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Applications of the Single-probe: Mass Spectrometry Imaging and Single Cell Analysis under Ambient Conditions
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Applications of the Single-probe: Mass Spectrometry Imaging and Single Cell Analysis under Ambient Conditions

Published on: June 14, 2016

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Crenolanib-Derived Probes Suitable for Cell- and Tissue-Based Protein Profiling and Single-Cell Imaging

Yu Chang1, Dongsheng Zhu2,3, Haijun Guo1

  • 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, P.R. China.

Chembiochem : a European Journal of Chemical Biology
|April 4, 2019
PubMed

Insights

Researchers identified novel protein targets of Crenolanib, a cancer drug, using chemical probes. This discovery aids in understanding its mechanism of action and potential side effects in acute myeloid leukemia treatment.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Biochemistry

Background:

  • Crenolanib is a potent inhibitor of FLT3 and PDGFRα/β, currently in Phase III trials for acute myeloid leukemia.
  • The precise protein targets of Crenolanib within cancer cells are not fully understood, hindering comprehension of its mechanism and side effects.

Purpose of the Study:

  • To identify unknown cellular targets of Crenolanib.
  • To develop tools for visualizing drug distribution and understanding drug action.

Main Methods:

  • Synthesis of a Crenolanib-based photoaffinity probe and two fluorescent probes.
  • Competitive protein profiling using pull-down assays combined with liquid chromatography-tandem mass spectrometry (LC-MS/MS).
  • Bioimaging studies using fluorescent probes for single-cell level analysis.

Main Results:

  • Identification of several previously unknown protein targets, including MAPK1, SHMT2, SLC25A11, and HIGD1A.
  • Successful characterization of cellular targets through proteomic analysis.
  • Demonstration of fluorescent probes' utility for imaging drug distribution in single cells.

Conclusions:

  • The identified protein targets offer insights into Crenolanib's mechanism of action and potential toxicities.
  • Developed chemical probes are valuable tools for further research into Crenolanib's cellular interactions and distribution.
Keywords:
cancerfluorescenceimaging agentsinhibitorsproteomics

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