PSMA

PSMA ligands bind prostate-specific membrane antigen (PSMA), a cell-surface glutamate carboxypeptidase. A complementary DNA encoding PSMA was cloned in 1993 from a human prostate carcinoma cell line. In 1996 the protein was shown to act as a hydrolase with the substrate and inhibitor profile of a neuropeptidase that cleaves N-acetylaspartylglutamate. The enzyme is also known as glutamate carboxypeptidase II and folate hydrolase 1 (FOLH1). Many compounds here carry a urea-linked glutamate motif that fits the active site, coupled to a chelator or labeling group. PSMA-11 carries a chelator for gallium-68, while PSMA-1007 and piflufolastat are fluorinated ligands. tert-Butyl-DCL is a protected inhibitor intermediate, and PSMA-ALB-56 adds an albumin-binding group.