Patent ID: 7279549

Claim:
An isolated α-conotoxin peptide selected from the group consisting of (i) a peptide having the amino acid sequence Gly-Cys-Cys-Ser-Asp-Xaa 5 -Arg-Cys-Arg-Xaa 4 -Arg-Cys-Arg (SEQ ID NO:9), wherein Xaa 4 is Tyr, nor-Tyr, mono-halo-Tyr, di-halo-Tyr, O-sulpho-Tyr, O-phospho-Tyr or nitro-Tyr; and Xaa 5 is Pro or hydroxy-Pro; and the C-terminus contains a carboxyl or amide group, and or (ii) a derivative thereof, wherein the derivative is a peptide of (i) in which a Ser residue may be substituted with Thr or a Ser residue modified to contain an O-glycan; an Arg residue may be substituted by Lys, ornithine, homoarginine, N-methyl-Lys, N,N-dimethyl-Lys, N,N,N-trimethyl-Lys or an unnatural basic amino acid; a Tyr residue may be substituted with an unnatural hydroxy containing amino acid, a 3-hydroxyl or 2-hydroxyl isomer of Tyr or a corresponding O-sulpho-derivative or O-phospho-derivative; the Cys residues may be in D or L configuration or may be substituted with homocysteine in the D or L configuration or pairs of Cys residues may be replaced pairwise with a Ser/(Glu or Asp) combination or a Lys/(Glu or Asp) combination; an Asp residue may be substituted with a synthetic acidic bioisoteric amino acid surrogate; and wherein the unnatural basic amino acid is selected from the group consisting of N-1-(2-pyrazolinyl)-Arg, 2-(4-piperinyl)-Gly, 2-(4-piperinyl)-Ala, 2-[3-(2S)pyrrolininyl)-Gly and 2-[3-(2S)pyrrolininyl)-Ala; the unnatural hydroxy containing amino acid is selected from the group consisting of 4-hydroxymethyl-Phe, 4-hydroxyphenyl-Gly, 2,6-dimethyl-Tyr and 5-amino-Tyr; and the synthetic acidic bioisoteric amino acid surrogate is selected from the group of a tetrazolyl derivative of Gly and a tetrazolyl derivative of Ala.