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Prostate-specific membrane antigen (PSMA) is a nonsecretory membrane enzyme with carboxypeptidase and folate hydrolase activities and a large extracellular domain. PSMA receptors have an oncogenic signaling role in prostate cancer cells, acting on glutamate receptors and activating Pi3K and Akt growth pathways. It is overexpressed in 90% of metastatic prostate cancers, with low physiological expression in normal tissues (prostate, small intestine, salivary and lacrimal glands, and kidney).