Identification of [F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging.
|Title||Identification of [F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging.|
|Publication Type||Journal Article|
|Year of Publication||2018|
|Authors||Bernard-Gauthier V, Mossine AV, Mahringer A, Aliaga A, Bailey JJ, Shao X, Stauff J, Arteaga J, Sherman P, Grand'Maison M, Rochon P-L, Wängler B, Wängler C, Bartenstein P, Kostikov A, Kaplan DR, Fricker G, Rosa-Neto P, Scott PJH, Schirrmacher R|
|Journal||J Med Chem|
|Date Published||2018 Feb 22|
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-labeled optimized lead suitable for in vivo imaging of Trk, [F]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.
|Alternate Journal||J. Med. Chem.|