Article
Mechanisms and clinical activity of an EGFR and HER2 exon 20-selective kinase inhibitor in non-small cell lung cancer.
Nature medicine - 1 May 2018
Robichaux Jacqulyne P, Elamin Yasir Y, Tan Zhi, Carter Brett W, Zhang Shuxing, Liu Shengwu, Li Shuai, Chen Ting, Poteete Alissa, Estrada-Bernal Adriana, Le Anh T, Truini Anna, Nilsson Monique B, Sun Huiying, Roarty Emily, Goldberg Sarah B, Brahmer Julie R, Altan Mehmet, Lu Charles, Papadimitrakopoulou Vassiliki, Politi Katerina, Doebele Robert C, Wong Kwok-Kin, Heymach John V
Abstract excerpt
Although most activating mutations of epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancers (NSCLCs) are sensitive to available EGFR tyrosine kinase inhibitors (TKIs), a subset with alterations in exon 20 of EGFR and HER2 are intrinsically resistant and lack an effective therapy. We used in silico, in vitro, and in vivo testing to model structural alterations induced by exon 20 mutations and...
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