Home > Browse Issues > Vol.37 No.10
The Progress on MEK Kinases and Their Inhibitors
Hao Peiqi, An Shu, Yang Yang, Liu Ying, Guo Xiaoxi, Xu Tianrui*
Cell Signaling Laboratory, Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, China
Abstract: The mitogen-activated extracellular signal-regulated kinase (MEK) is a dual specificity kinase， and a key component of RAS-RAF-MEK-ERK/MAPK signaling pathway that phosphorylate serine/threonine and tyrosine residues on target protein. It plays a critical role in the regulation of diverse cellular processes， such as cell proliferation， differentiation， motility and survival， etc. Deregulation of Ras-Raf-MEK-MAPK/ERK pathway occurs in more than 30% of human cancers. As a key node of this pathway， MEK inhibition is an attractive therapeutics strategy in a number of cancers. Several potent， highly selective， non-ATP-competitive MEK inhibitors have been developed and assessed in numerous clinical studies over the past decades. Some of them showed promising therapeutic effects in different types of solid tumors. Here we summarize the advances in MEK structure and function research and discuss the development of MEK inhibitors.
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