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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; Waengler, Carmen; Bartenstein, Peter; Kostikov, Alexey; Kaplan, David R.; Fricker, Gert; Rosa-Neto, Pedro; Scott, Peter J. H.; Schirrmacher, Ralf (2018): Identification of [F-18]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging. In: Journal of Medicinal Chemistry, Vol. 61, No. 4: pp. 1737-1743
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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 F-18-labeled optimized lead suitable for in vivo imaging of Trk, [F-18]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.