| Literature DB >> 29257860 |
Vadim Bernard-Gauthier1, Andrew V Mossine2, Anne Mahringer3, Arturo Aliaga4, Justin J Bailey1, Xia Shao2, Jenelle Stauff2, Janna Arteaga2, Phillip Sherman2, Marilyn Grand'Maison5, Pierre-Luc Rochon6, Björn Wängler, Carmen Wängler, Peter Bartenstein7, Alexey Kostikov6, David R Kaplan8, Gert Fricker3, Pedro Rosa-Neto4, Peter J H Scott2,9, Ralf Schirrmacher1.
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.Entities:
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Year: 2018 PMID： 29257860 DOI： 10.1021/acs.jmedchem.7b01607
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446