用于非典型趋化因子受体3（ACKR3）的小分子荧光配体
Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3).
作者信息
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
机构信息
Biodiscovery Institute, School of Pharmacy, University of Nottingham, Nottingham NG7 2RD, United Kingdom.
Centre of Membrane Proteins and Receptors, University of Birmingham and University of Nottingham, The Midlands NG7 2UH, United Kingdom.
出版信息
ACS Med Chem Lett. 2023 Dec 8;15(1):143-148. doi: 10.1021/acsmedchemlett.3c00469. eCollection 2024 Jan 11.
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.
非典型趋化因子受体3（ACKR3）是一种能在多种细胞类型中诱导癌症进展和转移的受体。因此，需要新的化学工具来研究ACKR3在癌症和其他疾病中的作用。在本研究中，基于一系列小分子ACKR3激动剂合成了荧光探针。公开了三种通过基于发光的纳米生物发光共振能量转移结合试验（p值范围为6.8至7.8）显示与ACKR3特异性结合的荧光探针。由于它们对ACKR3具有高亲和力，我们已展示了它们在竞争结合实验和共聚焦显微镜研究中的应用，这些研究显示了该受体的细胞分布。
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