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• W1640214770 abstract "The prostate-specific membrane antigen (PSMA) represents an ideal target for imaging and targeted therapy of prostate cancer (PC) for several reasons: PSMA is a type II transmembrane protein with glutamate-carboxypeptidase activity and a known substrate, which is optimal for developing small molecule radiopharmaceuticals, typically showing fast blood clearance and excretion resulting in low background activity. Furthermore, upon ligand binding PSMA is internalised via clathrin-coated pits and subsequent endocytosis with an effective transport of the bound molecule into the cells. Since internalisation leads to enhanced tumour uptake and retention, targeting PSMA is expected to result in high image quality for diagnostic procedures and a high local intracellular deposit for therapeutic applications. In addition, PSMA is a cell surface protein that shows a significant overexpression on PC cells and especially in advanced stage PC with a low expression in normal human tissues. Therefore, several groups engaged in the development of PSMA ligands for diagnosis and therapy of PC, either based on antibodies or on small molecules [1–4]. Studies using the radiolabelled anti-PSMA monoclonal antibody J591 have shown targeting of PSMAexpressing PC. Although antibodies offer a potential for tumour imaging, their effectiveness as diagnostic radiopharmaceuticals is limited by a long biological half-life and poor tumour penetrability, particularly for bone metastases. Recent developments may overcome these limitations, such as combination with longer-lived positron emission tomography (PET) radionuclides such as Zr and Cu [1] or" @default.
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• W1640214770 date "2016-03-01" @default.
• W1640214770 modified "2023-09-26" @default.
• W1640214770 title "Positron Emission Tomography–computed Tomography with Prostate-specific Membrane Antigen Ligands as a Promising Tool for Imaging of Prostate Cancer" @default.
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• W1640214770 doi "https://doi.org/10.1016/j.eururo.2015.08.059" @default.
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