Anti-androgen peptides and uses thereof in cancer therapy

Abstract

The present invention relates to isolated or purified or partially purified peptide derived molecules having the following general formula (S1): X-[(Pro) n -His-Pro-His-Ala-Arg-Ile-Lys] m -Y. The peptides are for medical use, in particular as anti-tumoral agents.

1 . An isolated or purified or partially purified peptide-derived molecule having the general formula:
   X-[(Pro) n -His-Pro-His-Ala-Arg-Ile-Lys] m -Y  (S1)   wherein X is H, or an acetyl group or any natural amino acid or sequence of amino acids provided with a free or at least acetyl-derivatized NH2 group; Y is an OH group or an NH2 group or any amino acid or sequence of amino acids with a C-terminal carboxy-amide group; “n” is an integer from 1 to 10 and “m” is an integer from 1 to 3.   
     
     
         2 . The peptide-derived molecule according to  claim 1  which is effective to inhibit or prevent the interaction of the androgen receptor (AR) with the SH3 domain of the tyrosine kinase Src. 
     
     
         3 . The peptide-derived molecule according to  claim 1  having an anti-tumor activity in vitro or in vivo. 
     
     
         4 . The peptide-derived molecule according to  claim 1  having the amino acid sequence of SEQ.ID NO.1. 
     
     
         5 . The peptide-derived molecule according to  claim 1  having the amino acid sequence of SEQ.ID NO.2. 
     
     
         6 . The peptide-derived molecule according to  claim 1  having the amino acid sequence of SEQ.ID NO.3. 
     
     
         7 . The peptide-derived molecule according to  claim 1  having the amino acid sequence of SEQ.ID NO.4. 
     
     
         8 .- 10 . (canceled) 
     
     
         11 . A pharmaceutical composition comprising a pharmaceutically acceptable and effective amount of the peptide-derived molecule according to  claim 1 . 
     
     
         12 . The composition according to  claim 11  wherein said peptide is linked to a carrier molecule such as BSA or KLH and/or is comprised in a lipid composition such as a lipid particle, a nanocapsule, a liposome or lipid vesicles with a pharmaceutical excipient. 
     
     
         13 . The composition according to  claim 11  further comprising at least a second anti-cancer agent. 
     
     
         14 .- 16 . (canceled) 
     
     
         17 . An antibody able to recognize specifically a peptide-derived molecule according to any of  claim 1 . 
     
     
         18 . A nucleic acid sequence that encodes a peptide according to any of  claim 1 . 
     
     
         19 . A recombinant vector that expresses a peptide according to  claim 1 . 
     
     
         20 . Mammalian, human or bacterial host cells comprising the recombinant vector according to  claim 19 . 
     
     
         21 . A method of killing a cancer cell comprising providing the cell with a peptide-derived molecule according to  claim 1 . 
     
     
         22 . The method of  claim 21  wherein the cell is a breast or prostate cell. 
     
     
         23 . The method of  claim 21 , further comprising providing the cell with at least a second anti-cancer agent. 
     
     
         24 . A method for treating an animal affected by cancer, comprising administering to the animal a therapeutic amount of the peptide-derived molecule according to  claim 1 . 
     
     
         25 . A method for treating an animal affected by cancer, comprising administering to the animal a therapeutic amount of the composition according to  claim 1 . 
     
     
         26 . The method of  claim 24  wherein said animal is a human. 
     
     
         27 . A kit comprising an antibody according to  claim 17 , operably attached to a detectable label and immunodetection reagents in a single or multiple containers. 
     
     
         28 . The method of  claim 25 , wherein said animal is a human.