Journal
PHARMACEUTICALS
Volume 7, Issue 5, Pages 517-529Publisher
MDPI
DOI: 10.3390/ph7050517
Keywords
PSMA; prostate-specific membrane antigen; PET; positron emission tomography; prostate cancer; DUPA; Ga-68; Y-90; Lu-177; radionuclide therapy
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Funding
- University of Milano-Bicocca (Milan, Italy)
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Since prostate-specific membrane antigen (PSMA) has been identified as a diagnostic target for prostate cancer, many urea-based small PSMA-targeting molecules were developed. First, the clinical application of these Ga-68 labelled compounds in positron emission tomography (PET) showed their diagnostic potential. Besides, the therapy of prostate cancer is a demanding field, and the use of radiometals with PSMA bearing ligands is a valid approach. In this work, we describe the synthesis of a new PSMA ligand, CHX-A-DTPA-DUPA-Pep, the subsequent labelling with Ga-68, Lu-177 and Y-90 and the first in vitro characterization. In cell investigations with PSMA-positive LNCaP C4-2 cells, K-D values of <= 14.67 +/- 1.95 nM were determined, indicating high biological activities towards PSMA. Radiosyntheses with Ga-68, Lu-177 and Y-90 were developed under mild reaction conditions (room temperature, moderate pH of 5.5 and 7.4, respectively) and resulted in nearly quantitative radiochemical yields within 5 min.
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