PEPTIDE ANTAGONIST OF MULTIPLE CHEMOKINE RECEPTORS AND USES THEREOF

摘要

The present invention provides a peptide, with the structure of Formula (I), having antagonist activity toward multiple chemokine receptors: NH2-F P M F K R G R - X wherein X is: C; K; a covalent linker; C* --- C* R G R K F M P F - NH2, wherein C* --- C* represents a disulphide bridge; K - R G R K F M P F - NH2, wherein K - R represents an amide bond between the epsilon -amino group of K and the carboxyl group of R; or a covalent linker additionally bound to a second NH2 - F P M F K R G R at its C- terminal R, and wherein NH2 represents the N-terminus. The present invention also teaches methods for the production and testing of the peptide antagonist, in addition to methods of chemically modifying the peptide of Formula (I) to enhance bioavailability and/or activity. Also provided is a therapeutic method comprising administration of the peptide antagonist to a patient in need of a reduction of chemokine receptor(s) function in the treatment of inflammatory diseases or disorders or for the prevention or reduction of HIV infection.