Altieri Amanda S, Kelman Zvi
Institute for Bioscience and Biotechnology Research, University of Maryland and the National Institute of Standards and Technology, Rockville, MD, United States.
Biomolecular Labeling Laboratory, Institute for Bioscience and Biotechnology Research, National Institute of Standards and Technology, Rockville, MD, United States.
Front Mol Biosci. 2018 Oct 22;5:87. doi: 10.3389/fmolb.2018.00087. eCollection 2018.
Chromosomal DNA replication is achieved by an assembly of multi-protein complexes at the replication fork. DNA sliding clamps play an important role in this assembly and are essential for cell viability. Inhibitors of bacterial (β-clamp) and eukaryal DNA clamps, proliferating cell nuclear antigen (PCNA), have been explored for use as antibacterial and anti-cancer drugs, respectively. Inhibitors for bacterial β-clamps include modified peptides, small molecule inhibitors, natural products, and modified non-steroidal anti-inflammatory drugs. Targeting eukaryotic PCNA sliding clamp in its role in replication can be complicated by undesired effects on healthy cells. Some success has been seen in the design of peptide inhibitors, however, other research has focused on targeting PCNA molecules that are modified in diseased states. These inhibitors that are targeted to PCNA involved in DNA repair can sensitize cancer cells to existing anti-cancer therapeutics, and a DNA aptamer has also been shown to inhibit PCNA. In this review, studies in the use of both bacterial and eukaryotic sliding clamps as therapeutic targets are summarized.
染色体DNA复制是通过在复制叉处组装多蛋白复合物来实现的。DNA滑动夹在这种组装过程中发挥着重要作用,并且对细胞活力至关重要。细菌(β夹)和真核生物DNA夹增殖细胞核抗原(PCNA)的抑制剂,分别已被探索用作抗菌和抗癌药物。细菌β夹的抑制剂包括修饰肽、小分子抑制剂、天然产物和修饰的非甾体抗炎药。针对真核生物PCNA滑动夹在复制中的作用可能会因对健康细胞产生不良影响而变得复杂。然而,在肽抑制剂的设计方面已经取得了一些成功,其他研究则集中在靶向疾病状态下修饰的PCNA分子。这些靶向参与DNA修复的PCNA的抑制剂可以使癌细胞对现有的抗癌疗法敏感,并且一种DNA适配体也已被证明可以抑制PCNA。在这篇综述中,总结了将细菌和真核生物滑动夹用作治疗靶点的研究。