Synthesis and biological evaluation of an albumin-binding prodrug of doxorubicin that is cleaved by prostate-specific antigen (PSA) in a PSA-positive orthotopic prostate carcinoma model (LNCaP)

The prostate‐specific antigen (PSA) is a serine protease that is over‐expressed in prostate carcinoma and represents a molecular target for selectively releasing an anticancer agent from a prodrug formulation. We have recently investigated a macromolecular prodrug strategy for improved cancer chemotherapy based on 2 features: ( i ) rapid and selective binding of thiol‐reactive prodrugs to the cysteine‐34 position of endogenous albumin after...