristics of welded part of the steel. The corrosion depth of the weld toe of transverse weld line became 1.35 times as large as that of the base metal part because of the remained salt water on the weld toe. The coating thickness at the weld toe became thin by vertically painting on the transverse weld line. When the scribe line was installed at the thin painted weld toe under the transverse weld line, the paint blister area became 15% larger than that of the base metal part. The paint coating thickness at the weld toe in different weld line directions and paint orientations should be confirmed and ensured from the viewpoints of manufacturing and maintaining steel structures.     

Expression of Human DNAJ (Heat Shock Protein-40) B3 in Humanized UDP-glucuronosyltransferase 1 Mice

The human DNAJB3 gene encodes a DNAJ (Heat shock protein 40; Hsp40) homolog, subfamily B, member 3 chaperone protein (DNAJB3), which can be down-regulated in disease conditions, as observed in decreased expression of DNAJB3 mRNA in peripheral blood mononuclear cells (PBMC) of obese patients. Recently, humanized UDP-glucuronosyltransferase (UGT) 1 mice (hUGT1 mice) were developed, in which the introduced human UGT1 gene contained a gene encoding human DNAJB3. In the present study, we analyzed the expression of human DNAJB3 mRNA in hUGT1 mice. Among the examined tissues, the testis had the highest expression of human DNAJB3 mRNA, while the lowest expression was observed in the liver. We found that the pattern of tissue-specific expression of mouse Dnajb3 in hUGT1 mice was very similar to that of human DNAJB3. We further demonstrated that the expression of human DNAJB3 in the liver was significantly reduced in high-fat-diet-fed hUGT1 mice compared to the expression level in the control mice, indicating that the expression of human DNAJB3 in hUGT1 mice could be similarly regulated in disease conditions such as obesity. Humanized UGT1 mice might therefore be useful to investigate the physiological role of human DNAJB3 in vivo.     

Abstract picture generation and zooming user interface for intuitive music browsing

Today many people store music media files in personal computers or portable audio players, thanks to recent evolution of multimedia technologies. The more music media files these devices store, the messier it is to search for tunes that users want to listen to. We propose MusCat, a music browser to interactively search for the tunes according to features, not according to metadata (e.g. title, artist name). The technique firstly calculates features of tunes, and then hierarchically clusters the tunes according to the features. It then automatically generates abstract pictures, so that users can recognize characteristics of tunes more instantly and intuitionally. It finally visualizes the tunes by using abstract pictures. MusCat enables intuitive music selection with the zooming user interface.