Toward the Development of Potent and Selective Bisubstrate Inhibitors of Protein Arginine Methyltransferases

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2010 Mar 12

PMID 20219369

Citations 26

Authors

James Dowden

Wei Hong

Richard V Parry

Richard A Pike

Stephen G Ward

Affiliations

Soon will be listed here.

Abstract

Prototype inhibitors of protein arginine methyltransferases (PRMTs) have been constructed by attaching guanidine functionality via a variable linker to non-reactive amine analogues of the cellular co-factor (S)-adenosyl methionine (AdoMet). Potent inhibition of PRMT1 (IC(50) of approximately 3-6 microM) combined with weak inhibition of the lysine methyltransferase SET7 (approximately 50% of activity at 100 microM) was observed for two such compounds.

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