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Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases.1 GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 (Item No. 17488) and GSK199 (Item No. 17489).2 It does not inhibit PAD4 nor does it prevent the citrullination of PAD4 target proteins or the formation of neutrophil extracellular traps in mouse or human neutrophils (IC50s > 100 µM).2 See the Structural Genomics Consortium (SGC) website for more information on both GSK484 and GSK106.
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1. Protein arginine deiminase 4 (PAD4): Current understanding and future therapeutic potential. Curr. Opin. Drug Discov. Devel. 12(5), 616-627 (2009).
2. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat. Chem. Biol. 11(3), 189-191 (2015).