Cover Image

Identification of [18F]TRACK, a fluorine-18-labeled tropomyosin receptor kinase (Trk) inhibitor for PET imaging

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...

Full description

Saved in:
Bibliographic Details
Main Authors: Bernard-Gauthier, Vadim (Author) , Mahringer, Anne (Author) , Wängler, Björn (Author) , Wängler, Carmen (Author) , Fricker, Gert (Author)
Format: Article (Journal)
Language:English
Published: 2018
In: Journal of medicinal chemistry
Year: 2017, Volume: 61, Issue: 4, Pages: 1737-1743
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.7b01607
Online Access:Verlag, Volltext: https://doi.org/10.1021/acs.jmedchem.7b01607
Get full text
Author Notes:Vadim Bernard-Gauthier, Andrew V. Mossine, Anne Mahringer, Arturo Aliaga, Justin J. Bailey, Xia Shao, Jenelle Stauff, Janna Arteaga, Phillip Sherman, Marilyn Grand’Maison, Pierre-Luc Rochon, Björn Wängler, Carmen Wängler, Peter Bartenstein, Alexey Kostikov, David R. Kaplan, Gert Fricker, Pedro Rosa-Neto, Peter J. H. Scott, and Ralf Schirrmacher
Description
Summary: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.
Item Description:Gesehen am 24.07.2019
Published: December 19, 2017
Im Titel ist die 18 in [18F]TRACK hochgestellt
Physical Description:Online Resource
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.7b01607

Similar Items