Copeland Robert A, Solomon Michael E, Richon Victoria M
Epizyme, Inc., 840 Memorial Drive, Cambridge, Massachussets 02139, USA.
Nat Rev Drug Discov. 2009 Sep;8(9):724-32. doi: 10.1038/nrd2974.
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.
蛋白质甲基转移酶（PMTs）——可使蛋白质赖氨酸和精氨酸残基发生甲基化，在基因转录中起关键作用——正成为一类重要的酶，在正常生理和人类疾病中发挥关键作用。人类PMTs是一组庞大且多样的酶，具有共同的催化机制。在此，我们综述生物学、生物化学和结构数据，这些数据共同表明PMTs是一类用于药物发现的新型、化学上易于处理的靶点。
