abstract |
The compounds of the invention are generally described by the formula: n nB 1 Z* 2 B 3 Z* 4 X* 5 Q 6 F 7 X 8 X 9 X 10 X 11 ( 1 ), n nB 1 X 2 X 3 X 4 X 5 Q 6 F 7 X 8 X 9 X 10 X 11 ( 2 ), or n nB 1 Z 2 B 3 X 4 Z 5 Q 6 F 7 Z 8 X 9 X 10 X 11 ( 3 ) nand the salts, esters, amides, and acyl forms thereof. Each position represented by a letter indicates a single amino acid residue: B is a basic of 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 of hydrophobic amino acid or a modified form thereof. As described below, one or more of the peptide linkages between the amino acid residues may be replaced by a peptide linkage mimic. These compounds may be used as molecular building blocks to create compounds that are optimized for inhibiting the protease activity of Botulinum b and tetanus toxins. |