| 书目名称 | Total Synthesis of Thielocin B1 as a Protein-Protein Interaction Inhibitor of PAC3 Homodimer | | 编辑 | Kosuke Ohsawa | | 视频video | http://file.papertrans.cn/927/926639/926639.mp4 | | 概述 | Nominated by Tohoku University as an outstanding Ph.D. thesis.Provides efficient information for a rare inhibitor of protein–protein interactions (PPIs).Reconfirms the potential of complicated natural | | 丛书名称 | Springer Theses | | 图书封面 |  | | 描述 | .This book focuses on thielocin B1 (TB1), which was found to be an inhibitor of protein–protein interactions (PPIs) of proteasome assembling chaperone (PAC) 3 homodimer, and elucidates the mechanism by nuclear magnetic resonance (NMR) studies. Interfaces of PPIs recently have been expected to be novel therapeutic targets, while it is difficult to apply conventional methodology based on lock and key theory. The author achieved the first total synthesis of TB1 and its spin-labeled derivative to carry out NMR experiments because the supply of TB1 from natural sources was limited. Unique 2,2’,6,6’-tetrasubstituted diphenyl ether moiety of TB1 was synthesized from a depsidone skeleton by chemoselective reduction of lactone. In the process of elongating side wings, efficient formylation utilizing dichloromethyl methyl ether–silver trifluoromethanesulfonate was developed for the sterically hindered aromatic compound. NMR titration experiments and paramagnetic relaxation enhancement observation of PAC3 homodimer were performed with synthesized TB1 and its molecular probe, respectively. The results of the above NMR studies and additional .in silico. docking studies suggested that TB1 promot | | 出版日期 | Book 2015 | | 关键词 | 2,2’,6,6’-Tetrasubstituted Diphenyl Ether; Docking Study; Effects Observation; PPIs; PRE Effects Observa | | 版次 | 1 | | doi | https://doi.org/10.1007/978-4-431-55447-9 | | isbn_softcover | 978-4-431-56287-0 | | isbn_ebook | 978-4-431-55447-9Series ISSN 2190-5053 Series E-ISSN 2190-5061 | | issn_series | 2190-5053 | | copyright | Springer Japan 2015 |
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