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Article

Structural analysis of the macrocyclic inhibitor BI-4020 binding to EGFR kinase

2022-08-27

Abstract excerpt

A novel macrocyclic inhibitor of mutant EGFR ( BI-4020 ) has shown promise in pre-clinical studies of T790M and C797S drug-resistant non-small cell lung cancer. To better understand the molecular basis for BI-4020 selectivity and potency, we have carried out biochemical activity assays and structural analysis with X-ray crystallography. Biochemical potencies agree with previous studies indicating that BI-4020 is...

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Literature Corpus work
8d7db938-f969-58e1-aac5-d2e09f1c3054
DOI
10.1101/2022.08.27.505540
Open publication

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Structural analysis of the macrocyclic inhibitor BI-4020 binding to EGFR kinaseDOI 10.1101/2022.08.27.505540
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