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同位素  2011 

抗肿瘤药物PARP-1抑制剂及其放射性核素标记的研究进展

, PP. 45-58

Keywords: 放射性核素,标记,PARP-1抑制剂,抗肿瘤药物

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Abstract:

聚(腺苷二磷酸-核糖)多聚酶(poly(ADP-ribose)polymerase,PARP)是当今癌症治疗的一个新靶点。PARP不但能修复DNA损伤和调控转录,维持细胞内环境与基因组稳定,调节细胞存活和死亡过程,同时也是肿瘤发展和炎症发生过程中的主要转录因子。抑制PARP活性能降低肿瘤细胞的DNA修复功能,增强其对DNA损伤因子的敏感性,从而提高肿瘤放疗和化疗疗效。大量的研究表明,无论单一用药或联合化疗药物,PARP抑制剂都显示了在抗肿瘤治疗领域的潜力。本文综述了PARP-1抑制剂在抗肿瘤方面的研究进展。根据PARP-1抑制剂的发展阶段进行分类,着重介绍几种有代表性的,处于临床试验阶段,且具有潜在临床应用价值的PARP-1抑制剂。正电子发射计算机断层扫描(PositronEmissionTomograph,PET)利用组成人体主要元素的短半衰期核素作示踪剂,在分子水平上,无创伤、定量、动态地观察代谢物或药物在人体内的各种变化,是当代最先进的影像诊断技术,本文也将简单介绍用放射性核素标记PARP-1抑制剂的研究进展。

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