Development of Chemical Tools to Monitor and Control Isoaspartyl Peptide Methyltransferase Activity

Yusuke Kimura, Toru Komatsu, Kouichi Yanagi, Kenjiro Hanaoka, Tasuku Ueno, Takuya Terai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Yasuteru Urano

研究成果: Article査読

10 被引用数 (Scopus)

抄録

We have established a coupled assay system targeting protein l-isoaspartyl methyltransferase (PIMT), a key enzyme in the metabolism of isoaspartyl peptides and proteins. The system utilizes a fluorogenic peptide probe containing an isoaspartyl residue at the P1′ position of the caspase-3 recognition sequence. Following PIMT-catalyzed methyl transfer reaction, the methylated probe is specifically cleaved by caspase-3 to give fluorescence activation. High-throughput screening of our chemical library with this assay system identified PIMT inhibitors that may be useful as leads in the design of chemical probes for controlling PIMT activity.

本文言語English
ページ(範囲)153-157
ページ数5
ジャーナルAngewandte Chemie - International Edition
56
1
DOI
出版ステータスPublished - 2017 1月 2
外部発表はい

ASJC Scopus subject areas

  • 触媒
  • 化学一般

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