Abstract: The compounds of the invention are generally described by the formula: B1Z*2B3Z*4X*5Q6F7X8X9X10X11 ??(1), B1X2X3X4X5Q6F7X8X9X10X11 ??(2), or B1Z2B3X4Z5Q6F7Z8X9X10X11 ??(3) and 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.
Type:
Application
Filed:
November 4, 2005
Publication date:
November 2, 2006
Applicant:
Army, Government of the United States Department of the Army
Inventors:
Richard Gordon, Deborah Moorad, Bhupendra Doctor, Gregory Garcia
Abstract: The compounds of the invention are generally described by the formula: B1Z*2B3Z*4X*5Q6F7X8X9X10X11 ??(1), B1X2X3X4X5Q6F7X8X9X10X11 ??(2), or B1Z2B3X4Z5Q6F7Z8X9X10X11 ??(3) and 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.
Type:
Application
Filed:
May 27, 2004
Publication date:
May 26, 2005
Applicant:
Army, Government of the United States Department of the Army
Inventors:
Richard Gordon, Deborah Moorad, Bhupendra Doctor, Gregory Garcia