热休克蛋白90抑制剂Ganetespib治疗实体肿瘤研究进展  

Advances in ganetespib as inhibitor of HSP90 in treatment of solid tumors

作　　者：翟红燕[1] 梁萍[1] 

机构地区：[1]解放军总医院介入超声科,北京100853

出　　处：《解放军医学院学报》2016年第5期506-510,共5页Academic Journal of Chinese PLA Medical School

基　　金：国家自然科学基金项目(81127006;81430039)~~

摘　　要：分子伴侣热休克蛋白90(heat shock protein 90,HSP90)能够通过泛素化途径保护细胞内蛋白质功能,其在肿瘤细胞中呈过表达状态,维持肿瘤细胞生长、增殖、抗凋亡及转移能力。Ganetespib是目前广泛应用于多种肿瘤治疗临床试验的小分子HSP90抑制剂,其单药具有高效能的抗肿瘤活性,联合用药能增强标准化疗或其他靶向治疗疗效,且能同时克服多种肿瘤的耐药机制,本文就Ganetespib在多种人类恶性实体肿瘤治疗中的疗效进行讨论。The heat shock protein 90（HSP90） molecular chaperone protects cellular proteins through the ubiquitin-proteasome pathway. HSP90 is overexpressed in cancer cells to maintain the potential of survival, proliferation, anti-apoptosis and metastasis. This review focuses on the small molecule HSP90 inhibitor-ganetespib, which has been widely used in the clinical trials of cancer treatment. Single-agent HSP90 inhibitor therapy is efficacious. Besides, this inhibitor can potentiate the effects of other molecularly targeted therapy and standard chemotherapy while overcoming drug resistance in some type of tumors. The efficacy of ganetespib in treatment of human solid tumor is reviewed in this article.

关 键 词：热休克蛋白90 Ganetespib 非小细胞肺癌 乳腺癌 恶性黑色素瘤 

分 类 号：R730.5[医药卫生—肿瘤]