Colic Eva, Patel Preya U, Kent Oliver A
Department of Pharmacology, adMare BioInnovations, Montreal, Quebec, Canada.
Onco Targets Ther. 2022 Nov 5;15:1331-1346. doi: 10.2147/OTT.S361512. eCollection 2022.
Ovarian cancer remains the most lethal gynecological malignancy worldwide due to lack of effective screening, vague early symptoms, poor description of biomarkers, and absence of effective treatment regimes. Epithelial ovarian carcinoma (EOC) is categorized into five distinct disease subtypes which collectively account for ~90% of ovarian carcinomas. Most women present at advanced stages contributing to a poor overall 5-year survival rate. Standard treatment for EOC is cytoreductive surgery and platinum-based chemotherapy; however, most patients suffer from recurrence and platinum-resistant disease, which highlights an urgent need for targeted therapy. The high frequency of molecular alterations affecting gain-of-function signaling through the RAS mitogen-activated protein kinase (MAPK) pathway in EOC has prompted pre-clinical and clinical efforts toward research into the effectiveness of MAPK pathway inhibition as a second-line treatment. The RAS/MAPK pathway is a highly conserved signal transduction cascade, often disrupted in cancer, that regulates tumorigenic phenotypes including cellular proliferation, survival, migration, apoptosis, and differentiation. Herein, the role of the MAPK pathway in EOC with emphasis on targetability of the pathway is described. Pre-clinical and clinical efforts to target MAPK signaling in EOC have identified several MAPK pathway inhibitors that offer efficacious potential for monotherapy and in combination with other compounds. Thus, inhibition of the RAS/MAPK pathway is emerging as a tractable strategy for treatment of ovarian cancer that may permit development of personalized therapy and improved prognosis for women challenged by this disease.
由于缺乏有效的筛查手段、早期症状不明确、生物标志物描述不佳以及缺乏有效的治疗方案,卵巢癌仍然是全球最致命的妇科恶性肿瘤。上皮性卵巢癌(EOC)分为五种不同的疾病亚型,共占卵巢癌的约90%。大多数女性就诊时已处于晚期,导致总体5年生存率较低。EOC的标准治疗方法是细胞减灭术和铂类化疗;然而,大多数患者会复发并出现铂耐药疾病,这凸显了对靶向治疗的迫切需求。EOC中通过RAS丝裂原活化蛋白激酶(MAPK)途径影响功能获得性信号传导的分子改变频率较高,这促使临床前和临床研究致力于探究MAPK途径抑制作为二线治疗的有效性。RAS/MAPK途径是一种高度保守的信号转导级联反应,在癌症中常被破坏,它调节包括细胞增殖、存活、迁移、凋亡和分化在内的致瘤表型。本文描述了MAPK途径在EOC中的作用,重点是该途径的可靶向性。针对EOC中MAPK信号传导的临床前和临床研究已确定了几种MAPK途径抑制剂,它们在单药治疗以及与其他化合物联合使用时具有有效的潜力。因此,抑制RAS/MAPK途径正在成为一种可处理的卵巢癌治疗策略,这可能有助于开发个性化治疗方案并改善受该疾病困扰的女性的预后。