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热激蛋白(HSP)在协助人类细胞正确折叠、激活以及装配方面起关键作用,并影响肿瘤细胞增殖、分化、浸润、血管生成、转移和细胞凋亡. 同时,其还能促使肿瘤细胞刺激免疫系统并产生免疫应答,HSP作为新的肿瘤靶向治疗位点已经进入临床应用. 最新的研究表明,格尔德霉素类似物以及其他新型小分子HSP抑制剂能抑制与肿瘤相关的HSP伴侣蛋白的活性,从而发挥抗肿瘤作用,但仍需进一步的临床试验对其进行评估. 该文就HSP抑制剂在抗肿瘤方面的应用进行综述.“,”Heat shock proteins(HSP) play an essential role in assisting correct folding,activation and assembling of human cells,and affect the proliferation,differentiation,infiltration of tumor cells,angiogenesis, metastasis and apoptosis.They also have the ability to stimulate the immune system and produce an immune response.HSP,as the new targeted sites of anticancer treatment,are under clinical evaluation.The latest evi-dence indicates application of geldanamycin analogues or new synthetics small molecule HSP inhibitors can inhibit the activity of HSP chaperones associated with tumor so as to develop antitumor effect ,which needs to be evaluated by further clinical trials.Here is to make a review of application of HSP inhibitors in antitumor therapy.