A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.

Activation of the ERK pathway is a hallmark of cancer, and targeting of upstream signaling partners led to the development of approved drugs. Recently, SCH772984 has been shown to be a selective and potent ERK1/2 inhibitor. Here we report the structural mechanism for its remarkable selectivity. In E...

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Bibliographic Details
Main Authors: Chaikuad, A, Tacconi, E, Zimmer, J, Liang, Y, Gray, N, Tarsounas, M, Knapp, S
Format: Journal article
Language:English
Published: 2014