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晚期前列腺癌特别是去势治疗后复发的去势抵抗性前列腺癌目前临床无法治愈,迫切需要合适的新型治疗药物。磷脂酰肌醇3-激酶家族(PI3K)是一组细胞内重要信号分子,其活性增强是肿瘤发生与发展的关键因素之一,其中IA类PI3K激酶在大多数癌症组织有异常表达与激活。临床与基础研究已经证实IA类p110β在前列腺癌细胞的表达明显增高,并参与了雄激素受体调控的基因表达,参与去势治疗后病情复发与恶性演变,是治疗晚期前列腺癌的新靶点。目前文献已经有多种p110β特异性抑制剂的报道,其中两个抑制剂(GSK2636771和AZD8186)已进入临床试验。本文对PI3K/p110β在前列腺癌中的表达及其靶向药物的应用进行综述。
Late prostate cancer, especially after castration treatment of castrated resistant prostate cancer is currently clinically incurable, the urgent need for a suitable new type of treatment. Phosphatidylinositol 3-kinase family (PI3K) is a group of intracellular important signaling molecules, and its activity is one of the key factors in tumorigenesis and development. Among them, type IA PI3K kinase is abnormally expressed and activated in most cancerous tissues. Clinical and basic studies have confirmed that the expression of type IA p110β in prostate cancer cells was significantly increased and involved in androgen receptor-regulated gene expression in castration treatment of disease recurrence and malignant evolution is a new target for the treatment of advanced prostate cancer . Currently there are many p110β inhibitors reported in the literature, of which two inhibitors (GSK2636771 and AZD8186) have entered clinical trials. This article reviews the expression of PI3K / p110β in prostate cancer and the application of its targeted drugs.