Schematic representation of PSMA molecular structure. PSMA inhibitors (PSMAi) expolit glutamate carboxypeptidase enzymatic activity of the extracellular domain of PSMA and can be labeled either with positron-emitting nuclides (e.g., 68Ga, 64Cu, 18F) for imaging or with beta/alpha emitting radioisotopes (e.g., 177Lu, 213Bi, 225Ac) for radionuclide therapy. Monoclonal antibodies (MoAbs) have also been developed: 111In-capromab is directed towards the intracellular PSMA domain and is utilized for scintigraphic imaging, 89Zr-DFO-J591 targets the extracellular portion of PSMA and is suitable for PET imaging (figure created with Biorender.com (accessed on 8 March 2021)).