分子靶向药物PI3K抑制剂研究进展.pdfVIP

评价与指南 Evaluation and Guide 分子靶向药物PI3K抑制剂的研究进展 金美花，孔德新* 天津医科大学药学院 天津市临床药物关键技术重点实验室、基础医学研究中心，天津 300070 [摘要] 本文通过文献检索和归纳总结,介绍了抗癌靶点分子PI3K及靶向药物PI3K抑制剂的研究进展。PI3K在肿瘤发生中起着关 键性作用，因此PI3K抑制剂已成为当前抗癌新药开发的热点。迄今为止，已有包括ZSTK474在内的近20种新型PI3K抑制剂因具 有较好的抗肿瘤效果和较低的毒性而被批准进入临床试验。PI3K抑制剂与其他药物的联合治疗试验也已取得较好效果。PI3K抑 制剂有望在不远的将来成为一类新型分子靶向药物。 [关键词] 分子靶向药物；磷脂酰肌醇3-激酶抑制剂；肿瘤药物 [中图分类号] R966 [文献标识码] A [文章编号]1672-2809(2012)05-0020-06 AAdvances in Development of Phosphatidylinositol 3-Kinase Inhibidvances in Development of Phosphatidylinositol 3-Kinase Inhibittors ors JIN Mei-hua, KONG De-xin* Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics, School of Pharmaceutical Sciences and Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin 300070, China [[Abstract] By reviewing the related publications in recent yearAbstract] s, the advances in development of phosphatidylinositol 3-kinase (PI3K) inhibitors were summarized after a brief introduction of PI3K. Accumulating reports have shown that PI3K plays an important role in tumorigenesis, therefore, development of PI3K inhibitor for cancer chemotherapy has attracted attention from researchers of both academic institutes and industries. Until now, up to 20 PI3K inhibitors have revealed favorable anticancer efficacy in preclinical experiments and entered clinical trials for further evaluation. Combination of PI3K inhibitors with other anticancer drugs showed promising efficacy. In conclusion, PI3K inhibitors are expected to become a new type of molecular-targeted drug in the near future. [[Keywords] Molecular-targeted Drug; Phosphatidylinositol 3-kinaKeywords] se inhibitors; Antitumor drug 世纪末期到21世纪初期分子靶向药物 磷脂酰肌醇3-激酶 (phosphatidylinositol 20的出现是抗癌药物研究进展的里程碑 3-kinase, PI3K) 为一种由调节亚单位p85或p101和 式的事件。分子靶向药物是指作用于肿瘤细胞的特 催化亚单位