Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3)

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2024 Jan 17

PMID 38229752

Authors

Sebastian Dekkers

Dehan Comez

Noemi Karsai

Marta Arimont-Segura

Meritxell Canals

Birgit Caspar

Chris de Graaf

Laura E Kilpatrick

Rob Leurs

Barrie Kellam

Stephen J Hill

Stephen J Briddon

Michael J Stocks

Affiliations

Soon will be listed here.

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 (p 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.

Citing Articles

Multiplex Detection of Fluorescent Chemokine Binding to CXC Chemokine Receptors by NanoBRET.

Adamska J, Leftheriotis S, Bosma R, Vischer H, Leurs R Int J Mol Sci. 2024; 25(9).

PMID: 38732237 PMC: 11084278. DOI: 10.3390/ijms25095018.

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