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  3. Peptidylarginine deiminases 4 as a promising target in drug discovery

Peptidylarginine deiminases 4 as a promising target in drug discovery

  • Eur J Med Chem. 2021 Dec 15:226:113840. doi: 10.1016/j.ejmech.2021.113840.
Chao Yang 1,  Zhen-Zhen Dong 2,  Jing Zhang 1,  Dehong Teng 1,  Xinzhi Luo 1,  Dan Li 3,  Yingtang Zhou 4
Affiliations

Affiliations

  • 1 National Engineering Research Center for Marine Aquaculture, Institute of Innovation & Application, Zhejiang Ocean University, Zhoushan, Zhejiang Province, 316022, China.
  • 2 Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China.
  • 3 State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China. Electronic address: lidan@cdutcm.edu.cn.
  • 4 National Engineering Research Center for Marine Aquaculture, Institute of Innovation & Application, Zhejiang Ocean University, Zhoushan, Zhejiang Province, 316022, China. Electronic address: zhouyingtang@zjou.edu.cn.
PMID: 34520958 DOI: 10.1016/j.ejmech.2021.113840
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.

Keywords

Autoimmune disease; Citrullination; Histone; NETs; PAD4 inhibitor.

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