CRUK and MRC Oxford Institute for Radiation Oncology, University of Oxford, Department of Oncology, Old Road Campus Research Building, OX37DQ Oxford. United Kingdom.
Curr Pharm Des. 2017;23(32):4758-4772. doi: 10.2174/1381612823666170710123602.
Our current understanding of cancer suggests that every tumour has individual features. Approaches to cancer treatment require thorough comprehension of the mechanisms triggering genomic instability and protecting cancer cells from therapeutic treatments. Base excision repair (BER) is a frontline DNA repair system that is responsible for maintaining genome integrity. The BER pathway prevents the occurrence of disease, including cancer, by constantly repairing DNA base lesions and DNA single strand breaks caused by endogenous and exogenous mutagens. BER is an important DNA repair system for cancer cell survival, as it can affect both chemoand radio-resistance of tumours. Variations in BER capacity are likely responsible for a number of cases of sporadic cancer and may also modulate cancer sensitivity and resistance to therapeutic treatments. For these reasons, it is broadly accepted that targeting BER enzymes might be a promising approach to personalised anti-cancer therapy. However, recent advances in both treatment strategies and the comprehension of cancer development call for a better understanding of the consequences of BER inhibition. Indeed, the impact on both the tumour microenvironment and healthy tissues is still unclear. This review will summarise the current status of the approaches exploiting BER targeting, describing the most promising small molecule inhibitors and synthetic lethality strategies, as well as potential limitations of these approaches.
我们目前对癌症的认识表明,每个肿瘤都具有个体特征。癌症治疗方法需要彻底理解触发基因组不稳定性和保护癌细胞免受治疗的机制。碱基切除修复(BER)是负责维持基因组完整性的一线 DNA 修复系统。BER 途径通过不断修复内源性和外源性诱变剂引起的 DNA 碱基损伤和 DNA 单链断裂,防止疾病(包括癌症)的发生。BER 是癌细胞存活的重要 DNA 修复系统,因为它可以影响肿瘤的化疗和放疗耐药性。BER 能力的变化可能是许多散发性癌症的原因,也可能调节癌症对治疗的敏感性和耐药性。基于这些原因,广泛认为靶向 BER 酶可能是一种有前途的个性化抗癌治疗方法。然而,治疗策略和癌症发展的理解的最新进展需要更好地了解 BER 抑制的后果。事实上,BER 抑制对肿瘤微环境和健康组织的影响尚不清楚。本文综述了利用 BER 靶向的方法的现状,描述了最有前途的小分子抑制剂和合成致死性策略,以及这些方法的潜在局限性。