Mu-Conotoxin Peptides And Use Thereof As A Local Anesthetic

Abstract

The present invention relates to novel mu-conotoxin peptides, biologically active fragments thereof, combinations thereof and/or variants thereof. The invention also relates to their use in pharmaceutical composition for the treatment or prevention of pain, and their use in the preparation of an anesthetic.

1 - 28 . (canceled) 
     
     
         29 . An isolated and purified nucleic acid sequence comprising
 i) a nucleotide sequence encoding a mu-conotoxin peptide consisting of the amino acid sequence: Xaa1-Xaa2-Cys-Cys-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Cys-Xaa8-Xaa9-Xaa10-Xaa11-Cys-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-Cys-Cys-Xaa17 [SEQ ID NO:1], wherein
 Xaa1 is any N-modified amino acid, 
 Xaa2 is glycine, 
 Xaa3 is absent or is any acidic amino acid or any of its amide form, 
 Xaa4 is absent or is glycine, 
 Xaa5 is absent or is proline or hydroxy-proline, 
 Xaa6 is absent or is any basic amino acid, 
 Xaa7 is absent or is glycine, 
 Xaa8 is absent or is any non-aromatic hydroxyl amino acid, 
 Xaa9 is absent or is any non-aromatic hydroxyl amino acid, 
 Xaa10 is absent or is any basic amino acid, 
 Xaa11 is absent or is any aromatic amino acid, 
 Xaa12 is absent or is any basic amino acid, 
 Xaa13 is absent or is any acidic amino acid or any of its amide form, 
 Xaa14 is absent or is any basic amino acid, or any sulfur-containing amino acid, 
 Xaa15 is absent or is any hydrophobic or apolar amino acid, or any non-aromatic hydroxyl amino acid, 
   Xaa16 is absent or is any basic amino acid,   Xaa17 is absent or is any apolar amino acid, or an amide group,   ii) a nucleic acid sequence complementary to i),   iii) a degenerated nucleic acid sequence of i) or ii),   iv) a nucleic acid sequence capable of hybridizing under stringent conditions to or iii),   v) a nucleic acid sequence encoding a truncation or an analog of the mu-conotoxin peptide,   vi) and/or a fragment of i), ii), iii), or v) encoding a biologically active fragment of the mu-conotoxin peptide.   
     
     
         30 . A vector comprising the isolated and purified nucleic acid sequence of  claim 29 .