Protein methyltransferases as a target class for drug discovery.
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.
Copeland
Robert A
RA
Epizyme, Inc., 840 Memorial Drive, Cambridge, Massachussets 02139, USA. RCopeland@epizyme.com
Solomon
Michael E
ME
Richon
Victoria M
VM
D020134:Catalytic Domain; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015894:Genome, Human; D006801:Humans; D008958:Models, Molecular; D010600:Pharmacology / Q000639:trends; D011496:Protein Methyltransferases / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000502:physiology
D004791:Enzyme Inhibitors; D011496:Protein Methyltransferases