Drug target analysis based on proteomic analysis by 2D-DIGE.


The exposure of the cells to bioactive small-molecules induces specific changes of the proteome. Using two-dimensional difference gel electrophoresis (2D-DIGE), proteomic analysis of the HeLa cells treated with a new compound is performed. Based on the expression data of ~300 spots, we compare well-characterized inhibitors and new compounds by hierarchical cluster analysis.

Compounds:Iejimalide A, BNS-22

  1. Proteomic profiling system for drug target analysis using 2D-DIGE.(2)
  2. Clustering of BNS-22 and well-known inhibitors based on the data of proteomic analysis using 2D-DIGE.

HeLa cells were treated with compound or with DMSO for 18 h were analyzed by 2D-DIGE and hierarchical cluster analysis was performed using the quantitative data of spots. The target of BNS-22 was estimated to Topo II by the system and inhibitory activity against Topo II was verified. This figure was modified based on the previously published data.(3)


  1. M. Muroi, S. Kazami, K. Noda, H. Kondo, H. Takayama, M. Kawatani, T. Usui, H. Osada.
    Application of proteomic profiling based on 2D-DIGE for classification of compounds according to the mechanism of action,
    Chem. Biol., 17, 460-70 (2010).

  2. K. Wierzba, M. Muroi, H. Osada.
    Proteomics accelerating the identification of the target molecule of bioactive small molecules.
    Curr. Opin. Chem.Biol., 15, 57-65 (2011).

  3. M. Kawatani, H. Takayama, M. Muroi, S. Kimura, T Maekawa, H. Osada.
    Identification of a small-molecule inhibitor of DNA topoisomerase II by proteomic profiling,
    Chem. Biol., 18, 743-751 (2011).


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