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Advanced prostate cancer, especially at the castration-resistant stage, remains incurable clinically and, therefore, urgently requires new therapeutics for the patients. PI3K is a family of critical cell signal transduction molecules and their over-activation is an important factor in cancer development and progression. It has been demonstrated that class IA PI3K p110 is drastically overexpressed in prostate cancer and involved in androgen receptor-mediated gene expression and castration-resistant progression and regarded as a potential therapeutic target for prostate cancer. Several p110-specific inhibitors have been reported recently and two of them, GSK2636771 and AZD8186, are being tested in clinical trials.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。. |
