The Scripps Research Institute, Department of Molecular Medicine, 130 Scripps Way, Jupiter, FL 33458, United States.
Cell Signal. 2018 Jan;41:65-74. doi: 10.1016/j.cellsig.2017.09.005. Epub 2017 Sep 18.
G protein-coupled receptors (GPCRs) constitute the largest and most diverse protein family in the human genome with over 800 members identified to date. They play critical roles in numerous cellular and physiological processes, including cell proliferation, differentiation, neurotransmission, development and apoptosis. Consequently, aberrant receptor activity has been demonstrated in numerous disorders/diseases, and as a result GPCRs have become the most successful drug target class in pharmaceuticals treating a wide variety of indications such as pain, inflammation, neurobiological and metabolic disorders. Many independent studies have also demonstrated a key role for GPCRs in tumourigenesis, establishing their involvement in cancer initiation, progression, and metastasis. Given the growing appreciation of the role(s) that GPCRs play in cancer pathogenesis, it is surprising to note that very few GPCRs have been effectively exploited in pursuit of anti-cancer therapies. The present review provides a broad overview of the roles that various GPCRs play in cancer growth and development, highlighting the potential of pharmacologically modulating these receptors for the development of novel anti-cancer therapeutics.
G 蛋白偶联受体（GPCRs）是人类基因组中最大、最多样化的蛋白质家族，迄今为止已鉴定出超过 800 个成员。它们在许多细胞和生理过程中发挥着关键作用，包括细胞增殖、分化、神经传递、发育和细胞凋亡。因此，受体活性异常已在许多疾病/病症中得到证实，因此 GPCR 已成为制药领域最成功的药物靶点之一，可治疗多种适应症，如疼痛、炎症、神经生物学和代谢紊乱。许多独立的研究也证明了 GPCR 在肿瘤发生中的关键作用，确立了它们在癌症起始、进展和转移中的参与。鉴于人们对 GPCR 在癌症发病机制中所起作用的认识不断提高，令人惊讶的是，很少有 GPCR 被有效地用于寻求抗癌疗法。本综述广泛概述了各种 GPCR 在癌症生长和发展中的作用，强调了药理学调节这些受体的潜力，以开发新型抗癌疗法。
