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    • 1. 发明申请
    • Azoline Compound and Azole Compound Library and Method for Producing Same
    • 唑啉化合物和唑类化合物库及其制备方法
    • US20140113830A1
    • 2014-04-24
    • US14003506
    • 2012-03-09
    • Hiroaki SugaYuki GotoYumi Ito
    • Hiroaki SugaYuki GotoYumi Ito
    • G01N33/543
    • G01N33/54393C07K14/47C12N15/1062C12P17/16C12P21/02C12Q1/37G01N2500/00
    • An object of the present invention is to provide a method of efficiently constructing a library abundant in diversity and also usable for screening of a compound that binds to a target substance having protease activity.The present invention provides a method of constructing an azoline compound library containing two or more azoline compounds having an azoline backbone introduced into at least one of Cys, Ser, Thr, and 2,3-diamino acid, and analogs thereof of Xaa0 of a peptide represented by the following formula (I): A-(Xaa0)n-B  (I) [wherein, m numbers of Xaa0s respectively represent arbitrary amino acids, at least one of which is an amino acid selected from the group consisting of Cys, Ser, Thr, and 2,3-diamino acid, and analogs thereof, m represents an inter selected from 2 to 40, and A and B each independently represent a peptide composed of from 0 to 100 amino acids].
    • 本发明的目的是提供一种有效地构建多样性丰富的文库并且也可用于筛选结合具有蛋白酶活性的目标物质的化合物的方法。 本发明提供一种构建含有两个或更多个具有引入到Cys,Ser,Thr和2,3-二氨基酸中的至少一种的唑啉主链的二环或二唑化合物的唑啉化合物文献的方法,以及肽类似物的Xaa0 由下式(I)表示:A-(Xaa0)nB(I)[其中,Xaa0的m个数分别表示任意氨基酸,其中至少一个是选自Cys,Ser, Thr和2,3-二氨基酸及其类似物,m表示选自2至40个,A和B各自独立地表示由0至100个氨基酸组成的肽]。