College of Medical Sciences, Nova Southeastern University, Fort Lauderdale, FL, United States.
Rumbaugh Goodwin Institute for Cancer Research, Nova Southeastern University, Fort Lauderdale, FL, United States.
Curr Cancer Drug Targets. 2019;19(3):179-188. doi: 10.2174/1568009618666180706165222.
Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase, which is an essential player in regulating cell migration, invasion, adhesion, proliferation, and survival. Its overexpression and activation have been identified in sixty-eight percent of epithelial ovarian cancer patients and this is significantly associated with higher tumor stage, metastasis, and shorter overall survival of these patients. Most recently, a new role has emerged for FAK in promoting resistance to taxane and platinum-based therapy in ovarian and other cancers. The development of resistance is a complex network of molecular processes that make the identification of a targetable biomarker in platinum and taxane-resistant ovarian cancer a major challenge. FAK overexpression upregulates ALDH and XIAP activity in platinum-resistant and increases CD44, YB1, and MDR-1 activity in taxaneresistant tumors. FAK is therefore now emerging as a prognostically significant candidate in this regard, with mounting evidence from recent successes in preclinical and clinical trials using small molecule FAK inhibitors. This review will summarize the significance and function of FAK in ovarian cancer, and its emerging role in chemotherapeutic resistance. We will discuss the current status of FAK inhibitors in ovarian cancers, their therapeutic competencies and limitations, and further propose that the combination of FAK inhibitors with platinum and taxane-based therapies could be an efficacious approach in chemotherapeutic resistant disease.
黏着斑激酶(FAK)是一种非受体酪氨酸激酶,在调节细胞迁移、侵袭、黏附、增殖和存活方面发挥着重要作用。在 68%的上皮性卵巢癌患者中发现了其过表达和激活,这与更高的肿瘤分期、转移和这些患者的总体生存率降低显著相关。最近,FAK 在促进卵巢癌和其他癌症对紫杉烷和铂类药物治疗的耐药性方面出现了一个新的作用。耐药性的发展是一个复杂的分子过程网络,使得在铂类和紫杉烷耐药性卵巢癌中鉴定出一个可靶向的生物标志物成为一个主要挑战。FAK 过表达在上皮性铂耐药肿瘤中上调 ALDH 和 XIAP 的活性,并在紫杉烷耐药肿瘤中增加 CD44、YB1 和 MDR-1 的活性。因此,FAK 现在作为一个预后相关的候选标志物而出现,最近在使用小分子 FAK 抑制剂的临床前和临床试验中取得了成功,这为其提供了越来越多的证据。这篇综述将总结 FAK 在卵巢癌中的意义和功能,以及其在化疗耐药性方面的新兴作用。我们将讨论卵巢癌中 FAK 抑制剂的现状、它们的治疗能力和局限性,并进一步提出,FAK 抑制剂与铂类和紫杉烷类药物联合治疗可能是治疗耐药性疾病的一种有效方法。