タナベ ケンジ
  田邊 賢司
   所属   研究施設 研究施設
   職種   准教授
論文種別 原著
言語種別 英語
査読の有無 査読あり
表題 Image-based compound profiling reveals a dual inhibitor of tyrosine kinase and microtubule polymerization.
掲載誌名 正式名:Scientific reports
略  称:Sci Rep
ISSNコード:(2045-2322)2045-2322(Linking)
掲載区分国外
巻・号・頁 6,25095頁
著者・共著者 Tanabe Kenji
発行年月 2016/04
概要 Small-molecule compounds are widely used as biological research tools and therapeutic drugs. Therefore, uncovering novel targets of these compounds should provide insights that are valuable in both basic and clinical studies. I developed a method for image-based compound profiling by quantitating the effects of compounds on signal transduction and vesicle trafficking of epidermal growth factor receptor (EGFR). Using six signal transduction molecules and two markers of vesicle trafficking, 570 image features were obtained and subjected to multivariate analysis. Fourteen compounds that affected EGFR or its pathways were classified into four clusters, based on their phenotypic features. Surprisingly, one EGFR inhibitor (CAS 879127-07-8) was classified into the same cluster as nocodazole, a microtubule depolymerizer. In fact, this compound directly depolymerized microtubules. These results indicate that CAS 879127-07-8 could be used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics. The image-based multivariate analysis developed herein has potential as a powerful tool for discovering unexpected drug properties.
DOI 10.1038/srep25095
PMID 27117592