Laboratory of Bioimaging Probe Development, Singapore Bioimaging Consortium, Agency for Science, Technology and Research, Singapore, 138667, Republic of Singapore.
Department of Chemistry, Seoul National University, Seoul, 08826, Republic of Korea.
Nat Commun. 2019 Mar 7;10(1):1111. doi: 10.1038/s41467-019-08990-9.
Activated macrophages have the potential to be ideal targets for imaging inflammation. However, probe selectivity over non-activated macrophages and probe delivery to target tissue have been challenging. Here, we report a small molecule probe specific for activated macrophages, called CDg16, and demonstrate its application to visualizing inflammatory atherosclerotic plaques in vivo. Through a systematic transporter screen using a CRISPR activation library, we identify the orphan transporter Slc18b1/SLC18B1 as the gating target of CDg16.
活化的巨噬细胞有可能成为炎症成像的理想靶点。然而，如何使探针具有针对未活化巨噬细胞的选择性，以及如何将探针递送至靶组织，一直是颇具挑战性的问题。在这里，我们报告了一种针对活化的巨噬细胞的小分子探针，称为 CDg16，并展示了其在体内可视化炎症性动脉粥样硬化斑块中的应用。通过使用 CRISPR 激活文库进行系统的转运体筛选，我们确定了孤儿转运体 Slc18b1/SLC18B1 是 CDg16 的门控靶点。
