Small‐Molecule Modulation of Protein Lipidation: From Chemical Probes to Therapeutics

Abstract

AbstractProtein lipidation is a widespread modification that regulates protein subcellular localization, structure and function. Dysregulation of protein lipidation has been implicated in various human diseases, including neurological disorders, infectious diseases and cancers. Thus lipid‐modifying enzymes and their substrate proteins are emerging as attractive drug targets. The development of small‐molecule modulators of protein lipidation has remarkably impacted our understanding of lipid‐modification biology and potential therapeutics. In this review, we summarize recent progress in small‐molecule targeting of protein lipidation and highlight therapeutic opportunities.