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Article

Activation of tyrosine kinases by mutation of the gatekeeper threonine.

Nature structural & molecular biology - 1 Oct 2008

Azam Mohammad, Seeliger Markus A, Gray Nathanael S, Kuriyan John, Daley George Q

Abstract excerpt

Protein kinases targeted by small-molecule inhibitors develop resistance through mutation of the 'gatekeeper' threonine residue of the active site. Here we show that the gatekeeper mutation in the cellular forms of c-ABL, c-SRC, platelet-derived growth factor receptor-alpha and -beta, and epiderm...

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Share to Crystallography, X-Ray
Share to CSK Tyrosine-Protein Kinase
Share to Hydrophobic and Hydrophilic Interactions

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Share to Proto-Oncogene Proteins c-abl

Share to Receptors, Platelet-Derived Growth Factor

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Source

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Identifiers

PMID: 18794843
DOI: 10.1038/nsmb.1486
PMCID: PMC2575426

Genes

BCR
SRC

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026. Prepared record publication-18794843-2026-09-02.2. Manifest publication-graph-cohort-2026-09-02.2.

Source receipt: PubMed via Helena Literature Corpus, retrieved 2 Sept 2026.

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