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. 2022 Oct 31;23(21):13264. doi: 10.3390/ijms232113264

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© 2022 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).

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PAD inhibitor YW3-56 inhibits histone citrullination and NET formation. (A) YW3-56 is designed based on a structural similarity with the substrate of PAD family peptidylarginine. (B) YW3-56 inhibits mouse PAD4 and human PAD4 activity with IC50 of 2.54 × 10³ nM and 1.19 × 10³ nM. (C) YW3-56 inhibits PAD1, 2, and 3 with IC50 of 1.45 × 10³ nM, 6.34 × 10³ nM, and 53.43 × 10³ nM. (D) Upon calcium ionophore treatment, human peripheral blood neutrophils increased histone citrullination (red) and NET formation (white arrow) detected by immunostaining with a histone H3Cit (Cit2, 8, 17) antibody. DNA dye DAPI staining in blue. NET formation and histone citrullination were decreased upon YW3-56 treatment. (E) Mouse bone marrow neutrophils showed a dramatic increase of histone citrullination after calcium ionophore treatment. YW3-56 treatment blocked the increase of histone citrullination. Scale bars represent 50 μm. hPMN, human polymorphonuclear cell; mPMN, mouse polymorphonuclear cell; PAD, peptidylarginine deiminase. NET, neutrophil extracellular trap.