Article
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer.
Nature cancer - 1 Apr 2022
To Ciric, Beyett Tyler S, Jang Jaebong, Feng William W, Bahcall Magda, Haikala Heidi M, Shin Bo H, Heppner David E, Rana Jaimin K, Leeper Brittaney A, Soroko Kara M, Poitras Michael J, Gokhale Prafulla C, Kobayashi Yoshihisa, Wahid Kamal, Kurppa Kari J, Gero Thomas W, Cameron Michael D, Ogino Atsuko, Mushajiang Mierzhati, Xu Chunxiao, Zhang Yanxi, Scott David A, Eck Michael J, Gray Nathanael S, Jänne Pasi A
Abstract excerpt
Epidermal growth factor receptor (EGFR) therapy using small-molecule tyrosine kinase inhibitors (TKIs) is initially efficacious in patients with EGFR-mutant lung cancer, although drug resistance eventually develops. Allosteric EGFR inhibitors, which bind to a different EGFR site than existing ATP-competitive EGFR TKIs, have been developed as a strategy to overcome therapy-resistant EGFR mutations. Here we...
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