Zahmatkesh Mona Haddad, Hosseinimehr Seyed Jalal, Mahdiuni Hamid
Department of Radiopharmacy, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.
Mini Rev Med Chem. 2014;14(10):812-8.
Ionizing radiation is the more effective therapy to reduce tumor growth through damaging the DNA of cells. In response to DNA damage, cells activate the checkpoint kinases such as CHK2, which signal to initiate repair processes and cell-cycle arrest, until the damaged DNA is repaired. At present, the development of CHK2 inhibitors has provided an interesting strategy for the treatment of cancer by introducing new radiation modifier agents. CHK2 inhibitors can contribute for the improvement of cancer therapy through sensitizing cancerous cells and radioprotection of normal cells against ionizing radiation. This review describes and discusses the most recent inhibitors of CHK2 and presents an evaluation of chemical structures and biological activities. As well as their role in cell growth during exposure to ionizing radiation.
电离辐射是通过破坏细胞DNA来减少肿瘤生长的更有效疗法。响应DNA损伤,细胞会激活诸如CHK2之类的检查点激酶,这些激酶会发出信号启动修复过程并使细胞周期停滞,直到受损的DNA得到修复。目前,CHK2抑制剂的开发通过引入新的辐射修饰剂为癌症治疗提供了一种有趣的策略。CHK2抑制剂可通过使癌细胞敏感化以及对正常细胞进行电离辐射防护来促进癌症治疗的改善。本综述描述并讨论了CHK2的最新抑制剂,并对化学结构和生物活性进行了评估。以及它们在暴露于电离辐射期间在细胞生长中的作用。