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Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3).
Dekkers, Sebastian; Comez, Dehan; Karsai, Noemi; Arimont-Segura, Marta; Canals, Meritxell; Caspar, Birgit; de Graaf, Chris; Kilpatrick, Laura E; Leurs, Rob; Kellam, Barrie; Hill, Stephen J; Briddon, Stephen J; Stocks, Michael J.
  • Dekkers S; Biodiscovery Institute, School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, United Kingdom.
  • Comez D; Centre of Membrane Proteins and Receptors, University of Birmingham and University of Nottingham, The Midlands NG7 2UH, United Kingdom.
  • Karsai N; Division of Physiology, Pharmacology & Neuroscience, Medical School, University of Nottingham, Nottingham NG7 2UH, U.K.
  • Arimont-Segura M; Centre of Membrane Proteins and Receptors, University of Birmingham and University of Nottingham, The Midlands NG7 2UH, United Kingdom.
  • Canals M; Division of Physiology, Pharmacology & Neuroscience, Medical School, University of Nottingham, Nottingham NG7 2UH, U.K.
  • Caspar B; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, Amsterdam 1081 HZ, The Netherlands.
  • de Graaf C; Centre of Membrane Proteins and Receptors, University of Birmingham and University of Nottingham, The Midlands NG7 2UH, United Kingdom.
  • Kilpatrick LE; Division of Physiology, Pharmacology & Neuroscience, Medical School, University of Nottingham, Nottingham NG7 2UH, U.K.
  • Leurs R; Centre of Membrane Proteins and Receptors, University of Birmingham and University of Nottingham, The Midlands NG7 2UH, United Kingdom.
  • Kellam B; Division of Physiology, Pharmacology & Neuroscience, Medical School, University of Nottingham, Nottingham NG7 2UH, U.K.
  • Hill SJ; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, Amsterdam 1081 HZ, The Netherlands.
  • Briddon SJ; Biodiscovery Institute, School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, United Kingdom.
  • Stocks MJ; Centre of Membrane Proteins and Receptors, University of Birmingham and University of Nottingham, The Midlands NG7 2UH, United Kingdom.
ACS Med Chem Lett ; 15(1): 143-148, 2024 Jan 11.
Article en En | MEDLINE | ID: mdl-38229752
ABSTRACT
The atypical chemokine receptor 3 (ACKR3) is a receptor that induces cancer progression and metastasis in multiple cell types. Therefore, new chemical tools are required to study the role of ACKR3 in cancer and other diseases. In this study, fluorescent probes, based on a series of small molecule ACKR3 agonists, were synthesized. Three fluorescent probes, which showed specific binding to ACKR3 through a luminescence-based NanoBRET binding assay (pKd ranging from 6.8 to 7.8) are disclosed. Due to their high affinity at the ACKR3, we have shown their application in both competition binding experiments and confocal microscopy studies showing the cellular distribution of this receptor.
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Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2024 Tipo del documento: Article
Texto completo
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PubMed Links
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Texto completo: 1 Banco de datos: MEDLINE Idioma: En Año: 2024 Tipo del documento: Article