期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 66, 期 7, 页码 4491-4502出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.3c00072
关键词
-
This Miniperspective summarizes the evidence for using the extracellular signal-regulated kinase 5 (ERK5) signaling pathway as a drug target in cancer chemotherapy. It discusses the structure of ERK5 and the evolution of structurally distinct chemotypes of ERK5 kinase domain inhibitors. The complexities of ERK5 pharmacology, including paradoxical ERK5 activation by small molecule inhibitors, are also explored.
The extracellular signal-regulated kinase 5 (ERK5) signaling pathway is one of four conventional mitogen-activated protein (MAP) kinase pathways. Genetic perturbation of ERK5 has suggested that modulation of ERK5 activity may have therapeutic potential in cancer chemotherapy. This Miniperspective examines the evidence for ERK5 as a drug target in cancer, the structure of ERK5, and the evolution of structurally distinct chemotypes of ERK5 kinase domain inhibitors. The emerging complexities of ERK5 pharmacology are discussed, including the confounding phenomenon of paradoxical ERK5 activation by small molecule ERK5 inhibitors. The impact of the recent development and biological evaluation of potent and selective bifunctional degraders of ERK5 and future opportunities in ERK modulation are also explored.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据