A suite of macrocyclic peptide inhibitors and substrate probes for arginine methyltransferases

Ryoji Yoshisada; Yurui Zhang; Elwin Janssen; Caroline Bouchard; David Poole; Tianzheng Wan; Leonardo Soares; Isabel Houtkamp; Jeroen de Ridder; Halima Mouhib; Matthijs J. van Haren; N. Marechal; N. Troffer-Charlier; Vincent Cura; J. Cavarelli; Hugo van Ingen; Uta-Maria Bauer; Nathaniel I. Martin; Seino A. K. Jongkees

doi:10.1039/d5sc09232a

Key Points

The aim is to develop effective inhibitors and probes for arginine methyltransferases, which play crucial roles in various cellular processes.
Synthesis of macrocyclic peptide inhibitors and substrate probes
Assessment of inhibitory potency against arginine methyltransferases
Evaluation of effects on chromatin structure and RNA processing
Identified multiple potent macrocyclic peptide inhibitors for PRMTs
Demonstrated effectiveness in modulating chromatin structure and RNA processing
Highlighting potential implications for therapeutic strategies in cancer treatment

Implication

Research investigates novel inhibitors and probes targeting arginine methyltransferases, suggesting therapeutic potential for cancer.

Abstract

Arginine methyltransferases (PRMTs) are key regulators of chromatin structure, RNA processing, and signal transduction, and their dysregulation has been linked to cancer and other diseases. The development of potent and...

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Cite This Study

Yoshisada et al. (2026) studied this question.

synapsesocial.com/papers/699fe3ec95ddcd3a253e806b https://doi.org/10.1039/d5sc09232a

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A suite of macrocyclic peptide inhibitors and substrate probes for arginine methyltransferases

Key Points

Implication

Abstract

Discussion

Cite This Study

A suite of macrocyclic peptide inhibitors and substrate probes for arginine methyltransferases

Key Points

Implication

Abstract

Discussion

Cite This Study

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