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Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging.
Bernard-Gauthier, Vadim; Mossine, Andrew V; Mahringer, Anne; Aliaga, Arturo; Bailey, Justin J; Shao, Xia; Stauff, Jenelle; Arteaga, Janna; Sherman, Phillip; Grand'Maison, Marilyn; Rochon, Pierre-Luc; Wängler, Björn; Wängler, Carmen; Bartenstein, Peter; Kostikov, Alexey; Kaplan, David R; Fricker, Gert; Rosa-Neto, Pedro; Scott, Peter J H; Schirrmacher, Ralf.
Afiliación
  • Bernard-Gauthier V; Department of Oncology, Division of Oncological Imaging, University of Alberta , Edmonton, AB T6G 2R3, Canada.
  • Mossine AV; Department of Radiology, Division of Nuclear Medicine, The University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Mahringer A; Institute of Pharmacy and Molecular Biotechnology, University of Heidelberg , Heidelberg 69120, Germany.
  • Aliaga A; Translational Neuroimaging Laboratory, McGill Centre for Studies in Aging, Douglas Mental Health University Institute , Montreal, QC H4H 1R3, Canada.
  • Bailey JJ; Department of Oncology, Division of Oncological Imaging, University of Alberta , Edmonton, AB T6G 2R3, Canada.
  • Shao X; Department of Radiology, Division of Nuclear Medicine, The University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Stauff J; Department of Radiology, Division of Nuclear Medicine, The University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Arteaga J; Department of Radiology, Division of Nuclear Medicine, The University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Sherman P; Department of Radiology, Division of Nuclear Medicine, The University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Grand'Maison M; Biospective Inc. , Montreal, QC H4P 2R2, Canada.
  • Rochon PL; McConnell Brain Imaging Centre, Montreal Neurological Institute, McGill University , Montreal, QC H3A 2B4, Canada.
  • Bartenstein P; Department of Nuclear Medicine, Ludwig-Maximilians-University of Munich , Munich 81377, Germany.
  • Kostikov A; McConnell Brain Imaging Centre, Montreal Neurological Institute, McGill University , Montreal, QC H3A 2B4, Canada.
  • Kaplan DR; Program in Neurosciences and Mental Health, Hospital for Sick Children , Toronto, ON M5G 0A4, Canada.
  • Fricker G; Institute of Pharmacy and Molecular Biotechnology, University of Heidelberg , Heidelberg 69120, Germany.
  • Rosa-Neto P; Translational Neuroimaging Laboratory, McGill Centre for Studies in Aging, Douglas Mental Health University Institute , Montreal, QC H4H 1R3, Canada.
  • Scott PJH; Department of Radiology, Division of Nuclear Medicine, The University of Michigan Medical School , Ann Arbor, Michigan 48109, United States.
  • Schirrmacher R; The Interdepartmental Program in Medicinal Chemistry, University of Michigan , Ann Arbor, Michigan 48109, United States.
J Med Chem ; 61(4): 1737-1743, 2018 02 22.
Article en En | MEDLINE | ID: mdl-29257860
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Radioisótopos de Flúor / Receptor trkA / Tomografía de Emisión de Positrones Tipo de estudio: Diagnostic_studies Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Canadá
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Radioisótopos de Flúor / Receptor trkA / Tomografía de Emisión de Positrones Tipo de estudio: Diagnostic_studies Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2018 Tipo del documento: Article País de afiliación: Canadá