公开(公告)号：EP2393519A1

公开(公告)日：2011-12-14

申请号：EP10704093.3

申请日：2010-02-04

申请人： Medical Research Council

发明人： WINTER, Gregory Paul ,  HEINIS, Christian ,  BERNARD, Elise ,  LOAKES, David ,  TITE, John Paul ,  VAYSBURD, Marina ,  TEUFEL, Daniel Paul

IPC分类号： A61K47/48 ,  G01N33/68

CPC分类号： C12N15/1037 ,  A61K47/55 ,  A61K47/64 ,  A61K47/643 ,  C07K14/001 ,  C12N15/1044 ,  C12N15/1058 ,  C40B40/08 ,  C40B40/10 ,  C40B50/06 ,  G01N33/531

摘要： The invention relates to a method for modifying one or more peptide ligands, comprising polypeptides covalently linked to a molecular scaffold at two or more amino acid residues, comprising the steps of providing one or more peptide ligands, wherein the polypeptide comprises two or more reactive groups which form a covalent linkage to the molecular scaffold, and at least one loop which comprises a sequence of two or more amino acids subtended between two of said reactive groups; exposing the peptide ligands to one or more proteases; and sorting the ligands according to the extent of proteolytic cleavage.

摘要翻译： 本发明涉及一种修饰一种或多种肽配体的方法，其包括在两个或多个氨基酸残基处共价连接到分子支架的多肽，包括提供一个或多个肽配体的步骤，其中所述多肽包含两个或多个反应性基团 其形成与分子支架的共价键，以及至少一个环，其包含在两个所述反应性基团之间对位的两个或更多个氨基酸的序列; 将肽配体暴露于一种或多种蛋白酶; 并根据蛋白水解切割的程度对配体进行分选。