Patent ID: 8598314

Claim:
A method for synthesizing a peptide-peptidase inhibitor conjugate having peptide comprising the structure: peptide-linker-peptidase inhibitor, wherein the linker is optional; wherein the method comprises: a) coupling a peptidase inhibitor to a resin under conditions suitable to form a resin-bound peptidase inhibitor, wherein the peptidase inhibitor comprises a peptidase inhibitor core and an initial linker covalently hound thereto, wherein the peptidase inhibitor comprises a first amine and a second amine, and wherein the peptidase inhibitor is coupled to the resin through the first amine; b) optionally coupling at the second amine an extended linker to form the optional linker, wherein the extended linker comprises an amine which replaces the second amine; c) coupling the peptide, one or more amino acids, or one or more fragments of the peptide at the second amine under conditions suitable to form the peptide-peptidase inhibitor conjugate; and d) cleaving the peptide-peptidase inhibitor conjugate from the resin, thereby providing the peptide-peptidase inhibitor conjugate; wherein the peptide comprises the amino acid sequence of any one of SEQ ID NOs:1-189, 190-232, 268, 269, and 274.