Wielgos Monica, Yang Eddy S
Department of Radiation Oncology, Comprehensive Cancer Center, School of Medicine, University of Alabama at Birmingham, 1700 6th Avenue South, AL 35294-6832, USA.
Pharm Pat Anal. 2013 Nov;2(6):755-66. doi: 10.4155/ppa.13.53.
Poly (ADP-ribose) polymerases (PARP) are a family of enzymes that play a very important role in preserving the integrity of the genome. Recently, PARP inhibitors have been shown to enhance the therapeutic ratio in cancer patients due to their specific targeting of homologous recombination repair-defective tumors, through a synthetic lethal interaction. Researchers are also presently investigating novel strategies for the treatment of sporadic cancers by combining PARP inhibitors with other DNA-damaging agents. This review will focus on recently patented PARP inhibitors and literature that supports the reported claims presented in these patents. The patents reviewed were categorized into two groups: PARP inhibitors as a single-agent or in combination with other agents for the treatment of various types of cancer. These compounds are currently in clinical trials and, if successful, can greatly impact therapeutic index in cancer therapy.
聚（ADP - 核糖）聚合酶（PARP）是一类在维持基因组完整性方面发挥非常重要作用的酶。最近，PARP抑制剂已被证明可通过合成致死相互作用特异性靶向同源重组修复缺陷的肿瘤，从而提高癌症患者的治疗率。研究人员目前也在研究将PARP抑制剂与其他DNA损伤剂联合使用治疗散发性癌症的新策略。本综述将聚焦于最近获得专利的PARP抑制剂以及支持这些专利中所报道声明的文献。所审查的专利分为两组：PARP抑制剂作为单一药物或与其他药物联合用于治疗各种类型的癌症。这些化合物目前正处于临床试验阶段，如果试验成功，可能会对癌症治疗的治疗指数产生重大影响。
