^99mTc-Labeled Small-Molecule Inhibitors of Prostate-Specific Membrane Antigen for Molecular Imaging of Prostate Cancer

Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Drugs to Renal Cell Carcinoma

“…The biodistribution profiles of acetazolamide derivatives compares favourably with the ones previously reported for other ligands [23][24][25][26]. In particular, we were pleased to see that %ID/g values in the tumor were higher than the corresponding values in the kidney (the main organ for drug clearance), even as early as one hour after intravenous administration of the product [18].…”

“…Aliquots (150 μl) were taken at different time points (0, 15', 1h, 6h, 24h, 48h) and frozen at -20°C. Standard solutions of the conjugates were prepared in PBS at different concentration (25,50, 100, 150 μg/ml) and stored at -20 °C. The standards and the samples were analyzed in triplicate by Liquid Chromatography -Mass Spectrometry (LC-MS) on a Waters Xevo G2-XS QTOF coupled to a Waters Acquity UPLC H-Class System using a ACQUITY UPLC BEH C18 Column, 130 Å, 1.7 µm, 2.1 mm × 50 mm column.…”

“…Aliquots of 150 μl were taken at different time points (0, 20', 1h, 3h, 6h, 24h) and frozen at -20°C. Standard solutions were prepared in mouse serum (Invitrogen) at different concentration (25,50, 100, 150 μg/ml) and stored at -20°C. All the samples and the standards were thawed and diluted with four volumes of MeOH.…”

“…Unlike antibodies (which can easily be raised against the majority of target proteins of interest), it is not always easy to generate high-affinity small molecule ligands to tumor-associated antigens. However, excellent tumor-targeting results have been reported for folate analogues targeting folate-receptor positive tumors [23,24], substituted urea derivatives targeting prostate-specific membrane antigen [25], somatostatin antagonists targeting the somatostatin receptor [26] and for carbonic anhydrase IX (CAIX) ligands [16][17][18]27].…”

New Radiopharmaceuticals Based on Prostate-Specific Inhibitors of Membrane Antigen for Diagnostics and Therapy of Metastatic Prostate Cancer

“…В дальнейшем были разработаны улучшенные вари-анты подобного РФП для радиоизотопной диагностики c 123 I и терапии с изотопами 131 I, 177 Lu и 90 Y [11,16]. Однако, несмотря на лучшие результаты доклинических и пилотных клинических исследований, по сравнению с 111 In-capromab, новые РФП не нашли клинического применения, т.к.…”