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 radiosynthesize...
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| Veröffentlicht in: | Journal of medicinal chemistry 2018-02, Vol.61 (4), p.1737-1743 |
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| container_title | Journal of medicinal chemistry |
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| creator | Bernard-Gauthier, Vadim Mossine, Andrew V Mahringer, Anne Aliaga, Arturo Bailey, Justin J Shao, Xia Stauff, Jenelle Arteaga, Janna Sherman, Phillip Grand’Maison, Marilyn Rochon, Pierre-Luc Wängler, Björn Wängler, Carmen Bartenstein, Peter Kostikov, Alexey Kaplan, David R Fricker, Gert Rosa-Neto, Pedro Scott, Peter J. H Schirrmacher, Ralf |
| description | 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. |
| doi_str_mv | 10.1021/acs.jmedchem.7b01607 |
| format | Article |
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| language | eng |
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| source | ACS Publications; MEDLINE |
| subjects | Drug Design Fluorine Radioisotopes Humans Neoplasms - diagnostic imaging Neurodegenerative Diseases - diagnostic imaging Pharmacology & Pharmacy Positron-Emission Tomography - methods Protein Kinase Inhibitors Receptor, trkA - antagonists & inhibitors |
| title | Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging |
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