血栓形成の制御を目指した多数のジスルフィド結合を持つ天然物様環状ペプチドの開発

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This research aims at discovery of de novo disulfide-rich peptides (DRPs) with desired conformations and biological activities using in vitro selection. In this year of my JSPS fellowship, I first finished the paper publication of the research that identified an ultrapotent cyclotide-based FXIIa inhibitor. This work was published on J. Am. Chem. Soc. 2021, 143, 18481-18489. In this year, I also continued the research of controlling disulfide connectivity in DRPs taking advantage of protected cysteines. In brief, I constructed bicyclic or tricyclic DRP libraries with controllable disulfide conformations and conducted in vitro selection to yield several potent target-binding peptides with designed structures. The following work is being performed and will be summarized into publications.