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Prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein highly overexpressed in prostate carcinoma and expressed in all types of prostatic tissue, including benign, dysplastic, and malignant cells. PSMA is also found on the neovasculature of most solid tumors but has minimal expression in normal tissues outside the prostate. It acts as a glutamate-preferring carboxypeptidase and is a target for diagnostic imaging and therapeutic interventions in prostate cancer.
PSMA inhibitors bind to the active site of PSMA, inhibiting its enzymatic activity. Antibody-drug conjugates bind to PSMA and are internalized, delivering a cytotoxic payload to the tumor cell.
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