Imaging inflammation using an activated macrophage probe with Slc18b1 as the activation-selective gating target.

Park, Sung-Jin; Kim, Beomsue; Choi, Sejong; Balasubramaniam, Sivaraman; Lee, Sung-Chan; Lee, Jung Yeol; Kim, Heon Seok; Kim, Jun-Young et al. · Nat Commun · 2019

basic_science · Level V

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Abstract

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.

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