A pro-moiety for forming a prodrug selectively cleaved by prostate-specific antigen (psa)

Abstract

A pro-moiety and a composition comprising a pro-moiety for use in a therapeutically or diagnostically effective amount in a method for detecting and/or treating prostate cancer in a subject is disclosed. The pro-moiety comprises a first peptide, and a second peptide that is linked to the first peptide, wherein the peptide comprises a sequence that is configured near a first terminus for conjugating to a drug to form a prodrug that is rapidly and/or highly selectively cleaved by prostate-specific antigen (PSA), and configured at a second terminus to bind with high selectivity to the active site of PSA, and the second peptide comprises a sequence having a negative charge to slow uptake of the prodrug by cells, and wherein the second peptide is cleaved from the first peptide upon proteolysis by PSA to produce a conjugate of the first peptide and the drug that is suitable for uptake by target cells.

Dependencies are inferred from the claim text.