Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019–2024)

Das, Debasis; Xie, Lingzhi; Hong, Jian

doi:10.1039/d4md00384e

RSC Med. Chem.

2024

DOI: 10.1039/d4md00384e

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Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019–2024)

Debasis Das,

Lingzhi Xie,

Jian Hong

Abstract: Prospects of novel fourth-generation EGFR-TKIs overcoming C797S-mediated resistance in non-small cell lung cancer.

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Cited by 3 publications

References 103 publications

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Coccinic acid exhibits anti-tumor efficacy against NSCLC harboring EGFR L858R/T790M mutation via the EGFR/STAT3 pathway

Sun,

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et al. 2025

Bioorganic Chemistry

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Coccinic acid exhibits anti-tumor efficacy against NSCLC harboring EGFR L858R/T790M mutation via the EGFR/STAT3 pathway

Sun,

Zhang,

et al. 2025

Bioorganic Chemistry

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Gold(I) complexes bearing EGFR-inhibiting ligands as anti-HCC agents through dual targeting of EGFR and TrxR

Wang,

Ma,

Chen

et al. 2025

European Journal of Medicinal Chemistry

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Inhibitory effect of 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone against NSCLC with L858R/T790M/C797S mutant EGFR

Wang,

Zhang

et al. 2024

Sci Rep

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Epidermal growth factor receptor (EGFR)-activating mutations are critical factors in the development of EGFR-driven non-small-cell lung cancer (NSCLC), and molecular targeted therapies have focused on inhibiting these mutations. EGFR tyrosine kinase inhibitors (TKIs) have remarkable inhibitory effects on NSCLC with EGFR mutations. However, acquired resistance limits the clinical application of EGFR-TKIs, highlighting the need for discovery of novel therapeutic strategies. 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone is a natural product derived from Garcinia xanthochymus , has shown potential anti-tumor activity, but the underlying mechanism needs further elucidation. In this study, we developed Ba/F3 and NIH/3T3 cells harboring EGFR L858R/T790M/C797S mutation, and then found that 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone exerted inhibitory effects against cells with EGFR L858R/T790M/C797S mutation. Additionally, 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone exhibited potent anti-tumor activity against cells harboring the triple-mutant EGFR by promoting apoptosis and inducing changes in cell cycle distribution. Furthermore, 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone was found to significantly reduce tumor growth via suppressing the phosphorylation of EGFR in tumor tissues. These effects are associated with binding of 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone to EGFR resulting in the suppression of extracellular signal-regulated kinase (Erk) phosphorylation. In conclusion, our results suggest that 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone may be a potential novel candidate for further investigation and treatment of NSCLC with the triple-mutant EGFR. Supplementary Information The online version contains supplementary material available at 10.1038/s41598-024-78146-3.

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Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019–2024)

Abstract: Prospects of novel fourth-generation EGFR-TKIs overcoming C797S-mediated resistance in non-small cell lung cancer.

Cited by 3 publications

References 103 publications

Coccinic acid exhibits anti-tumor efficacy against NSCLC harboring EGFR L858R/T790M mutation via the EGFR/STAT3 pathway

Coccinic acid exhibits anti-tumor efficacy against NSCLC harboring EGFR L858R/T790M mutation via the EGFR/STAT3 pathway

Gold(I) complexes bearing EGFR-inhibiting ligands as anti-HCC agents through dual targeting of EGFR and TrxR

Inhibitory effect of 1,4,5,6-tetrahydroxy-7,8-diprenylxanthone against NSCLC with L858R/T790M/C797S mutant EGFR

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