Laboratory of Molecular Pharmacology, Department of Pharmacy, Birla Institute of Technology and Science Pilani, Pilani Campus, Rajasthan, 333031, India.
CSIR-Central Drug Research Institute, Sitapur Road, Sector 10, Jankipuram Extension, Lucknow, Uttar Pradesh, 226031, India.
Drug Discov Today. 2020 Jul;25(7):1253-1261. doi: 10.1016/j.drudis.2020.04.019. Epub 2020 May 1.
Fibrosis is a wound-healing process that results in tissue scarring and organ dysfunction. Several novel mechanisms of fibrogenesis have been discovered recently. In this review, we focus on the role of poly-ADP ribose polymerase (PARP) in major organ fibrosis, such as lungs, heart, liver, and kidneys. PARP is a dynamic enzyme that modulates different cellular proteins by the addition of PAR groups and mediates an array of cellular events in both normal physiological and pathophysiological states. The US Food and Drug Administration (FDA) and European Medicines Agency (EMA) recently approved several PARP inhibitors, such as olaparib, niraparib, talazoparib, and rucaparib, for the treatment of ovarian and germline BRCA-mutant breast cancers. Consequently, repurposing these drugs could provide an opportunity to counter organ fibrosis.
纤维化是一种导致组织瘢痕和器官功能障碍的创伤愈合过程。最近发现了几种新的纤维化发生机制。在这篇综述中，我们重点介绍聚 ADP 核糖聚合酶 (PARP) 在主要器官纤维化（如肺、心脏、肝脏和肾脏）中的作用。PARP 是一种动态酶，通过添加 PAR 基团来调节不同的细胞蛋白，并在正常生理和病理生理状态下介导一系列细胞事件。美国食品和药物管理局 (FDA) 和欧洲药品管理局 (EMA) 最近批准了几种 PARP 抑制剂，如奥拉帕利、尼拉帕利、他拉唑帕利和鲁卡帕利，用于治疗卵巢和种系 BRCA 突变型乳腺癌。因此，重新利用这些药物为对抗器官纤维化提供了机会。
