Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors

Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as (18)F‐labeled PET tracers. The derivatives were evaluated extensively for their off‐target profile at 48 different targets. The most potent and selective candidate was applied in vivo in a biodistribution s...

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Autores principales: Wagner, Stefan, de Moura Gatti, Fernando, Silva, Daniel G., Ortiz Zacarias, Natalia V., Zweemer, Annelien J. M., Hermann, Sven, De Maria, Monica, Koch, Michael, Weiss, Christina, Schepmann, Dirk, Heitman, Laura H., Tschammer, Nuska, Kopka, Klaus, Junker, Anna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Full Papers
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7983900/
https://www.ncbi.nlm.nih.gov/pubmed/33205603
http://dx.doi.org/10.1002/cmdc.202000728
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author Wagner, Stefan
de Moura Gatti, Fernando
Silva, Daniel G.
Ortiz Zacarias, Natalia V.
Zweemer, Annelien J. M.
Hermann, Sven
De Maria, Monica
Koch, Michael
Weiss, Christina
Schepmann, Dirk
Heitman, Laura H.
Tschammer, Nuska
Kopka, Klaus
Junker, Anna
author_facet Wagner, Stefan
de Moura Gatti, Fernando
Silva, Daniel G.
Ortiz Zacarias, Natalia V.
Zweemer, Annelien J. M.
Hermann, Sven
De Maria, Monica
Koch, Michael
Weiss, Christina
Schepmann, Dirk
Heitman, Laura H.
Tschammer, Nuska
Kopka, Klaus
Junker, Anna
author_sort Wagner, Stefan
collection PubMed
description Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as (18)F‐labeled PET tracers. The derivatives were evaluated extensively for their off‐target profile at 48 different targets. The most potent and selective candidate was applied in vivo in a biodistribution study, demonstrating a promising profile for further preclinical development. This compound represents the first potential nonpeptidic PET tracer for the imaging of CCR2 receptors.
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spelling pubmed-79839002021-03-24 Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors Wagner, Stefan de Moura Gatti, Fernando Silva, Daniel G. Ortiz Zacarias, Natalia V. Zweemer, Annelien J. M. Hermann, Sven De Maria, Monica Koch, Michael Weiss, Christina Schepmann, Dirk Heitman, Laura H. Tschammer, Nuska Kopka, Klaus Junker, Anna ChemMedChem Full Papers Herein we report the design and synthesis of a series of highly selective CCR2 antagonists as (18)F‐labeled PET tracers. The derivatives were evaluated extensively for their off‐target profile at 48 different targets. The most potent and selective candidate was applied in vivo in a biodistribution study, demonstrating a promising profile for further preclinical development. This compound represents the first potential nonpeptidic PET tracer for the imaging of CCR2 receptors. John Wiley and Sons Inc. 2020-11-23 2021-02-17 /pmc/articles/PMC7983900/ /pubmed/33205603 http://dx.doi.org/10.1002/cmdc.202000728 Text en © 2020 The Authors. ChemMedChem published by Wiley-VCH GmbH This is an open access article under the terms of the http://creativecommons.org/licenses/by-nc-nd/4.0/ License, which permits use and distribution in any medium, provided the original work is properly cited, the use is non‐commercial and no modifications or adaptations are made.
spellingShingle Full Papers
Wagner, Stefan
de Moura Gatti, Fernando
Silva, Daniel G.
Ortiz Zacarias, Natalia V.
Zweemer, Annelien J. M.
Hermann, Sven
De Maria, Monica
Koch, Michael
Weiss, Christina
Schepmann, Dirk
Heitman, Laura H.
Tschammer, Nuska
Kopka, Klaus
Junker, Anna
Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors
title Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors
title_full Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors
title_fullStr Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors
title_full_unstemmed Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors
title_short Development of the First Potential Nonpeptidic Positron Emission Tomography Tracer for the Imaging of CCR2 Receptors
title_sort development of the first potential nonpeptidic positron emission tomography tracer for the imaging of ccr2 receptors
topic Full Papers
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7983900/
https://www.ncbi.nlm.nih.gov/pubmed/33205603
http://dx.doi.org/10.1002/cmdc.202000728
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