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

  • Nat Commun. 2019 Mar 7;10(1):1111. doi: 10.1038/s41467-019-08990-9.
Sung-Jin Park  1 ,  Beomsue Kim  1 ,  Sejong Choi  2 ,  Sivaraman Balasubramaniam  1 ,  Sung-Chan Lee  1 ,  Jung Yeol Lee  3 ,  Heon Seok Kim  2 ,  Jun-Young Kim  1 ,  Jong-Jin Kim  1  4 ,  Yong-An Lee  1 ,  Nam-Young Kang  1  5 ,  Jin-Soo Kim  6  7 ,  Young-Tae Chang  8  9  10
Affiliations
  • 1. Laboratory of Bioimaging Probe Development, Singapore Bioimaging Consortium, Agency for Science, Technology and Research, Singapore, 138667, Republic of Singapore.
  • 2. Department of Chemistry, Seoul National University, Seoul, 08826, Republic of Korea.
  • 3. Department of Chemistry, Pohang University of Science and Technology (POSTECH), Pohang, 37673, Republic of Korea.
  • 4. Center for Self-assembly and Complexity, Institute for Basic Science (IBS), Pohang, 37673, Republic of Korea.
  • 5. New Drug Discovery Center, Daegu-Gyeongbuk Medical Innovation Foundation (DGMIF), Daegu, 41061, Republic of Korea.
  • 6. Department of Chemistry, Seoul National University, Seoul, 08826, Republic of Korea. [email protected].
  • 7. Center for Genome Engineering, Institute for Basic Science (IBS), Daejeon, 34126, Republic of Korea. [email protected].
  • 8. Laboratory of Bioimaging Probe Development, Singapore Bioimaging Consortium, Agency for Science, Technology and Research, Singapore, 138667, Republic of Singapore. [email protected].
  • 9. Department of Chemistry, Pohang University of Science and Technology (POSTECH), Pohang, 37673, Republic of Korea. [email protected].
  • 10. Center for Self-assembly and Complexity, Institute for Basic Science (IBS), Pohang, 37673, Republic of Korea. [email protected].
PMID: 30846702 DOI: 10.1038/s41467-019-08990-9
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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