Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9±0.3 μM for PAD4.
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PAD4 (protein arginine deiminase 4) is a transcriptional coregulator that catalyzes the calcium-dependent conversion of specific arginine residues in proteins to citrulline. Cl-amidine is a first-generation irreversible PADs inhibitor with IC50 values of 0.8, 17, 6 and 5.9μM for PAD1, PAD2, PAD3 and PAD4, respectively. Cl-amidine at concentration ranging in 25-200μM dose-dependently inhibited the PAD4-mediated enhancement of the p300GBD-GRIP1 interaction in CV-1 cells post 40-hour treatment. Cl-amidine at concentration of 100μM significantly reduced the level of citrullinated histone H3 induced by A23187 in HL-60 granulocytes. Administration of 40mg/kg Cl-amidine, i.p., exhibited protective effect on CLP (cecal ligation and puncture)-induced lethal septic shock in mice asi it significantly decreased BM and thymus atrophy, restored innate immune cells in BM, increased blood monocytes and blood/liver bacteria clearance and attenuated pro-inflammatory cytokine production.
作用机制
Cl-amidine specifically inactivates PAD4 by modifying Cys645.[1]
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