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

Resistance to Osimertinib via the EGFR C797S mutation is a major challenge in the treatment of nonsmall cell lung cancer (NSCLC). Combining Osimertinib with <b>SG-55</b>, 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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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2026-03-13
DOI
https://doi.org/10.1021/acs.jmedchem.6c00654
Primary Topic
Aldose Reductase and Taurine
Type
article
Field-Weighted Citation Impact
0.00
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article

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

Wei Li
Journal of Medicinal Chemistry
Aldose Reductase and Taurine
article

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

Wei Li
article en

Abstract

Resistance to Osimertinib via the EGFR C797S mutation is a major challenge in the treatment of nonsmall cell lung cancer (NSCLC). Combining Osimertinib with <b>SG-55</b>, 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.

Journal of Medicinal ChemistryVol. 69(6)
China Pharmaceutical University (CN)
Good health and well-being
Openalex Percentile: Top 23%
Aldose Reductase and Taurine
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AKR1C3 Inhibition: A Strategy to Reverse Osimertinib Resistance in Non-small Cell Lung Cancer — Wei Li · Journal of Medicinal Chemistry (2026) | TGRS Research Map | TGRS