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Article

Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR.

Journal of enzyme inhibition and medicinal chemistry - 1 Dec 2023

Foschi Francesca, Tinivella Annachiara, Crippa Valentina, Pinzi Luca, Mologni Luca, Passarella Daniele, Rastelli Giulio

Abstract excerpt

EGFR is a protein kinase whose aberrant activity is frequently involved in the development of non-small lung cancer (NSCLC) drug resistant forms. The allosteric inhibition of this enzyme is currently one among the most attractive approaches to design and develop anticancer drugs. In a previous study, we reported the identification of a hit compound acting as type III allosteric inhibitor of the L858R/T790M double...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 36373202
DOI: 10.1080/14756366.2022.2145284
PMCID: PMC9665079

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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