文章：

PIK3CA基因异常及其在实体恶性肿瘤靶向治疗中的作用

PIK3CA gene aberrancy and role in targeted therapy of solid malignancies 

原文发布日期：2020-01-28 

英文摘要：

Phosphoinositide kinases (PIKs) are a group of lipid kinases that are important upstream activators of various signaling pathways that drive oncogenesis. Hyperactivation of the PI3K/AKT/mTOR pathways—either via mutations or genomic amplification—confers key oncogenic activity, essential for the development and progression of several solid tumors. Alterations in the PIK3CA gene are associated with poor prognosis of solid malignancies. Contradictory reports exist in the literature regarding the prognostic value of PIK3CA in aggressive cancers, but most available data highlights an important role of PIK3CA mutation in mediating tumorigenesis via increased signaling of the PI3K/AKT/mTOR survival pathway. Several inhibitors of PI3K/AKT/mTOR pathways have been investigated as potential therapeutic options in solid malignancies. This article reviews the role of PIK3CA mutations and inhibitors of the PI3K/AKT/mTOR pathway in cancer and examines association with the clinico-pathological parameters and prognosis. 

摘要翻译： 

磷酸肌醇激酶（PIKs）是一类脂质激酶，作为多种致癌信号通路的重要上游激活因子，通过PI3K/AKT/mTOR通路的异常激活（由突变或基因组扩增引发）赋予关键致癌活性，这对多种实体肿瘤的发生发展至关重要。PIK3CA基因的改变与实体恶性肿瘤的不良预后相关。尽管文献中关于PIK3CA在侵袭性癌症中预后价值的报道存在矛盾，但现有数据大多表明PIK3CA突变通过增强PI3K/AKT/mTOR生存通路信号传导，在介导肿瘤发生中发挥重要作用。目前已有多种PI3K/AKT/mTOR通路抑制剂作为实体恶性肿瘤的潜在治疗选择被深入研究。本文综述了PIK3CA突变及PI3K/AKT/mTOR通路抑制剂在癌症中的作用，并探讨其与临床病理参数和预后的关联性。

原文链接：

PIK3CA gene aberrancy and role in targeted therapy of solid malignancies