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Nat Rev Drug Discov. 2009 Sep;8(9):724-32. doi: 10.1038/nrd2974.

Protein methyltransferases as a target class for drug discovery.

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1
Epizyme, Inc., 840 Memorial Drive, Cambridge, Massachussets 02139, USA. RCopeland@epizyme.com

Abstract

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.

PMID:
19721445
DOI:
10.1038/nrd2974
[Indexed for MEDLINE]
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