Identification of [18F]TRACK, a fluorine-18-labeled tropomyosin receptor kinase (Trk) inhibitor for PET imaging
Changes in expression and dysfunctional signaling of TrkA/B/C receptors and oncogenic Trk fusion proteins are found in neurological diseases and cancers. Here, we describe the development of a first 18F-labeled optimized lead suitable for in vivo imaging of Trk, [18F]TRACK, which is radiosynthesized...
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| Main Authors: | , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
2018
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| In: |
Journal of medicinal chemistry
Year: 2017, Volume: 61, Issue: 4, Pages: 1737-1743 |
| ISSN: | 1520-4804 |
| DOI: | 10.1021/acs.jmedchem.7b01607 |
| Online Access: | Verlag, Volltext: https://doi.org/10.1021/acs.jmedchem.7b01607
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| Author Notes: | Vadim Bernard-Gauthier, Andrew V. Mossine, Anne Mahringer, Arturo Aliaga, Justin J. Bailey, Xia Shao, Jenelle Stauff, Janna Arteaga, Phillip Sherman, Marilyn Grand’Maison, Pierre-Luc Rochon, Björn Wängler, Carmen Wängler, Peter Bartenstein, Alexey Kostikov, David R. Kaplan, Gert Fricker, Pedro Rosa-Neto, Peter J. H. Scott, and Ralf Schirrmacher |
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| 520 | |a Changes in expression and dysfunctional signaling of TrkA/B/C receptors and oncogenic Trk fusion proteins are found in neurological diseases and cancers. Here, we describe the development of a first 18F-labeled optimized lead suitable for in vivo imaging of Trk, [18F]TRACK, which is radiosynthesized with ease from a nonactivated aryl precursor concurrently combining largely reduced P-gp liability and improved brain kinetics compared to previous leads while displaying high on-target affinity and human kinome selectivity. | ||
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