Convergence of EGFR glioblastoma mutations: evolution and allostery rationalizing targeted therapy.
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Mol Cell Oncol 6 (5) e1630798 [2019-07-04; online 2019-07-04]
EGFR mutations display striking organ-site asymmetry and heterogeneity. We have shown that structurally diverse extracellular mutations, typical of glioblastomas, converge to a similar intermediate conformation, which can be synergistically targeted extra- and intracelullarly by antibody mAb806 and type-II kinase inhibitors. Our findings reveal convergence behind heterogeneity, paving the way for allostery-based co-targeting.
PubMed 31528699
DOI 10.1080/23723556.2019.1630798
Crossref 10.1080/23723556.2019.1630798
pmc: PMC6736128
pii: 1630798