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Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays.
Ertl, Fabian J; Kopanchuk, Sergei; Dijon, Nicola C; Veiksina, Santa; Tahk, Maris-Johanna; Laasfeld, Tõnis; Schettler, Franziska; Gattor, Albert O; Hübner, Harald; Archipowa, Nataliya; Köckenberger, Johannes; Heinrich, Markus R; Gmeiner, Peter; Kutta, Roger J; Holliday, Nicholas D; Rinken, Ago; Keller, Max.
Afiliación
  • Ertl FJ; Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany.
  • Kopanchuk S; Institute of Chemistry, University of Tartu, Ravila 14a, 50411 Tartu, Estonia.
  • Dijon NC; School of Life Sciences, University of Nottingham, Queen's Medical Centre, Nottingham NG7 2UH, U.K.
  • Veiksina S; Institute of Chemistry, University of Tartu, Ravila 14a, 50411 Tartu, Estonia.
  • Tahk MJ; Institute of Chemistry, University of Tartu, Ravila 14a, 50411 Tartu, Estonia.
  • Laasfeld T; Institute of Chemistry, University of Tartu, Ravila 14a, 50411 Tartu, Estonia.
  • Schettler F; Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany.
  • Gattor AO; Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany.
  • Hübner H; Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich Alexander University, Nikolaus-Fiebiger-Straße 10, D-91058 Erlangen, Germany.
  • Archipowa N; Institute of Biophysics and Physical Biochemistry, Faculty of Biology and Preclinical Medicine, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany.
  • Köckenberger J; Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich Alexander University, Nikolaus-Fiebiger-Straße 10, D-91058 Erlangen, Germany.
  • Heinrich MR; Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich Alexander University, Nikolaus-Fiebiger-Straße 10, D-91058 Erlangen, Germany.
  • Gmeiner P; Department of Chemistry and Pharmacy, Medicinal Chemistry, Friedrich Alexander University, Nikolaus-Fiebiger-Straße 10, D-91058 Erlangen, Germany.
  • Kutta RJ; Institute of Physical and Theoretical Chemistry, Faculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany.
  • Holliday ND; School of Life Sciences, University of Nottingham, Queen's Medical Centre, Nottingham NG7 2UH, U.K.
  • Rinken A; Institute of Chemistry, University of Tartu, Ravila 14a, 50411 Tartu, Estonia.
  • Keller M; Institute of Pharmacy, Faculty of Chemistry and Pharmacy, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany.
J Med Chem ; 67(18): 16664-16691, 2024 Sep 26.
Article en En | MEDLINE | ID: mdl-39261089
ABSTRACT
The determination of ligand-receptor binding affinities plays a key role in the development process of pharmaceuticals. While the classical radiochemical binding assay uses radioligands, fluorescence-based binding assays require fluorescent probes. Usually, radio- and fluorescence-labeled ligands are dissimilar in terms of structure and bioactivity, and can be used in either radiochemical or fluorescence-based assays. Aiming for a close comparison of both assay types, we synthesized tritiated fluorescent neurotensin receptor ligands ([3H]13, [3H]18) and their nontritiated analogues (13, 18). The labeled probes were studied in radiochemical and fluorescence-based (high-content imaging, flow cytometry, fluorescence anisotropy) binding assays. Equilibrium saturation binding yielded well-comparable ligand-receptor affinities, indicating that all these setups can be used for the screening of new drugs. In contrast, discrepancies were found in the kinetic behavior of the probes, which can be attributed to technical differences of the methods and require further studies with respect to the elucidation of the underlying mechanisms.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Neurotensina / Colorantes Fluorescentes Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Estados Unidos
Texto completo
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XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptores de Neurotensina / Colorantes Fluorescentes Límite: Animals / Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2024 Tipo del documento: Article País de afiliación: Alemania Pais de publicación: Estados Unidos