Long lasting anti-angiogenic peptides
AssigneeConjuChem Biotechnologies Inc.
InventorsDominique P. Bridon, Michele Rasamoelisolo, Karen Thibaudeau, Xicai Huang, Richard Beliveau
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Abstract
Modified anti-angiogenic peptides are disclosed. The modified peptides are capable of forming a peptidase stabilized anti-angiogenic peptide. The modified anti-angiogenic peptides, particularly modified kringle 5 peptides are capable of forming a conjugate with a blood protein. Conjugates are prepared from anti-angiogenic peptides, particularly kringle 5 peptides, by combining the peptide with a reactive functional group with a blood protein. The conjugates may be formed in vivo or ex vivo. The conjugates are administered to patients to provide an anti-angiogenic effect.
Claims18
A conjugate formed by a method comprising covalently coupling a modified kringle 5 peptide with human serum albumin, wherein the modified kringle 5 peptide comprises a kringle 5 peptide and a maleimido group coupled to the kringle 5 peptide, optionally via a linking group;
- wherein the kringle 5 peptide is a peptide fragment of amino acid residues 443 to 546 of SEQ ID NO:
- 1, of between 4 and 104 amino acids, and optionally having an amino acid substitution at Cys523;
- wherein the maleimido group and optional linking group is optionally coupled to the kringle 5 peptide by one or more additional amino acids;
- wherein the kringle 5 peptide is optionally coupled to an N-terminal protecting group;
- wherein the kringle 5 peptide has an α-C-terminal carboxy, an α-C-terminal carboxamide, or an α-C-terminal alkylcarboxamide;
- wherein said maleimido group reacts with a thiol group of Cys34 of said human serum albumin to form a conjugate that has a 1:1 loading of said kringle 5 peptide to said human serum albumin.
Dependencies are inferred from the claim text.