Toward the Discovery and Development of PSMA Targeted Inhibitors for Nuclear Medicine Applications
| Autor: | Andrea Ciarmiello, Sara Pastorino, Elisabetta Giovannini, Valerio Duce, Mattia Riondato, Giampiero Giovacchini, Licia Uccelli |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Male
medicine.drug_class Nuclear imaging Organophosphonates urologic and male genital diseases Monoclonal antibody NO Prostate cancer Drug Development Glutamates Spect imaging Drug Discovery PSMA Glutamate carboxypeptidase II Humans Urea Medicine Phosphoric Acids Radiology Nuclear Medicine and imaging Sulfhydryl Compounds Immunoglobulin Fragments Pharmacology Current Radiopharmaceuticals business.industry Antibodies Monoclonal Prostatic Neoplasms imaging THERAPEUTIC RADIOPHARMACEUTICALS radionuclide therapy molecular docking Pet imaging Aptamers Nucleotide Prostate-Specific Antigen medicine.disease Amides PET PSMA SPECT imaging molecular docking prostate cancer radionuclide therapy PET SPECT Radionuclide therapy Kallikreins Nuclear Medicine Radiopharmaceuticals business Nuclear medicine |
| Zdroj: | Current Radiopharmaceuticals |
| ISSN: | 1874-4710 |
| DOI: | 10.2174/1874471012666190729151540 |
| Popis: | Background::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.Results::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.Conclusion::PSMA represents for researchers the most attractive target for the detection and treatment of patients affected by PCa using nuclear medicine modalities. [99mTc]MIP-1404 is considered the tracer of choice for SPECT imaging and [68Ga]PSMA-11 is the leading diagnostic for PET imaging by general consensus. [18F]DCFPyL and [18F]PSMA-1007 are clearly the emerging PET PSMA candidates for their great potential for a widespread commercial distribution. After paving the way with new imaging tools, academic and industrial R&Ds are now focusing on the development of PSMA inhibitors labeled with alpha or beta minus emitters for a theragnostic application. |
| Databáze: | OpenAIRE |
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