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 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.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Bernard-Gauthier V,Mossine AV,Mahringer A,Aliaga A,Bailey JJ,Shao X,Stauff J,Arteaga J,Sherman P,Grand'Maison M,Rochon PL,Wängler B,Wängler C,Bartenstein P,Kostikov A,Kaplan DR,Fricker G,Rosa-Neto P,Scott PJH,Schirrdoi
10.1021/acs.jmedchem.7b01607subject
Has Abstractpub_date
2018-02-22 00:00:00pages
1737-1743issue
4eissn
0022-2623issn
1520-4804journal_volume
61pub_type
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