| Literature DB >> 32852205 |
Jens Cardinale1, Mareike Roscher1, Martin Schäfer1, Max Geerlings1, Martina Benešová1, Ulrike Bauder-Wüst1, Yvonne Remde1, Matthias Eder1, Zora Nováková2, Lucia Motlová2, Cyril Barinka2, Frederik L Giesel3, Klaus Kopka4.
Abstract
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-rays with mixed results. Among 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.Entities:
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Year: 2020 PMID： 32852205 DOI： 10.1021/acs.jmedchem.9b01479
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446