专利号:US-9783800-B2 优先权日:2014-02-03 标 题:Method for producing peptides having azole-derived skeleton 发明人:SUGA HIROAKI; GOTO YUKI; KATO YASUHARU 权利人:UNIV TOKYO 摘要:Object of the present invention is to develop an artificial synthesis system of various peptides having an azole derivative structure and develop a library of such peptides. The present invention provides a method of producing a peptide having, in the backbone thereof, an azole derivative structure comprising the step of: synthesizing a substrate peptide of an azoline structure introducing enzyme having, in the modified region thereof, at least any one of the following amino acids, n n[in any of the compounds,n X 1 represents a group selected from the group consisting of SH, OH, NH 2 , SR 1 , OR 1 , NHR 1 , and N 3 (R 1 represents a protecting group), X 2 represents an easily eliminable group; and X 3 represents hydrogen or a substituted or unsubstituted alkyl or aryl group having from 1 to 10 carbon atoms]; reacting the substrate peptide with an azoline structure introducing enzyme to obtain a peptide having an azoline derivative structure; and converting the azoline derivative structure of the resulting peptide into an azole derivative structure by inducing an HX 2 elimination reaction of X 2 group.
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