Article
Identification of a novel nitroflavone-based scaffold for designing mutant-selective EGFR tyrosine kinase inhibitors targeting T790M and C797S resistance in advanced NSCLC.
Bioorganic chemistry - 1 Dec 2022
Cristina Minnelli, Emiliano Laudadio, Leonardo Sorci, Giulia Sabbatini, Roberta Galeazzi, Adolfo Amici, Marta Semrau S, Paola Storici, Samuele Rinaldi, Pierluigi Stipa, Massimo Marcaccio, Giovanna Mobbili
Abstract excerpt
The inhibition of the Epidermal Growth Factor (EGFR) represents one of the most promising strategies in non-small cell lung cancer (NSCLC) therapy. The recently identified C797S mutation causes resistance of EGFRL858R/T790M against osimertinib, the latest approved third generation EGFR inhibitor. The identification of small molecules capable of selectively inhibiting the T790M mutations also in the late-onset...
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