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A Novel Protein-Protein Interaction between RSK3 and IκBα and a New Binding Inhibitor That Suppresses Breast Cancer Tumorigenesis

 Hee-Sub Yoon  ;  Sung Hoon Choi  ;  Jung-Hyun Park  ;  Jin-Young Min  ;  Ju-Yong Hyon  ;  Yeji Yang  ;  Sejin Jung  ;  Jae-Young Kim  ;  Nam Doo Kim  ;  Ji Hoon Lee  ;  Eun Hee Han  ;  Sung-Gil Chi  ;  Young-Ho Chung 
 CANCERS, Vol.13(12) : 2973, 2021-06 
Journal Title
Issue Date
IκBα ; RSK3 (RPS6KA2) ; binding inhibition ; breast cancer ; cell-based unidentified protein interaction discovery (CUPID) ; protein-protein interaction (PPI)
Multiple cancer-related biological processes are mediated by protein-protein interactions (PPIs). Through interactions with a variety of factors, members of the ribosomal S6 kinase (RSK) family play roles in cell cycle progression and cell proliferation. In particular, RSK3 contributes to cancer viability, but the underlying mechanisms remain unknown. We performed a kinase library screen to find IκBα PPI binding partners and identified RSK3 as a novel IκBα binding partner using a cell-based distribution assay. In addition, we discovered a new PPI inhibitor using mammalian two-hybrid (MTH) analysis. We assessed the antitumor effects of the new inhibitor using cell proliferation and colony formation assays and monitored the rate of cell death by FACS apoptosis assay. IκBα is phosphorylated by the active form of the RSK3 kinase. A small-molecule inhibitor that targets the RSK3/IκBα complex exhibited antitumor activity in breast cancer cells and increased their rate of apoptosis. RSK3 phosphorylation and RSK3/IκBα complex formation might be functionally important in breast tumorigenesis. The RSK3/IκBα-specific binding inhibitor identified in this study represents a lead compound for the development of new anticancer drugs.
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1. College of Medicine (의과대학) > Yonsei Biomedical Research Center (연세의생명연구원) > 1. Journal Papers
Yonsei Authors
Choi, Sung Hoon(최성훈)
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