Toward the Discovery and Development of PSMA Targeted Inhibitors for Nuclear Medicine Applications.

Current Radiopharmaceuticals
Sara PastorinoAndrea Ciarmiello

Abstract

The rising incidence rate of prostate cancer (PCa) has promoted the development of new diagnostic and therapeutic radiopharmaceuticals during the last decades. Promising improvements have been achieved in clinical practice using prostate specific membrane antigen (PSMA) labeled agents, including specific antibodies and small molecular weight inhibitors. Focusing on molecular docking studies, this review aims to highlight the progress in the design of PSMA targeted agents for a potential use in nuclear medicine. Although the first development of radiopharmaceuticals able to specifically recognize PSMA was exclusively oriented to macromolecule protein structure such as radiolabeled monoclonal antibodies and derivatives, the isolation of the crystal structure of PSMA served as the trigger for the synthesis and the further evaluation of a variety of low molecular weight inhibitors. Among the nuclear imaging probes and radiotherapeutics that have been developed and tested till today, labeled Glutamate-ureido inhibitors are the most prevalent PSMA-targeting agents for nuclear medicine applications. PSMA represents for researchers the most attractive target for the detection and treatment of patients affected by PCa using nuclear medi...Continue Reading

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Citations

May 1, 2021·Biomedicines·Susana Hernando PoloFelipe Couñago
May 30, 2021·Prostate Cancer and Prostatic Diseases·Fujin WangMei Lin
Dec 20, 2019·Bioconjugate Chemistry·Albertus Wijnand HensbergenFijs W B van Leeuwen

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Methods Mentioned

BETA
biopsy
imaging techniques
xenografts

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NCT02349022
NCT02916537
NCT01417182
NCT01815515
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NCT02615067

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UCFS Chimera

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