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161.
Dr. Fumika Karaki Sho Umemoto Karin Ashizawa Tomoya Oki Noriko Sato Takumi Ogino Naoto Ishibashi Ryoto Someya Dr. Kanako Miyano Dr. Shigeto Hirayama Prof. Yasuhito Uezono Prof. Hideaki Fujii 《ChemMedChem》2019,14(21):1840-1848
Although the advantages of sp3-rich, sterically complicated molecules in drug development have been pointed out, modern screening libraries are filled with planar, sp2-rich components. Compounds that are sp3-rich are difficult to synthesize, and thus we aimed to invent an efficient method to construct sp3-rich libraries. By modifying sp3-rich 7-azanorbornane scaffolds through click chemistry, we efficiently prepared a small set of compounds. These compounds were not only sp3-rich, but also had sufficient “lead-like” properties in view of molecular weights and hydrophobicity. Screening assays of this library provided weak κ opioid receptor agonists and growth hormone secretagogue receptor agonists with high hit rates. These results indicate that the 7-azanorbornane scaffold may be a “privileged structure” for lead identification in drug discovery. 相似文献
162.
Peerawut Yutthagowith Akihiro Ametani Naoto Nagaoka Yoshihiro Baba 《IEEJ Transactions on Electrical and Electronic Engineering》2011,6(4):324-330
This article presents calculations of tower surge responses and insulator voltages of an actual transmission tower including ground wires and phase wires. The partial element equivalent circuit (PEEC) method is applied as a simulation tool. Surge responses of the tower and insulator voltages calculated by the PEEC method are compared with electro magnetic transients program (EMTP) simulated results and experimental results collected from the literatures. The results calculated by the PEEC method agree well with the experimetal results, not only amplitudes but also waveshapes. © 2011 Institute of Electrical Engineers of Japan. Published by John Wiley & Sons, Inc. 相似文献
163.
The performance of the Taylor‐Couette flow apparatus as a heat sterilizer is numerically investigated. The destruction of Clostridium botulinum and thiamine (vitamin B1) was selected as model reaction. When Taylor vortices were formed in the annular space, the heat transfer significantly enhanced as compared to the case without vortex flow. As a result, the equivalent lethality calculated from the temperature field increased, which is regarded as a quantum leap. Conversely, the improvement of heat transfer induced destruction of thiamine. These results suggest that there is a trade‐off relationship between the enhancement of heat transfer and the avoidance of thermal destruction of nutritional components. In conclusion, the Taylor‐Couette flow sterilizer has the potential for process intensification in heat sterilization processes. 相似文献
164.
Hiroyuki Koide Satoshi Hirano Takafumi Ide Kazuhiro Saito Hikaru Suzuki Go Yasuno Yoshitaka Hamashima Sei Yonezawa Naoto Oku Tomohiro Asai 《Advanced functional materials》2021,31(3):2005641
Protein affinity reagents (e.g., antibodies) are often used for basic research, diagnostics, separations, and disease therapy. Although a lot of “synthetic” protein affinity reagents have been developed as a cost-effective alternative to antibodies, their low biocompatibility is a considerable problem for clinical application. Lipid nanoparticles (LNP) represent a highly biocompatible drug delivery agent. However, little has been reported that LNP itself works as a protein affinity reagent in living animals. Here, LNP is engineered for binding to and neutralizing a target toxic peptide in living animals by multifunctionalization with amino acid derivatives. Multifunctionalized LNP (MF-LNP) is prepared using amino acid derivative-conjugated lipids. Optimized MF-LNP exhibits nanomolar affinity to the target toxic peptide and inhibits toxic peptide-dependent hemolysis and cytotoxicity. In addition, MF-LNP captures and neutralizes the toxic peptide after intravenous injection in the bloodstream; in addition, MF-LNP does not release the toxic peptide in the accumulated organ. These results reveal the potential of using LNP as a highly biocompatible protein affinity reagent such as an antidote. 相似文献
165.
