| Autor: |
Frederik J R, Rombouts, Lieven, Declercq, José-Ignacio, Andrés, Astrid, Bottelbergs, Lu, Chen, Laura, Iturrino, Joseph E, Leenaerts, Jonas, Mariën, Fengbin, Song, Cindy, Wintmolders, Stijn, Wuyts, Chunfang A, Xia, Paula, Te Riele, Guy, Bormans, Rik, Vandenberghe, Hartmuth, Kolb, Diederik, Moechars |
| Rok vydání: |
2019 |
| Předmět: |
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| Zdroj: |
Journal of medicinal chemistry. 62(6) |
| ISSN: |
1520-4804 |
| Popis: |
In Alzheimer's disease, the density and spread of aggregated tau protein track well with neurodegeneration and cognitive decline, making the imaging of aggregated tau a compelling biomarker. A structure-activity relationship exploration around an isoquinoline hit, followed by an exploration of tolerated fluorination positions, allowed us to identify 9 (JNJ-64326067), a potent and selective binder to aggregated tau with a favorable pharmacokinetic profile and no apparent off-target binding. This was confirmed in rat and monkey positron emission tomography studies using [ |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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