《生命科学》 2023, 35(12): 1660-1668

靶向A型红细胞生成素肝配蛋白受体-2治疗肿瘤的研究进展

傅　钰¹ , 全纯涛² , 王　岳³ , 谢　妮^2,*

¹广东医科大学，湛江 524023 ²广东医科大学深圳市第二人民医院，深圳 518035 ³南华大学衡阳医学院，衡阳 421001

摘　要：

基于肿瘤和正常组织基因差异表达开发的靶向药在临床上获得巨大成功。A 型红细胞生成素肝配蛋白受体2 (EphA2) 在多种人类肿瘤中高表达，发挥驱动肿瘤增殖、迁移和侵袭的癌基因功能，有作为肿瘤治疗靶点的潜力。靶向EphA2 可有效抑制肿瘤生长，并恢复耐药肿瘤细胞对药物的敏感性。该文详细介绍了EphA2 靶点结构和双向调控信号的机制，深入探讨了不同途径在其靶向治疗中的优势和复杂性，概述了EphA2 靶向治疗的最新临床前进展，以及未来临床应用的潜力。

通讯作者：谢　妮 , Email:xn100@szu.edu.cn

Progress for targeting erythropoietin-producing hepatocellular receptor A2 in cancer-specific therapy

FU Yu¹ , QUAN Chun-Tao² , WANG Yue³ , XIE Ni^2,*

¹Guangdong Medical University, Zhanjiang 524023, China ²Guangdong Medical University Shenzhen Second People's Hospital, Shenzhen 518035, China ³Hengyang Medical School, University of South China, Hengyang 421001, China

Abstract:

Targeted drugs developed based on the differential gene expression between cancerous and normal tissues have achieved significant success in clinical settings. Erythropoietin-producing hepatocellular receptor A2 (EphA2) has been found to be highly expressed in various human tumors, and plays a role as an oncogene driving tumor proliferation, migration, and invasion, making it a promising therapeutic target for cancer treatment. Targeting EphA2 can effectively inhibit tumor growth and restore drug sensitivity in drug-resistant tumor cells. This review provided a detailed overview of the mechanisms underlying EphA2 targeting, including its target structure and bidirectional regulatory signals, and investigated the advantages and complexities of strategies targeting EphA2 through canonical and noncanonical signaling pathways. Furthermore, it summarized the latest preclinical advancements in EphA2-targeted therapy and discussed its potential for future clinical applications.

Communication Author：XIE Ni , Email:xn100@szu.edu.cn