2D-DIGEによる薬剤標的解析 (ChemProteoBase)

概要

薬剤の作用に応答して細胞内の蛋白質の発現量や修飾が変化します。２次元電気泳動を用いた蛍光標識二次元ディファレンスゲル電気泳動解析システム(2D-DIGE)を用いて薬剤処理HeLa細胞のプロテオーム解析を行います。およそ３００スポットのデータをもとに作用標的の明らかな化合物とクラスター解析を用いて比較します。

主な解析化合物：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⁾

References:

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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