Patent ID: 6767896
Filing Date: 2004-07-27
Classification: A61K,C07K,Y10S

Abstract:
A substantially pure conotoxin peptide having the general formula I:Xaa-Xaa0-Xaa1-Cys-Cys-Gly-Xaa2-Xaa3-Xaa4-Cys-Xaa5-Xaa6-Cys-Xaa7 (SEQ E) NO:1), wherein Xaa is des-Xaa, Asn, Gln or pyro-Glu; Xaa0 is des-Xaa0, Gly, Ala, Glu, &ggr;-carboxy-Glu (Gla) Asp, Asn, Ser, Thr, g-Asn (where g is glycosylation), g-Ser or g-Thr; Xaa1 is Val, Ala, Gly, Leu, Ile, Ser, Thr, g-Asn, g-Ser or g-Thr; Xaa2 is Phe, Tyr, meta-Tyr, ortho-Tyr, nor-Tyr, mono-halo-Tyr, di-halo-Tyr, O-sulpho-Tyr, O-phospho-Tyr, nitro-Tyr, Trp (D or L), neo-Trp, halo-Trp (D or L), any non-natural aromatic amino acid, an aliphatic amino acid bearing linear or branched saturated hydrocarbon chains or a non-natural derivative of the aliphatic amino acid; Xaa3 is Lys, Arg, homolysine, homoarginine, ornithine, nor-Lys, His, N-methyl-Lys, N,Nâ€²-dimethyl-Lys, N,Nâ€²,Nâ€³-trimethyl-Lys, any non-natural basic amino acid, Ser, Thr, g-Ser, g-Thr or any non-natural hydroxylated residue; Xaa4 is an aliphatic amino acid bearing linear or branched saturated hydrocarbon chains or a non-natural derivative of the aliphatic amino acid, Met, Phe, Tyr, meta-Tyr, ortho-Tyr, nor-Tyr, mono-halo-Tyr, di-halo-Tyr, O-sulpho-Tyr, O-phospho-Tyr, nitro-Tyr, Trp (D or L), neo-Trp, halo-Trp (D or L) or any non-natural aromatic amino acid; Xaa5 is His, Ser, Thr, g-Ser, g-Thr, an aliphatic amino acid bearing linear or branched saturated hydrocarbon chains, a non-natural derivative of the aliphatic amino acid, Phe, Tyr, meta-Tyr, ortho-Tyr, nor-Tyr, mono-halo-Tyr, di-halo-Tyr, O-sulpho-Tyr, O-phospho-Tyr, nitro-Tyr, Trp (D or L), neo-Trp, halo-Trp (D or L) or a non-natural aromatic amino acid; Xaa6 is Pro, hydroxy-Pro (Hyp) or g-Hyp; Xaa7 is des-Xaa7, Gly, Ala, Lys,Arg, homolysine, homoarginine, ornithine, nor-Lys, His, N-methyl-Lys, N,Nâ€²-dimethyl-Lys, N,Nâ€²,Nâ€³-trimethyl-Lys or any non-natural basic amino acid; and the C-terminus contains a free carboxyl group or an amide group.