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 |
| Volume | 61 |
| Issue | 4 |
| Pagination | 1737-1743 |
| Date Published | 2018 Feb 22 |
| ISSN | 1520-4804 |
| Abstract | 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. |
| DOI | 10.1021/acs.jmedchem.7b01607 |
| Alternate Journal | J. Med. Chem. |
| PubMed ID | 29257860 |