期刊
MEDCHEMCOMM
卷 4, 期 7, 页码 1109-1113出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3md00091e
关键词
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资金
- BBSRC
- Child Research Appeal Trust
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.
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