Small-molecule inhibitors targeting small ubiquitin-like modifier pathway for the treatment of cancers and other diseases

SUMOylation is a key post-translational modification that involves the covalent attachment of small ubiquitin-like modifier (SUMO) to the lysine residues of target proteins. The well-balanced SUMOylation is essential for normal cellular behaviors, while disturbance of SUMOylation is associated with various cancers and other diseases. Herein, we summarize the structures and biological functions of proteins involved in the SUMOylation process, their dysregulation in human diseases, and the discovery of small-molecular inhibitors targeting this pathway. In addition, we highlight the emerging trends in this field. [Display omitted] •Targeting SUMOylation has emerged as a promising strategy for the treatment of various diseases.•The structures and functions of proteins involved in SUMOylation are summarized.•Both natural and synthetic small-molecular inhibitors targeting SUMOylation are discussed in details.