Diagnostic probes and therapeutics targeting uPA and uPAR

US6896870B1 · kind B1 · utility

Assignee

• Angstrom Pharmaceuticals, Inc. · US

Inventors

• Andrew P. Mazar · San Diego, US
• Terence R. Jones · San Diego, US

Key dates

• Filing date: Sep 27, 2000
• Grant date: May 24, 2005
• Expiry date: Dec 18, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K14/811
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A uPAR-targeting protein or peptide is diagnostically or therapeutically labeled and used in methods of diagnosis of therapy. The labeled protein or peptide preferably has the following properties: it comprises at least 38 amino acid residues, including residues 13-30 of the uPAR-binding site of uPA; competes with labeled DFP-uPA for binding to a cell or molecule that has a binding site for uPA, and has an IC50 value of about 10 nM or less; and is not a fusion protein wherein the uPA peptide is fused to another non-uPA protein or peptide. Preferred molecules are uPA, scuPA, tcuPA, an N-terminal fragment of uPA, residues 1-135, an N-terminal fragment of uPA, residues 1-143, an N-terminal fragment of uPA, residues 1-43; or an N-terminal fragment of uPA, residues 4-43. Detectable labels include a radionuclide, a PET-imageable agent, an MRI-imageable agent, a fluorescer, a fluorogen, a chromophore, a chromogen, a phosphorescer, a chemiluminescer or a bioluminescer. The disclosed methods are used to inhibit cell migration, cell invasion, cell proliferation or angiogenesis, or to induce apoptosis, preferably in the treatment of a subject having a disease or condition associated with unde…