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

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

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].
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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