Compounds that bind to p185 and methods of using the same
AssigneeThe Trustees of the University of Pennsylvania
InventorsMark I. Greene, Ramachandran Murali, Alan Berezov
Life of this patent
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Abstract
Novels peptides and pharmaceutical compositions comprising the same are disclosed. Conjugated compositions peptides linked to detectable agents and/or cytotoxic agents. are disclosed. Method of detecting tumors that have p185 on tumor cell surfaces are disclosed. Methods of preventing transformation of a normal cell into a tumor cell in an individual at risk of developing a tumor having tumor cells which have p185 on their surfaces are disclosed. Methods of treating an individual who has cancer characterized by tumor cells that have a p185 on their cell surfaces are disclosed.
Claims38
A peptide having the formula:
- R1—R2—R3—R4—R5
- wherein:
- R1 is O-benzyloxy or 1-4 amino acid residues including at least one of tyrosine or phenylalanine;
- R2 is a linking moiety which bonds with R1, R3 and R4 such that a portion of said peptide is cyclicized;
- R3 is 5 amino acids;
- R4 is a linking moiety which bonds with R3, R5 and R2 such that a portion of said peptide is cyclicized;
- R5 is 1-13 amino acid residues and at least one of which is tyrosine or phenylalanine;
- wherein:
- R1, R2, R3, R4, and R5 taken together, are 20 amino acids or less;
- and R3 is has the formula:
- R31—R32—R33—R34—R35;
- wherein:
- R31 is aspartic acid;
- R32 is glycine;
- R33 is phenylalanine, tyrosine, tryptophan, histidine, D-phenylalanine, D-tyrosine, D-tryptophan, or D-histidine;
- R34 is tyrosine;
- and
- R35 is alanine, glycine, proline, D-alanine, D-glycine, or D-proline;
- and the carboxy terminus of R5 is either amidated or hydroxylated.
A conjugated composition comprising a peptide linked to a detectable agent and/or cytotoxic agent, wherein the peptide has the formula:
- R6—R7—R8—R9—R10
- wherein
- R6 is 1-4 amino acid residues including at least one of tyrosine or phenylalanine;
- R, is cysteine;
- R8 is 5-7 amino acids;
- R9 is cysteine;
- RIO is 1-13 amino acid residues and at least one of which is tyrosine or phenylalanine;
- wherein:
- R6, R, R8, R9, and RIO taken together, are 20 amino acids or less;
- and R8 has the formula
- R8,-R82-R83
- wherein
- R8, is glycine-aspartic acid, proline-aspartic acid, or aspartic acid;
- R82 is glycine, proline or proline-proline;
- and R83 is phenylalanine-tyrosine-alanine;
- and the carboxy terminus of RIO is either amidated or hydroxylated.
Dependencies are inferred from the claim text.