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

Chem Commun (Camb). 2018 Aug 14;54(66):9202-9205. doi: 10.1039/c8cc03907k.

Authors

Yoshihiro Sohtome¹, Tadahiro Shimazu, Joaquin Barjau, Shinya Fujishiro, Mai Akakabe, Naoki Terayama, Kosuke Dodo, Akihiro Ito, Minoru Yoshida, Yoichi Shinkai, Mikiko Sodeoka

Affiliation

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

PMID: 30063235
DOI: 10.1039/c8cc03907k

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.

MeSH terms

Animals
Diketopiperazines / chemical synthesis
Diketopiperazines / chemistry
Diketopiperazines / pharmacology*
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
HEK293 Cells
Heterogeneous-Nuclear Ribonucleoprotein K
Humans
Mice
Organoselenium Compounds / chemistry
Piperazines / chemistry
Protein-Arginine N-Methyltransferases / antagonists & inhibitors*
Ribonucleoproteins / metabolism
S-Adenosylmethionine / analogs & derivatives
S-Adenosylmethionine / chemistry
Stereoisomerism

Substances

Diketopiperazines
Enzyme Inhibitors
HNRNPK protein, mouse
Heterogeneous-Nuclear Ribonucleoprotein K
Organoselenium Compounds
Piperazines
Ribonucleoproteins
SeAdoYn
epidithiodiketopiperazine
S-Adenosylmethionine
Prmt1 protein, mouse
Protein-Arginine N-Methyltransferases