BUFORNIN 1 AS A SPECIFIC INHIBITOR AND THERAPEUTIC AGENT FOR BOTULINUM TOXIN B AND TETANUS NEUROTOXINS

摘要

The compounds of the invention are generally described by the formula (I): X1X2B3X4B5X*6X7X8B9X10B11X12B13X14B15X16B17X*18X*19B20X21X22X23Q24F25Z*26X27X28B29X30B31B32X33X34B35B36X37Z38Z39, and the salts, esters, amides, and acyl forms thereof. Up to 15 amino acids may be truncated from the N-terminus and up to 6 amino acids may be truncated from the C-terminus. Each position represented by a letter indicates a single amino acid residue wherein B is a basic or polar/large amino acid or a modified form thereof; X is a small or hydrophobic amino acid or a modified form thereof; X* is a small or polar/large amino acid or a modified form thereof; Z is a polar/large or hydrophobic amino acid or a modified form thereof; Z* is Proline or a polar/large or hydrophobic amino acid or a modified form thereof. These compounds may be used to inhibit the protease activity of Botulinum B and tetanus toxins.