Inhibitor peptides

Abstract

The invention concerns peptides useful as MAP kinase/ERK pathway-specific inhibitors relative to a given substrate in a given subcellular compartment.

1 . A peptide comprising:
 at least one amino acid sequence which allows said peptide to penetrate into a cell;   optionally, an intracellular targeting amino acid sequence chosen from NESs;   optionally, an intracellular targeting sequence chosen from NLSs;   an amino acid sequence corresponding to a docking domain sequence of a substrate of an ERK-type MAP kinase;   optionally, at least one spacer sequence;   optionally, an enzymatic cleavage sequence possibly surrounded by spacer sequences.   
     
     
         2 . The peptide as claimed in  claim 1 , such that said docking domain sequence is chosen from the D or FXFP domains of the substrates of ERK-type MAP kinases. 
     
     
         3 . The peptide as claimed in  claim 1 , such that said sequence which allows said peptide to penetrate into a cell is chosen from the sequences of an HIV-TAT penetrating peptide, of penetratin, and the 7/11R or X7/11R sequences. 
     
     
         4 . The peptide as claimed in  claim 1 , which is coupled to a fluorophore, preferably covalently, or to an enzyme such as beta-galactosidase, or which is biotinylated. 
     
     
         5 . A nucleic acid encoding a peptide as claimed in  claim 1 . 
     
     
         6 . An expression vector comprising a nucleic acid as claimed in  claim 5 . 
     
     
         7 . A kit containing at least one peptide as claimed in  claim 1  and/or at least one expression vector as claimed in  claim 6 . 
     
     
         8 . The use of a peptide as claimed in  claim 1 , as an inhibitor, in vivo or in vitro, of the activity of said ERK-type MAP kinase relative to a given substrate in a given cell compartment. 
     
     
         9 . A non-human, transgenic mammal, in particular a rodent, capable of expressing at least one peptide as claimed in  claim 1 , which can, for example, be obtained by transgenesis using a vector as claimed in  claim 6 .