RESUMO
Prostate cancer is the most prevalent male malignancy in the United States, and remains the second leading cause of cancer-related death in the male population. Prostate specific membrane antigen (PSMA) is a type of Ⅱ transmembrane glycoproteins that is over-expressed in prostate cancer cell. More importantly, its expression is increased with cancer progression. PSMA has been a major target for imaging and therapeutic applications in prostate cancer. PSMA, also known as N-acetylated α-linked acidic dipeptidase Ⅰ and folate hydrolase, can catalyze the hydrolysis of α-or γ-linked glutamates from peptides or small molecules. This article provides a review of the recent applications of ligand-drug conjugates targeting PSMA and prodrugs activated by PSMA.