Li Yangyang, Yi ZhongQuan, Li Xia, Wang Rui, Zhao Mengjie, Mi Lida, Zhang Weisong, Guo Rongqi, Yan Song, Song JianXiang
Department of Cardiothoracic Surgery, Affiliated Hospital 6 of Nantong University, Yancheng Third People's Hospital, Yancheng, 224000, People's Republic of China.
Department of Central Laboratory, Affiliated Hospital 6 of Nantong University, Yancheng Third People's Hospital, Yancheng, 224000, People's Republic of China.
Onco Targets Ther. 2025 Apr 15;18:545-558. doi: 10.2147/OTT.S511943. eCollection 2025.
Receptors coupled with G proteins (GPCRs) are expressed in large numbers in multiple systems, such as endocrine, cardiovascular, digestive, immune, and reproductive systems. As an important signal transduction mediator, in recent years, the research on GPCRs has become more and more in-depth. Many articles have verified that in the gastrointestinal, reproductive, and urinary systems, GPCRs are contributed to the development and occurrence of cancerous tumors and have been associated with the infiltration of malignant tumors and metastasis. Currently, in clinical practice, GPCRs become the target of action for about 30% of drugs. However, it should be noted that there are still over 100 GPCRs collectively referred to as orphan GPCRs (OGPCRs) due to the lack of corresponding ligands. Despite the lack of known ligands, research in animals and experiments has proved that numerous OGPCRs regulate crucial physiological functions and are intriguing and undeveloped targets for therapeutics. GPR137 is a member of OGPCRS, which promotes carcinogenesis and progression of cancers, and its expression is elevated in various malignant tumor tissues. Additionally, GPR137 has been shown to play a role in promoting tumorigenesis and metastasis in colorectal, gastric, hepatocellular, ovarian and prostate cancers. Knockdown of the GPR137 leads to cell cycle arrest within cancer cells, effectively inhibiting their proliferation and colony-forming ability while promoting apoptosis. This highlights its potential therapeutic significance as a target for numerous cancers.
与G蛋白偶联的受体(GPCRs)在多个系统中大量表达,如内分泌、心血管、消化、免疫和生殖系统。作为一种重要的信号转导介质,近年来,对GPCRs的研究越来越深入。许多文章证实,在胃肠道、生殖和泌尿系统中,GPCRs与癌性肿瘤的发生和发展有关,并与恶性肿瘤的浸润和转移相关。目前,在临床实践中,GPCRs成为约30%药物的作用靶点。然而,应该注意的是,由于缺乏相应的配体,仍有100多种GPCRs被统称为孤儿GPCRs(OGPCRs)。尽管缺乏已知的配体,但动物研究和实验证明,许多OGPCRs调节关键的生理功能,是有趣且未开发的治疗靶点。GPR137是OGPCRS的成员之一,它促进癌症的发生和发展,其表达在各种恶性肿瘤组织中升高。此外,GPR137已被证明在结直肠癌、胃癌、肝细胞癌、卵巢癌和前列腺癌的肿瘤发生和转移中起作用。敲低GPR137会导致癌细胞内的细胞周期停滞,有效抑制其增殖和集落形成能力,同时促进细胞凋亡。这突出了其作为众多癌症靶点的潜在治疗意义。