癌症目前是威胁人类健康的最大杀手之一。越来越多的研究证实，SUMO特异性蛋白酶1（SENP1）在各种癌症组织中过表达。因此，靶向SENP1表达可能成为肿瘤治疗的一种新策略。本论文报道了过去10年中有关SENP1抑制剂开发的文献和专利的最新进展。使用SENP1作为关键词，在PubMed、Google学术和ScienceDirect数据库中涵盖了文章和专利。SEN P1-SUMO1的可用复合晶体结构提供了基于结构的药物设计机会，从而导致各种属于不同类别（苯甲酰胺衍生物，萘磺酸，吡啶酮等）的各种异构选择性小分子抑制剂的开发。临床前研究初步显示了这些化合物的潜在优势，对于抗癌药物的开发具有一定的意义。

Cancer is currently one of the biggest killers threatening human health. More and more studies have confirmed that SUMO-specific protease 1 (SENP1) is over-expressed in various cancer tissues. Therefore, targeting SENP1 expression may become a new strategy for tumor therapy.This review reports the latest advances in literature and patents on SENP1 inhibitor development over the past 10 years. With SENP1 as the keyword, articles and patents from PubMed, Google scholar and ScienceDirect databases were covered.The available complex crystal structures of SENP1-SUMO1, afforded structure-based drug design opportunities, which led to the development of various isoform-selective small molecule inhibitors belonging to diverse classes (derivatives of benzamides, naphthalenesulfonic acids, pyridones, and the like). Preclinical studies have initially shown the potential advantages of these compounds, which have certain significance for the development of anticancer drugs.