ArticleAngewandte Chemie (International ed. in English)2019
Halogen Bonding Increases the Potency and Isozyme Selectivity of Protein Arginine Deiminase 1 Inhibitors.
Article in Angewandte Chemie (International ed. in English), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
- Bibliometric and visualization analysis of arginine deiminase research from 2006 to 2025: trends, collaboration networks and emerging frontiers.Frontiers in immunology · 2026Article
- Protein citrullination: inhibition, identification and insertion.Philosophical transactions of the Royal Society of London. Series B, Biological sciences · 2023Review
- Development of LB244, an Irreversible STING Antagonist.Journal of the American Chemical Society · 2023Article
- Targeting STING oligomerization with small-molecule inhibitors.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- PAD4-dependent citrullination of nuclear translocation of GSK3β promotes colorectal cancer progression via the degradation of nuclear CDKN1A.Neoplasia (New York, N.Y.) · 2022Article
- A Pilot Study on Peptidylarginine Deiminases and Protein Deimination in Animal Cancers across Vertebrate Species.International journal of molecular sciences · 2022Article
- Exploring Unconventional SAM Analogues To Build Cell-Potent Bisubstrate Inhibitors for Nicotinamide N-Methyltransferase.Angewandte Chemie (International ed. in English) · 2022Article
- Chemical biology of protein citrullination by the protein A arginine deiminases.Current opinion in chemical biology · 2021Review
- Site-specific incorporation of citrulline into proteins in mammalian cells.Nature communications · 2021Article
- Epigenetic Mechanisms and Posttranslational Modifications in Systemic Lupus Erythematosus.International journal of molecular sciences · 2019Review
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Authors and funding
9 authors.
Funding
Abstract
Protein arginine deiminases (PADs) hydrolyze the side chain of arginine to form citrulline. Aberrant PAD activity is associated with rheumatoid arthritis, multiple sclerosis, lupus, and certain cancers. These pathologies established the PADs as therapeutic targets and multiple PAD inhibitors are known. Herein, we describe the first highly potent PAD1-selective inhibitors (1 and 19). Detailed structure-activity relationships indicate that their potency and selectivity is due to the formation of a halogen bond with PAD1. Importantly, these inhibitors inhibit histone H3 citrullination in HEK293TPAD1 cells and mouse zygotes with excellent potency. Based on this scaffold, we also developed a PAD1-selective activity-based probe that shows remarkable cellular efficacy and proteome selectivity. Based on their potency and selectivity we expect that 1 and 19 will be widely used chemical tools to understand PAD1 biology.
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