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Cell- and Tissue-Based Proteome Profiling and Bioimaging with Probes Derived from a Potent AXL Kinase Inhibitor

Binbin Zheng1, Haijun Guo1, Nan Ma1

  • 1School of Pharmacy, Jinan University, Guangzhou City Key Laboratory of Precision Chemical Drug Development, International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of People's Republic of China, 601 Huangpu Avenue West, Guangzhou, 510632, China.

Chemistry, an Asian Journal
|June 26, 2018
PubMed

Insights

Researchers identified new targets for the cancer drug AXL, including BCAP31 and LPCAT3. They also developed imaging probes to detect AXL binding in cells and tissues, aiding cancer research.

Area of Science:

  • Oncology
  • Biochemistry
  • Chemical Biology

Background:

  • AXL receptor tyrosine kinase is a novel target for cancer therapeutics.
  • Limited availability of potent and selective AXL inhibitors hinders therapeutic development.
  • Our group previously developed a lead compound, 9im, with potent and specific AXL inhibition.

Purpose of the Study:

  • To identify novel cellular targets of the AXL inhibitor 9im.
  • To develop imaging probes for visualizing 9im-target interactions in live systems.
  • To validate 9im as a tool for detecting AXL in biological contexts.

Main Methods:

  • Competitive affinity-based proteome profiling was employed to discover 9im's cellular targets.
  • Development of trans-cyclooctene (TCO) and acedan-containing probes for imaging.
  • In situ imaging of 9im-protein binding in live cells and tumor tissues.

Main Results:

  • Identification of several previously unknown cellular targets for 9im, including BCAP31, LPCAT3, POR, TM9SF3, SCCPDH, and CANX.
  • Successful development of TCO and acedan probes for visualizing target engagement.
  • Demonstration of probe utility in imaging 9im binding within cellular and tissue environments.

Conclusions:

  • The AXL inhibitor 9im engages multiple novel cellular targets beyond AXL.
  • Developed imaging probes are effective tools for studying drug-target interactions in complex biological systems.
  • These findings provide a foundation for advancing AXL-targeted cancer therapies and diagnostic tools.
Keywords:
AXLimagingprobesproteomicstarget identification

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