Natural products combating EGFR-TKIs resistance in cancer

European Journal of Medicinal Chemistry Reports Pub Date : 2025-02-11 DOI:10.1016/j.ejmcr.2025.100251

Li Xia , Gaohui Zhu , Qiyao Peng , Xiuyang Li , Xinrong Zou , Wanping Zhang , Lulu Zhao , Xiong Li , Ping Wu , Aimin Luo , Teng Yang , Meizi Chen , Teng Liu , Yongbo Peng

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Abstract

The role of natural products in cancer treatment has received substantial attention. Significantly, natural products can interact with multiple targets, which is meaningful in overcoming drug resistance synergistically. Resistance to epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors (TKIs) is a significant cause of treatment failure in non-small cell lung cancer (NSCLC). In this review, we summarize the main resistance mechanisms to EGFR-TKIs and present that 67 reported natural products (from 2005 to 2024) demonstrate the potential to combat EGFR-TKIs resistance in cancer via at least 30 pathways, mainly including ROS, PD-L1, EGFR, MAPK, mTOR, HSP90, JNK, PTEN, and FOXO. Based on the rule of five evaluation of druggability, we can obtain 37 natural products suitable for further development. This review aims to systematically summarize recent advances of natural products in overcoming EGFR-TKIs resistance, and provide some inspirations for novel drug discovery in cancer including NSCLC.

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来源期刊

European Journal of Medicinal Chemistry Reports

CiteScore

4.50

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0.00%

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