Prof. Dr. Fumitaka Kudo Jiahao Zhang Shusuke Sato Dr. Akane Hirayama Prof. Dr. Tadashi Eguchi 《Chembiochem : a European journal of chemical biology》2019,20(19):2458-2462
Pactamycin is an antibiotic produced by Streptomyces pactum with antitumor and antimalarial properties. Pactamycin has a unique aminocyclitol core that is decorated with 3-aminoacetophenone, 6-methylsaliciate, and an N,N-dimethylcarbamoyl group. Herein, we show that the adenylation enzyme PctU activates 3-aminobenzoic acid (3ABA) with adenosine triphosphate and ligates it to the holo form of the discrete acyl carrier protein PctK to yield 3ABA-PctK. Then, 3ABA-PctK is N-glycosylated with uridine diphosphate-N-acetyl-d -glucosamine (UDP-GlcNAc) by the glycosyltransferase PctL to yield GlcNAc-3ABA-PctK. Because 3ABA is known to be a precursor of the 3-aminoacetophenone moiety, PctU appears to be a gatekeeper that selects the appropriate 3-aminobenzoate starter unit. Overall, we propose that acyl carrier protein-bound glycosylated 3ABA derivatives are biosynthetic intermediates of pactamycin biosynthesis. 相似文献
166.
Yutaka Kudo Tomohiro Morimura Kiminori Sugauchi Tetsuya Masuishi Norihisa Komoda 《Electrical Engineering in Japan》2015,192(1):13-24
We developed a root cause analysis (RCA) system for an enterprise IT system environment. In this paper, we propose a rule‐construction method that builds analysis rule data objects from general analysis rules and the topology information of the actual target IT environment. Using this method, the IT administrator can use the RCA system without any manual rule modifications. For the execution of the analysis, we introduce the certainty factor to realize robust analysis when the order and reachability of a fault event cannot be guaranteed. 相似文献
167.
Effects of Smart Charging of Multiple Electric Vehicles in Reducing Power Generation Fuel Cost 下载免费PDF全文
Takashi Ikegami Hitoshi Yano Koji Kudo Kazuhiko Ogimoto 《Electrical Engineering in Japan》2015,193(2):42-57
The high penetration of variable sources of renewable power generation will lead to operational difficulties in supply/demand balancing in the entire power system. The mass deployment of electric vehicles (EVs) and plug‐in hybrid vehicles (PHEVs) will also cause significant changes in electricity demand. Therefore, controlling and managing the charging time of EVs/PHEVs are effective approaches that are imperative for improving balancing in power system operation. We assumed travel patterns for EVs in a model of the future Tokyo power system and analyzed the power system loads, including the charging load of the EVs, under several charging control scenarios. We verified that charging time controls are substantially effective for reducing the fuel costs in the power system. Further, we found that load leveling under a multicar charging management scenario gave the best results in terms of the fuel costs in all cases. 相似文献
168.
Sangho Koh Seika Imamura Naoto Fujino Masahiro Mizuno Nobuaki Sato Satoshi Makishima Peter Biely Yoshihiko Amano 《Journal of Applied Glycoscience》2019,66(4):131
The carbohydrate esterase family 1 (CE1) in CAZy contains acetylxylan esterases (AXEs) and feruloyl esterases (FAEs). Here we cloned a gene coding for an AXE belonging to CE1 from Irpex lacteus (IlAXE1). IlAXE1 was heterologously expressed in Pichia pastoris, and the recombinant enzyme was purified and characterized. IlAXE1 hydrolyzed p-nitrophenyl acetate, α-naphthyl acetate and 4-methylumbelliferyl acetate, however, it did not show any activity on ethyl ferulate and methyl p-coumarate. We also examined the activity on partially acetylated and feruloylated xylan extracted from corncob by hydrothermal reaction. Similarly, ferulic and p-coumaric acids were not liberated, and acetic acid was only detected in the reaction mixture. The results indicated that IlAXE1 is an acetylxylan esterase actually reacted to acetyl xylan. However, since IlAXE1 was unable to completely release acetic acid esterifying xylopyranosyl residues, it is assumed that acetyl groups exhibiting resistance to deacetylation by IlAXE1 are present in corn cob xylan. 相似文献
169.
Naoto Miyoshi 《Discrete Event Dynamic Systems》1997,7(3):275-293
Recently, Konstantopoulos and Zazanis (1992, 1994) and Brémaud and Lasgouttes (1993) derive the infinitesimal perturbation analysis (IPA) estimators for the stationary and ergodic G/G/1/ queue using Palm calculus, where neither regenerative structure nor convex property are required and the strong consistency is ensured by ergodic theorem. This work has been motivated by them and derives the smoothed perturbation analysis (SPA) estimator on the stationary and ergodic framework. The problem here is how to treat the catastrophic jumps on the sample path of the steady state and this is solved cleverly by using the Palm calculus. We deal with multi-class queues in this paper but our key formula is expected to be useful to any systems to which the SPA is applicable. 相似文献
170.