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| Verfasst von: | Cardinale, Jens [VerfasserIn]  |
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| | Roscher, Mareike [VerfasserIn] |
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| | Schäfer, Martin [VerfasserIn] |
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| | Geerlings, Max [VerfasserIn] |
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| | Benes̆ová, Martina [VerfasserIn] |
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| | Bauder-Wüst, Ulrike [VerfasserIn] |
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| | Remde, Yvonne [VerfasserIn] |
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| | Eder, Matthias [VerfasserIn] |
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| | Nováková, Zora [VerfasserIn] |
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| | Motlová, Lucia [VerfasserIn] |
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| | Barinka, Cyril [VerfasserIn] |
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| | Giesel, Frederik L. [VerfasserIn] |
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| | Kopka, Klaus [VerfasserIn] |
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| Titel: | Development of PSMA-1007-related series of 18F-labeled Glu-Ureido-type PSMA inhibitors |
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| Verf.angabe: | Jens Cardinale, Mareike Roscher, Martin Schäfer, Max Geerlings, Martina Benešová, Ulrike Bauder-Wüst, Yvonne Remde, Matthias Eder, Zora Nováková, Lucia Motlová, Cyril Barinka, Frederik L. Giesel, and Klaus Kopka |
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| E-Jahr: | 2020 |
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| Jahr: | August 27, 2020 |
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| Umfang: | 11 S. |
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| Teil: | volume:63 |
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| | year:2020 |
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| | number:19 |
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| | pages:10897-10907 |
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| | extent:11 |
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| Fussnoten: | Gesehen am 03.02.2021 |
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| Titel Quelle: | Enthalten in: Journal of medicinal chemistry |
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| Ort Quelle: | Washington, DC : ACS, 1959 |
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| Jahr Quelle: | 2020 |
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| Band/Heft Quelle: | 63(2020), 19, Seite 10897-10907 |
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| ISSN Quelle: | 1520-4804 |
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| 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. |
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| DOI: | doi:10.1021/acs.jmedchem.9b01479 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
Volltext: https://doi.org/10.1021/acs.jmedchem.9b01479 |
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| | DOI: https://doi.org/10.1021/acs.jmedchem.9b01479 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| K10plus-PPN: | 1747241202 |
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| Verknüpfungen: | → Zeitschrift |
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Development of PSMA-1007-related series of 18F-labeled Glu-Ureido-type PSMA inhibitors / Cardinale, Jens [VerfasserIn]; August 27, 2020 (Online-Ressource)
