Protein methyltransferases as a target class for drug discovery.

Nat Rev Drug Discov

Epizyme, Inc., 840 Memorial Drive, Cambridge, Massachussets 02139, USA.

Published: September 2009

The protein methyltransferases (PMTs) - which methylate protein lysine and arginine residues and have crucial roles in gene transcription - are emerging as an important group of enzymes that play key parts in normal physiology and human diseases. The collection of human PMTs is a large and diverse group of enzymes that have a common mechanism of catalysis. Here, we review the biological, biochemical and structural data that together present PMTs as a novel, chemically tractable target class for drug discovery.

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http://dx.doi.org/10.1038/nrd2974DOI Listing

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