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Article

AKR1C3 Inhibition: A Strategy to Reverse Osimertinib Resistance in Non-small Cell Lung Cancer.

Journal of medicinal chemistry - 26 Mar 2026

Li Wei

Abstract excerpt

Resistance to Osimertinib via the EGFR C797S mutation is a major challenge in the treatment of nonsmall cell lung cancer (NSCLC). Combining Osimertinib with SG-55, a novel selective AKR1C3 inhibitor, effectively reverses this resistance, restoring sensitivity in NSCLC cells with the C797S mutation. This highlights AKR1C3 inhibition in overcoming antitumor drug resistance for further preclinical investigation.

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Source

Identifiers

PMID: 41824443
DOI: 10.1021/acs.jmedchem.6c00654

Genes

AKR1C3
EGFR

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

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