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

Abstract:

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 ERK1/2, SCH772984 induces a so-far-unknown binding pocket that accommodates the piperazine-phenyl-pyrimidine decoration. This new binding pocket was created by an inactive conformation of the phosph...

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Publication status:
Published

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Publisher copy:
10.1038/nchembio.1629

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Journal:
Nature chemical biology
Volume:
10
Issue:
10
Pages:
853-860
Publication date:
2014-10-01
DOI:
EISSN:
1552-4469
ISSN:
1552-4450
Source identifiers:
484497

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