| Autor: |
Cardinale, J., Roscher, M., Schaefer, M., Geerlings, M., Benešová, M., Bauder-Wüst, U., Remde, Y., Eder, M., Novakova, Z., Motlová, L., Bařinka, C., Giesel, F., Kopka, K. |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Předmět: |
|
| Zdroj: |
Journal of Medicinal Chemistry 63(2020)19, 10897-10907 |
| Popis: |
In recent years, a number of drugs targeting the prostate specific-membrane antigen (PSMA) have become important tools in the diagnosis and treatment of prostate cancer. In the present work, we report on the synthesis and preclinical evaluation of a series of 18F-labeled PSMA ligands for diagnostic application based on the theragnostic ligand PSMA-617. By applying modifications to the linker-structure, insight into the structure-activity relationship could be gained highlighting the importance of hydrophilicity and stereoselectivity on interaction with PSMA and hence the biodistribution. Selected compounds were co-crystallized with the PSMA-protein and analyzed by X-ray with mixed results. Amongst these, PSMA-1007 (compound 5) showed the best interaction with the PSMA protein. The respective radiotracer [18F]PSMA-1007 was translated into the clinic and is in the meantime subject of advanced clinical trials. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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