Yang Linlin, Wang Jing, Gong Xiaodi, Fan Qiong, Yang Xiaoming, Cui Yunxia, Gao Xiaoyan, Li Lijuan, Sun Xiao, Li Yuhong, Wang Yudong
Department of Gynecological Oncology, The International Peace Maternity and Child Health Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, China.
Shanghai Municipal Key Clinical Specialty, Shanghai, China.
Front Genet. 2022 Jan 24;12:728827. doi: 10.3389/fgene.2021.728827. eCollection 2021.
The leucine-rich repeats containing G protein-coupled receptor 4 (LGR4) belonging to G protein-coupled receptors (GPCRs) family, had various regulatory roles at multiple cellular types and numerous targeting sites, and aberrant LGR4 signaling played crucial roles in diseases and carcinogenesis. On the basis of these facts, LGR4 may become an appealing therapeutic target for the treatment of diseases and tumors. However, a comprehensive investigation of its functions and applications was still lacking. Hence, this paper provided an overview of the molecular characteristics and signaling mechanisms of LGR4, its involvement in multiple organ development and participation in the modulation of immunology related diseases, metabolic diseases, and oxidative stress damage along with cancer progression. Given that GPCRs accounted for almost a third of current clinical drug targets, the in-depth understanding of the sophisticated connections of LGR4 and its ligands would not only enrich their regulatory networks, but also shed new light on designing novel molecular targeted drugs and small molecule blockers for revolutionizing the treatment of various diseases and tumors.
富含亮氨酸重复序列的G蛋白偶联受体4（LGR4）属于G蛋白偶联受体（GPCR）家族，在多种细胞类型和众多靶点发挥着多种调节作用，LGR4信号异常在疾病和肿瘤发生中起关键作用。基于这些事实，LGR4可能成为治疗疾病和肿瘤的有吸引力的治疗靶点。然而，对其功能和应用仍缺乏全面研究。因此，本文概述了LGR4的分子特征和信号机制，其在多个器官发育中的作用以及参与免疫相关疾病、代谢疾病、氧化应激损伤以及癌症进展的调节。鉴于GPCR占目前临床药物靶点的近三分之一，深入了解LGR4及其配体的复杂联系不仅会丰富其调控网络，还将为设计新型分子靶向药物和小分子阻滞剂带来新的启示，从而彻底改变各种疾病和肿瘤的治疗方式。
