Field Devon H, White Jack S, Warriner Stuart L, Wright Megan H
Astbury Centre for Structural Molecular Biology, and the School of Chemistry, University of Leeds, Woodhouse Lane Leeds LS2 9JT UK
RSC Chem Biol. 2023 Jan 13;4(3):216-222. doi: 10.1039/d2cb00199c. eCollection 2023 Mar 8.
Fluorescent ligands for G-protein coupled receptors (GPCRs) are valuable tools for studying the expression, pharmacology and modulation of these therapeutically important proteins in living cells. Here we report a fluorescent photoaffinity probe for Formyl peptide receptor 1 (FPR1), a critical component of the innate immune response to bacterial infection and a promising target in inflammatory diseases. We demonstrate that the probe binds and covalently crosslinks to FPR1 with good specificity at nanomolar concentrations in living cells and is a useful tool for visualisation and characterisation of this receptor.
用于G蛋白偶联受体(GPCRs)的荧光配体是研究这些在活细胞中具有重要治疗意义的蛋白质的表达、药理学和调节作用的宝贵工具。在此,我们报告了一种针对甲酰肽受体1(FPR1)的荧光光亲和探针,FPR1是对细菌感染的先天免疫反应的关键组成部分,也是炎症性疾病中一个有前景的靶点。我们证明,该探针在活细胞中以纳摩尔浓度与FPR1特异性结合并共价交联,是可视化和表征该受体的有用工具。