Kwon Mi Jeong
Vessel-Organ Interaction Research Center (MRC), College of Pharmacy, Kyungpook National University, Daegu, Republic of Korea.
BK21 FOUR KNU Community-Based Intelligent Novel Drug Discovery Education Unit, College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, 80 Daehak-ro, Buk-gu, Daegu, 41566, Republic of Korea.
Cancer Cell Int. 2023 Dec 18;23(1):331. doi: 10.1186/s12935-023-03180-6.
As aberrant alternative splicing by either dysregulation or mutations of splicing factors contributes to cancer initiation and progression, splicing factors are emerging as potential therapeutic targets for cancer therapy. Therefore, pharmacological modulators targeting splicing factors have been under development. Epithelial splicing regulatory protein 1 (ESRP1) is an epithelial cell-specific splicing factor, whose downregulation is associated with epithelial-mesenchymal transition (EMT) by regulating alternative splicing of multiple genes, such as CD44, CTNND1, ENAH, and FGFR2. Consistent with the downregulation of ESRP1 during EMT, it has been initially revealed that high ESRP1 expression is associated with favorable prognosis and ESRP1 plays a tumor-suppressive role in cancer progression. However, ESRP1 has been found to promote cancer progression in some cancers, such as breast and ovarian cancers, indicating that it plays a dual role in cancer progression depending on the type of cancer. Furthermore, recent studies have reported that ESRP1 affects tumor growth by regulating the metabolism of tumor cells or immune cell infiltration in the tumor microenvironment, suggesting the novel roles of ESRP1 in addition to EMT. ESRP1 expression was also associated with response to anticancer drugs. This review describes current understanding of the roles and mechanisms of ESRP1 in cancer progression, and further discusses the emerging novel roles of ESRP1 in cancer and recent attempts to target splicing factors for cancer therapy.
由于剪接因子的失调或突变导致的异常可变剪接促进了癌症的发生和发展,剪接因子正逐渐成为癌症治疗的潜在靶点。因此,针对剪接因子的药理调节剂正在研发中。上皮剪接调节蛋白1(ESRP1)是一种上皮细胞特异性剪接因子,其下调通过调节多个基因(如CD44、CTNND1、ENAH和FGFR2)的可变剪接与上皮-间质转化(EMT)相关。与EMT过程中ESRP1的下调一致,最初发现ESRP1高表达与良好预后相关,且ESRP1在癌症进展中发挥肿瘤抑制作用。然而,已发现ESRP1在某些癌症(如乳腺癌和卵巢癌)中促进癌症进展,这表明它在癌症进展中根据癌症类型发挥双重作用。此外,最近的研究报道ESRP1通过调节肿瘤细胞的代谢或肿瘤微环境中的免疫细胞浸润来影响肿瘤生长,这表明ESRP1除了在EMT中发挥作用外还有新的作用。ESRP1表达也与抗癌药物的反应相关。本综述描述了目前对ESRP1在癌症进展中的作用和机制的理解,并进一步讨论了ESRP1在癌症中的新出现的作用以及最近针对剪接因子进行癌症治疗的尝试。