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ID: ALA5034024

Journal: Eur J Med Chem

Title: Peptidylarginine deiminases 4 as a promising target in drug discovery.

Authors: Yang C, Dong ZZ, Zhang J, Teng D, Luo X, Li D, Zhou Y.

Abstract: Peptidylarginine deaminase 4 (PAD4) is a crucial post-translational modifying enzyme catalyzing the conversion of arginine into citrulline residues, and mediating the formation of neutrophil extracellular traps (NETs). PAD4 plays a vital role in the occurrence and development of cardiovascular diseases, autoimmune diseases, and various tumors. Therefore, PAD4 is considered as a promising drug target for disease diagnosis and treatment. More and more efforts are devoted to developing highly efficient and selective PAD4 inhibitors via high-throughput screening, structure-based drug design and structure-activity relationship study. This article outlined the physiological and pathological functions of PAD4, and corresponding representative small molecule inhibitors reported in recent years.

CiteXplore: 34520958

DOI: 10.1016/j.ejmech.2021.113840