Discovery of a structurally novel, drug-like and potent inhibitor of peptidylarginine deiminase

作者:Ferretti Patrizia; Pong Kin U; Vagaska Barbora; Merchant Rohan; Matthews Christopher J; Marson Charles M*
来源:Medchemcomm, 2013, 4(7): 1109-1113.
DOI:10.1039/c3md00091e

摘要

The synthesis and biological properties of a structurally novel, potent and non-peptidic inhibitor of peptidylarginine deiminase are described. The novel drug-like PAD inhibitor contains a 3,5-dihydroimidazol-4-one ring that replaces the acyclic guanidine-binding unit present in arginine residues. This new drug-like PAD inhibitor was effective at 100 nM or below and could have relevance to diseases in which PAD expression is up-regulated, including rheumatoid arthritis, cancer, multiple sclerosis, and neural injury.

  • 出版日期2013-7

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