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ABSTRACT Introduction 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. Areas covered 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. Expert opinion 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.