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Imaging inflammation using an activated macrophage probe with Slc18b1 as the activation-selective gating target
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Imaging inflammation using an activated macrophage probe with Slc18b1 as the activation-selective gating target
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Journal Article
Imaging inflammation using an activated macrophage probe with Slc18b1 as the activation-selective gating target
2019
Overview
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.
Attempts to image activated macrophages in vivo have been hampered by selectivity and delivery problems. Here the authors develop a small molecule fluorescent probe specific to activated M1 and M2 macrophages, identify the orphan receptor Slc18b1/SLC18B1 as the mechanism of uptake, and use it to image atherosclerosis in mice.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
Subject
/ 14/34
/ 49/47
/ 49/98
/ Animals
/ Cation Transport Proteins - metabolism
/ CRISPR
/ Humanities and Social Sciences
/ Humans
/ Inflammation - diagnostic imaging
/ Mice
/ Plaque, Atherosclerotic - diagnostic imaging
/ Plaque, Atherosclerotic - immunology
/ Plaque, Atherosclerotic - metabolism
/ Plaques
/ Science
