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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引用次数: 0

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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抗肿瘤中EGFR-TKIs耐药性的天然产物

天然产物在癌症治疗中的作用已受到广泛关注。重要的是，天然产物可以与多个靶点相互作用，这对协同克服耐药具有重要意义。对表皮生长因子受体(EGFR)-酪氨酸激酶抑制剂（TKIs）的耐药性是导致非小细胞肺癌（NSCLC）治疗失败的一个重要原因。在这篇综述中，我们总结了对EGFR- tkis的主要耐药机制，并提出67种已报道的天然产物（从2005年到2024年）通过至少30种途径显示出对抗癌症中EGFR- tkis耐药的潜力，主要包括ROS、PD-L1、EGFR、MAPK、mTOR、HSP90、JNK、PTEN和FOXO。根据五项可药性评价原则，得到37种适合进一步开发的天然产物。本文旨在系统总结天然产物在克服EGFR-TKIs耐药方面的最新进展，为非小细胞肺癌等癌症的新药开发提供一些启示。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

European Journal of Medicinal Chemistry Reports

CiteScore

4.50

自引率

0.00%

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