Protein methyltransferases as a target class for drug discovery

RA Copeland, ME Solomon, VM Richon - Nature reviews Drug …, 2009 - nature.com
RA Copeland, ME Solomon, VM Richon
Nature reviews Drug discovery, 2009nature.com
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.
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.
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