@article{1627e097128e4875a096b7c97ff5684f,
title = "Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control",
abstract = "The Ras/Raf/MEK/ERK signal transduction, an oncogenic pathway implicated in a variety of human cancers, is a key target in anticancer drug design. A novel series of pyrimidylpyrrole ERK inhibitors has been identified. Discovery of a conformational change for lead compound 2, when bound to ERK2 relative to antitarget GSK3, enabled structure-guided selectivity optimization, which led to the discovery of 11e, a potent, selective, and orally bioavailable inhibitor of ERK.",
author = "Aronov, {Alex M.} and Tang Qing and Gabriel Martinez-Botella and Bemis, {Guy W.} and Jingrong Cao and Guanjing Chen and Ewing, {Nigel P.} and Ford, {Pamella J.} and Germann, {Ursula A.} and Jeremy Green and Hale, {Michael R.} and Marc Jacobs and Janetka, {James W.} and Francois Maltais and William Markland and Namchuk, {Mark N.} and Suganthini Nanthakumar and Srinivasu Poondru and Judy Straub and {Ter Haar}, Ernst and Xie Xiaoling",
year = "2009",
month = oct,
day = "22",
doi = "10.1021/jm900630q",
language = "English",
volume = "52",
pages = "6362--6368",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
number = "20",
}