2. Academic Validation
  3. Visualizing Microglia with a Fluorescence Turn-On Ugt1a7c Substrate

Visualizing Microglia with a Fluorescence Turn-On Ugt1a7c Substrate

  • Angew Chem Int Ed Engl. 2019 Jun 11;58(24):7972-7976. doi: 10.1002/anie.201903058.
Beomsue Kim 1,  Masahiro Fukuda 2,  Jung-Yeol Lee 3 1 4,  Dongdong Su 1,  Srikanta Sanu 1,  Aymeric Silvin 5,  Audrey T T Khoo 2,  Taejoon Kwon 6,  Xiao Liu 3 7,  Weijie Chi 8,  Xiaogang Liu 8,  Sejong Choi 9,  Diana S Y Wan 1,  Sung-Jin Park 1,  Jin-Soo Kim 10,  Florent Ginhoux 5,  H Shawn Je 2,  Young-Tae Chang 3 1 7
Affiliations

Affiliations

  • 1 Singapore Bioimaging Consortium, Agency for Science Technology and Research (A*STAR), Singapore, 138667, Singapore.
  • 2 Program in Neuroscience and Behavioral Disorders, Duke-NUS Medical School, Singapore, 169857, Singapore.
  • 3 Department of Chemistry, Pohang University of Science and Technology, Pohang, 37673, Korea.
  • 4 Present address: New drug discovery center, DGMIF, Daegu, 41061, Korea.
  • 5 Singapore Immunology Network, A*STAR, Singapore, 138648, Singapore.
  • 6 Department of Biomedical Engineering, Ulsan National Institute of Science and Technology, Ulsan, 44919, Korea.
  • 7 Center for Self-assembly and Complexity, Institute for Basic Science (IBS), Pohang, 37673, Korea.
  • 8 Singapore University of Technology and Design, Singapore, 487372, Singapore.
  • 9 Department of Chemistry, Seoul National University, Seoul, 08826, Korea.
  • 10 Center for Genome Engineering, IBS, Daejeon, 34047, Korea.
PMID: 31038839 DOI: 10.1002/anie.201903058
Abstract

Microglia, the brain-resident macrophage, are involved in brain development and contribute to the progression of neural disorders. Despite the importance of microglia, imaging of live microglia at a cellular resolution has been limited to transgenic mice. Efforts have therefore been dedicated to developing new methods for microglia detection and imaging. Using a thorough structure-activity relationships study, we developed CDr20, a high-performance fluorogenic chemical probe that enables the visualization of microglia both in vitro and in vivo. Using a genome-scale CRISPR-Cas9 knockout screen, the UDP-glucuronosyltransferase Ugt1a7c was identified as the target of CDr20. The glucuronidation of CDr20 by Ugt1a7c in microglia produces fluorescence.

Keywords

biological activity; fluorescent probes; imaging agents; microglia; structure-activity relationships.

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