MAPK/ERK通路
化学
脚手架
信号转导
结构-活动关系
计算生物学
药物发现
钥匙(锁)
细胞生物学
生物化学
体外
生物
医学
生物医学工程
生态学
作者
Alex M. Aronov,Christopher T. H. Baker,Guy W. Bemis,Jingrong Cao,Guanjing Chen,Pamella J. Ford,Ursula A. Germann,J Green,Michael R. Hale,Marc Jacobs,James W. Janetka,François Maltais,Gabriel Martínez-Botella,Mark Namchuk,Judy Straub,Qing Tang,Xin Xie
摘要
The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.
科研通智能强力驱动
Strongly Powered by AbleSci AI