Dataset Information

Biochemical and Structural Basif for Differential Inhibitor Sensitivity of EGFR with Distinct Exon 19 Mutaions

ABSTRACT: Tyrosine kinase inhibitors (TKIs) are used to treat non-small cell lung cancers (NSCLC) driven by epidermal growth factor receptor (EGFR) mutations in the tyrosine kinase domain (TKD). We studied structural basis of differential TKI sensitivity among EGFR exon 19 mutants by HDX-MS.

INSTRUMENT(S): Synapt MS

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: Yuko Tsutsui

LAB HEAD: Yuko Tsutsui

PROVIDER: PXD037374 | Pride | 2023-03-11

REPOSITORIES: Pride

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			Action	DRS
	20210225_IndelP_180sec_01.raw.zip	Raw
	20210225_IndelP_600sec_01.raw.zip	Raw
	20210225_IndelP_60sec_01.raw.zip	Raw
	20210225_IndelP_60sec_02.raw.zip	Raw
	20210225_IndelP_FullD_01.raw.zip	Raw

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Biochemical and structural basis for differential inhibitor sensitivity of EGFR with distinct exon 19 mutations.

van Alderwerelt van Rosenburgh Iris K IK Lu David M DM Grant Michael J MJ Stayrook Steven E SE Phadke Manali M Walther Zenta Z Goldberg Sarah B SB Politi Katerina K Lemmon Mark A MA Ashtekar Kumar D KD Tsutsui Yuko Y

Nature communications 20221110 1

Tyrosine kinase inhibitors (TKIs) are used to treat non-small cell lung cancers (NSCLC) driven by epidermal growth factor receptor (EGFR) mutations in the tyrosine kinase domain (TKD). TKI responses vary across tumors driven by the heterogeneous group of exon 19 deletions and mutations, but the molecular basis for these differences is not understood. Using purified TKDs, we compared kinetic properties of several exon 19 variants. Although unaltered for the second generation TKI afatinib, sensiti ...[more]

PMID: 36357385

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