Cancer is a disease portrayed by the uncontrolled growth of irregular cells. Tankyrase, a member of poly(ADP-ribose)polymerase family, mediates Wnt signal transduction and has emerged as a new molecular target for the therapy of different kinds of cancer. Wnt/β-catenin signaling functions significantly in a wide scope of biological events, such as the upkeep of genomic stability, transcriptional control, energy metabolism, and apoptosis. ADP-ribosylation is a reversible posttranslational modification process that regulates several cellular signaling pathways in which transferase enzymes such as mono (ADP-ribosyl) and poly(ADP-ribosyl) transferases move a unit of ADP-ribose moiety from the NAD⁺ co-substrate to specific amino acid side chains and/or potentially ADP-ribose units on target proteins. Recently, inhibition of tankyrase has risen as an appealing strategy for the discovery of novel anticancer drugs. The current review offers an understanding of the ongoing improvements on new lead structures as inhibitors of tankyrase and their activities. A special spotlight is set on the structure-activity relationship, molecular docking, polypharmacology profile, and binding mode at the active center.

癌症是由不规则细胞不受控制的生长所描绘的疾病。Tankyrase是聚（ADP-核糖）聚合酶家族的成员，介导Wnt信号转导，并已成为治疗各种癌症的新分子靶标。Wnt /β-catenin信号传导在广泛的生物学事件中发挥重要作用，例如维持基因组稳定性，转录控制，能量代谢和细胞凋亡。ADP-核糖基化是可逆的翻译后修饰过程，可调节几种细胞信号通路，在该通路中，转移酶（例如单（ADP-核糖基）和聚（ADP-核糖基）转移酶）会将ADP-核糖部分从NAD ^+中移出。在靶蛋白上与特定氨基酸侧链和/或潜在的ADP-核糖单元共底物。近来，对坦科聚合酶的抑制已经作为发现新型抗癌药物的诱人策略而上升。当前的评论提供了对作为tankyrase抑制剂的新铅结构及其活性的持续改进的理解。在活动中心的结构-活性关系，分子对接，多药理学特征和结合方式方面设置了特别的关注点。