Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control

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 relat...

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Bibliographic Details

Published in:	Journal of medicinal chemistry 2009-10, Vol.52 (20), p.6362-6368
Main Authors:	Aronov, Alex M, Tang, Qing, Martinez-Botella, Gabriel, Bemis, Guy W, Cao, Jingrong, Chen, Guanjing, Ewing, Nigel P, Ford, Pamella J, Germann, Ursula A, Green, Jeremy, Hale, Michael R, Jacobs, Marc, Janetka, James W, Maltais, Francois, Markland, William, Namchuk, Mark N, Nanthakumar, Suganthini, Poondru, Srinivasu, Straub, Judy, ter Haar, Ernst, Xie, Xiaoling
Format:	Article
Language:	English
Subjects:	Antineoplastic agents Biological and medical sciences Drug Design Extracellular Signal-Regulated MAP Kinases - antagonists & inhibitors Extracellular Signal-Regulated MAP Kinases - chemistry General aspects Medical sciences Models, Molecular Molecular Conformation Pharmacology. Drug treatments Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyrroles - chemistry Pyrroles - pharmacology Substrate Specificity
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