Unveiling epidithiodiketopiperazine as a non-histone arginine methyltransferase inhibitor by chemical protein methylome analyses

Yoshihiro Sohtome; Tadahiro Shimazu; Joaquin Barjau; Shinya Fujishiro; Mai Akakabe; Naoki Terayama; Kosuke Dodo; Akihiro Ito; Minoru Yoshida; Yoichi Shinkai; Mikiko Sodeoka

doi:10.1039/C8CC03907K

Unveiling epidithiodiketopiperazine as a non-histone arginine methyltransferase inhibitor by chemical protein methylome analyses†

Yoshihiro Sohtome,

^abc Tadahiro Shimazu,^d Joaquin Barjau,^a Shinya Fujishiro,^a Mai Akakabe,^a Naoki Terayama,^abc Kosuke Dodo,

^abc Akihiro Ito,^be Minoru Yoshida,^bf Yoichi Shinkai^d and Mikiko Sodeoka

*^abc

Author affiliations

* Corresponding authors

^a Synthetic Organic Chemistry Laboratory, RIKEN Cluster for Pioneering Research, 2-1, Wako, Saitama 351-0198, Japan
E-mail: sodeoka@riken.jp

^b RIKEN Center for Sustainable Resource Science, RIKEN, Japan

^c AMED-CREST, Japan Agency for Medical Research and Development, Japan

^d Cellular Memory Laboratory, RIKEN Cluster for Pioneering Research, Japan

^e School of Life Sciences, Tokyo University of Pharmacy and Life Sciences, Japan

^f Department of Biotechnology, Graduate School of Agricultural Life Sciences, The University of Tokyo, Japan

Abstract

We present a chemical methylome analysis platform to evaluate the inhibitory activity of small molecules towards poorly characterized protein methyltransferases (PMTs), facsilitating to identify syn-HyPA-ETP-2 as a non-histone arginine methyltransferase inhibitor.

Chemical Communications

Unveiling epidithiodiketopiperazine as a non-histone arginine methyltransferase inhibitor by chemical protein methylome analyses†

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Unveiling epidithiodiketopiperazine as a non-histone arginine methyltransferase inhibitor by chemical protein methylome analyses

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