《生命科学》 2021, 33(10): 1231-1238

LGR5在结直肠癌中的作用机制及靶向治疗研究进展

彭立雄^1,2 , 常　江^1,2 , 张博威¹ , 胡学渝¹ , 谭忠鹏¹ , 柳增善^1,2,* , 胡　盼^1,2,*

¹吉林大学动物医学学院，长春 130062 ²吉林大学人兽共患病研究所教育部重点实验室，长春 130062

摘　要：

LGR5 是7 次跨膜G 蛋白偶联受体(G protein-coupled receptor, GPCR) 超家族成员，在结直肠癌中高表达。研究发现，LGR5 是结直肠癌干细胞的标志物，其异常表达能够促进结直肠癌的进展和转移，被认为是重要的结直肠癌预后不良分子。LGR5 主要通过Wnt/β-catenin 通路参与结直肠癌的发生发展，近年来针对该靶点的治疗研究不断增加。虽然靶向LGR5 的ADCs 类药物在治疗结直肠癌后存在复发的情况，但是联合用药使治疗结直肠癌的效果显著提升。该文综述了LGR5 在结直肠癌中的作用机制及靶向治疗进展，表明靶向LGR5 联合用药对于结直肠癌患者个性化治疗具有潜在的应用价值。

通讯作者：柳增善 , Email:zsliu1959@163.com 胡　盼 , Email:hupan84@163.com

The advance in the role of LGR5 and its targeted therapy in colorectal cancer

PENG Li-Xiong^1,2 , CHANG Jiang^1,2 , ZHANG Bo-Wei¹ , HU Xue-Yu¹ , TAN Zhong-Peng¹ , LIU Zeng-Shan^1,2,* , HU Pan^1,2,*

¹College of Veterinary Medicine, Jilin University, Changchun 130062, China ²Key Laboratory of Zoonosis Research, Ministry of Education/Institute of Zoonosis, Jilin University, Changchun 130062, China

Abstract:

LGR5 is a member of the seven transmembrane G protein-coupled receptor (GPCR) superfamily and is highly expressed in colorectal cancer. Studies have shown that LGR5 is a marker of colorectal cancer stem cells and its abnormal expression can promote the progression and metastasis of colorectal cancer, which is considered to be a poor prognostic molecule of colorectal cancer. LGR5 is mainly involved in the development of colorectal cancer through Wnt/β-catenin pathway, and the therapeutic researches targeting LGR5 have been increasing in recent years. Although partial treatments of colorectal cancer by ADCs drugs targeting LGR5 have recurrenced, combination therapy has significantly improved the efficacy of treatment. Here we review the role of LGR5 in colorectal cancer and its progress of targeted therapy. We indicate that targeting LGR5 combination therapy has potential value for colorectal cancer patients for personalized treatment.

Communication Author：LIU Zeng-Shan , Email:zsliu1959@163.com HU Pan , Email:hupan84@163.com