单军奇 张玉林 陈德喜 郭洪亮

    [摘要] HIV蛋白酶抑制剂(PIs)是一类抗HIV药物，其广泛应用大大提高了HIV感染者的生存率并延长了其生存期。近来，人们发现PIs具有抗肿瘤活性，这引发了将PIs重新定位为有效肿瘤化疗药物的想法。本文回顾综述了PIs近年来的研究进展以及其在肿瘤治疗中所起的作用，包括已确定的抗肿瘤机制，完成和正在进行的临床试验，为PIs在今后抗肿瘤方向奠定了基础。

    [关键词] HIV蛋白酶抑制剂；肿瘤；内质网应激；细胞自噬

    [中图分类号] R273 [文献标识码] A [文章编号] 1673-7210(2016)03(c)-0051-05

    [Abstract] HIV protease inhibitors (PIs) are widely used to anti-human immunodeficiency virus， which effectively improves the survival of HIV infected people. Recently， PIs were found to have an activity of anti-neoplasm. So PIs are now being considered as an agent to be used for anti-neoplasm chemotherapy. This artical will review and discuss the current research progress about the mechanism of PIs anti-neoplasm that has been identified， completed and ongoing clinical trials， which will lay the foundation for the future reaserch on PIs anti-neoplasm therapy.

    [Key words] HIV protease inhibitor； Neoplasm； Endoplasmic reticulum stress； Autophagy

    HIV蛋白酶抑制剂(PIs)的研发是通过抑制病毒的天冬氨酰蛋白前体裂解成其功能形式来阻止HIV病毒颗粒的成熟。自1995年第1种HIV PIs沙奎那韦被FDA批准后，相继有9种其他的HIV PIs被批准，分别为茚地那韦、奈非那韦、利托那韦、洛匹那韦、阿扎那韦、福沙那韦、替拉那韦、安普那韦和地瑞那韦 ......