公开(公告)号：EP1345627A1

公开(公告)日：2003-09-24

申请号：EP01273076.8

申请日：2001-11-13

申请人： Centre National De La Recherche Scientifique ,  THE MASSACHUSETTS GENERAL HOSPITAL ,  Molecular Sciences Institute

发明人： COLAS, Pierre ,  BRENT, Roger ,  COHEN, Barak, A.

IPC分类号： A61K47/48

CPC分类号： A61K47/6425

摘要： Process for specifically modulating the properties of an intracellular target molecule T, and/or of a cellular component C which interacts directly or indirectly in a cell with T, said process comprising: introducing into a cell a chimeric molecule, a so-called 'targeted effector', comprising: a recognition moiety R, comprising a peptide V having a length of five to sixty amino acids, preferably ten to forty amino acids, conformationally constrained by covalent linking to a platform, said recognition moiety R having the capacity to specifically interact, within the cell, with a site on an intracellular target molecule T, the interaction with T occurring with an affinity A1; and an effector moiety, E covalently linked to said recognition moiety R, E being a molecule, or a portion thereof, which has an initial capacity to exert an effect on at least one molecule M, and which when it is covalently linked to R, acquires the capacity to exert the effect on the intracellular target molecule T; wherein the targeted effector interacts with T with a second affinity A2, the affinity A1 or the affinity A2 corresponding to a Kd of less than 1 x 10-8 M, and the properties of T and/or of C are specifically modulated by the effector moiety E.