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- Title
Development of Chemical Tools to Monitor and Control Isoaspartyl Peptide Methyltransferase Activity.
- Authors
Kimura, Yusuke; Komatsu, Toru; Yanagi, Kouichi; Hanaoka, Kenjiro; Ueno, Tasuku; Terai, Takuya; Kojima, Hirotatsu; Okabe, Takayoshi; Nagano, Tetsuo; Urano, Yasuteru
- Abstract
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.
- Subjects
PROTEIN-L-isoaspartyl methyltransferase; METHYLTRANSFERASES; ASPARTYL peptides; CASPASE inhibitors; METHYLATION
- Publication
Angewandte Chemie International Edition, 2017, Vol 56, Issue 1, p153
- ISSN
1433-7851
- Publication type
Article
- DOI
10.1002/anie.201608677