| Summary: | Prostate-specific membrane antigen (PSMA) is the most extensively studied biomarker and antigen of prostate cancer. It is overexpressed in almost all prostate cancers, and the expression level increases with prostate cancer progression. PSMA is also highly expressed in the neovasculature of solid tumours including prostate cancer. As a result, numerous PSMA-specific ligands have been discovered for prostate cancer diagnosis and therapy, and one of them has been approved for clinical use. Moreover, a number of other PSMA-specific ligands are currently evaluated in clinical studies. In this review we discuss four major types of PSMA-specific ligands, including antibody, aptamer, peptide, and small molecule inhibitor. Their emerging applications in prostate cancer diagnosis, targeted drug delivery, and therapy are also discussed.
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