abstract |
This is a method for specifically modulating the properties of an intracellular target molecule T and / or an intracellular component C that interacts directly or indirectly with T within a cell. Effector directed to the target, wherein the effector directed to the target is conformationally constrained by a covalent bond to a platform and is 5-60 amino acids in length, preferably 10-10 amino acids. It comprises a recognition moiety R containing 40 peptides V and an effector moiety E covalently linked to this recognition moiety R. The recognition moiety R has the ability to act on site-specifically cross on intracellular target molecule T intracellularly, the interaction takes place with an affinity A 1. The effector moiety E has an initial ability to exert an effect on at least one molecule, and a molecule that acquires the ability to exert an effect on an intracellular target molecule T when bound to R by a covalent bond. Or its protein. Effectors directed to the targets interact with T and the second affinity A 2, affinity A 1 or A 2 corresponds to the K d values of less than 1 × 10 -8 M. The properties of T and / or C are specifically modulated by the effector moiety E. |