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

Sung-Jin Park1, Beomsue Kim1, Sejong Choi2

  • 1Laboratory of Bioimaging Probe Development, Singapore Bioimaging Consortium, Agency for Science, Technology and Research, Singapore, 138667, Republic of Singapore.

Nature Communications
|March 9, 2019
PubMed

Insights

Researchers developed a new small molecule probe, CDg16, that specifically targets activated macrophages for imaging inflammation. This probe visualizes atherosclerotic plaques in vivo by identifying the SLC18B1 transporter.

Area of Science:

  • Molecular biology
  • Immunology
  • Medical imaging

Background:

  • Activated macrophages are key targets for inflammation imaging.
  • Challenges include probe selectivity and delivery to target tissues.

Purpose of the Study:

  • To develop a novel small molecule probe for activated macrophage imaging.
  • To demonstrate its utility in visualizing inflammatory atherosclerotic plaques.

Main Methods:

  • Systematic transporter screen using a CRISPR activation library.
  • Development and in vivo application of the CDg16 probe.
  • Identification of the SLC18B1 transporter as the CDg16 target.

Main Results:

  • A small molecule probe, CDg16, was identified with specificity for activated macrophages.
  • CDg16 successfully visualized inflammatory atherosclerotic plaques in vivo.
  • The orphan transporter Slc18b1/SLC18B1 was identified as the gating target of CDg16.

Conclusions:

  • CDg16 is a selective probe for activated macrophages, overcoming previous challenges.
  • This probe enables in vivo imaging of inflammatory conditions like atherosclerosis.
  • Understanding the SLC18B1 transporter is crucial for CDg16's mechanism of action.

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