Novel Melanocortin Receptor Templates, Peptides, and Use Thereof

Abstract

The present invention relates to novel chimeric peptides and templates containing a combination of antagonist and agonist endogenous ligand residues. In particular, the present invention relates to novel chimeric peptides and templates thereof based upon melanocortin agonist peptides and agouti related protein (AGRP). The present invention provides multifunctional chimeric peptides having specific bioactivity at melanocortin receptors and their use as drugs to treat various diseases and conditions.

1 . A peptide that is biologically active at melanocortin receptors comprising a cyclic MTII heptapeptide template and hAGRP(111-113) bioactive determinant sequences which have been substituted for the analogous template sequences, wherein
 a) the hAGRP(111-113) bioactive determinant sequence is selected from the group consisting of:
 i) Arg-Phe-Phe; 
 ii) Pbe-Phe-Arg; 
 iii) DArg-Phe-Phe; 
 iv) Arg-DPhe-Phe; and 
 v) Arg-Phe-DPhe. 
   
     
     
         2 . The peptide according to  claim 2 , wherein the peptide is of any SEQ ID NOS:20-23. 
     
     
         3 . A composition comprising a peptide of  claim 2 . 
     
     
         4 . The composition according to  claim 3 , wherein the composition is an oral pharmaceutical composition.