ArticleACS chemical biology2018
The Development of Benzimidazole-Based Clickable Probes for the Efficient Labeling of Cellular Protein Arginine Deiminases (PADs).
Article in ACS chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Recent Advances in Fluorescent Probes for Imaging Enzyme Activity in NETosis.Chembiochem : a European journal of chemical biology · 2026Review
- Triazole-based STING inhibitors.Bioorganic & medicinal chemistry · 2026Article
- Article
- Nitrofuran-Based STING Inhibitors.ACS omega · 2025Article
- 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
- Current insights into the role of citrullination in thrombosis.Current opinion in chemical biology · 2023Review
- The role of SERPIN citrullination in thrombosis.Cell chemical biology · 2021Article
- Recent Advances about the Applications of Click Reaction in Chemical Proteomics.Molecules (Basel, Switzerland) · 2021Review
- Chemical biology of protein citrullination by the protein A arginine deiminases.Current opinion in chemical biology · 2021Review
- Cu/SiOHeliyon · 2021Article
- RGD Peptide and PAD4 Inhibitor-Loaded Gold Nanorods for Chemo-Photothermal Combined Therapy to Inhibit Tumor Growth, Prevent Lung Metastasis and Improve Biosafety.International journal of nanomedicine · 2021Article
- Click Chemistry in Proteomic Investigations.Cell · 2020Review
- Peptidyl arginine deiminases: detection and functional analysis of protein citrullination.Current opinion in structural biology · 2019Review
- Halogen Bonding Increases the Potency and Isozyme Selectivity of Protein Arginine Deiminase 1 Inhibitors.Angewandte Chemie (International ed. in English) · 2019Article
- Protein Arginine Deiminases (PADs): Biochemistry and Chemical Biology of Protein Citrullination.Accounts of chemical research · 2019Article
- Citrullination Inactivates Nicotinamide- N-methyltransferase.ACS chemical biology · 2018Article
- Photochemical Control of Protein Arginine Deiminase (PAD) Activity.ACS chemical biology · 2018Article
- Development of Activity-Based Proteomic Probes for Protein Citrullination.Current topics in microbiology and immunologyReview
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
Citrullination is the post-translational hydrolysis of peptidyl-arginines to form peptidyl-citrulline, a reaction that is catalyzed by the protein arginine deiminases (PADs), a family of calcium-regulated enzymes. Aberrantly increased protein citrullination is associated with a slew of autoimmune diseases (e.g., rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis) and certain cancers. Given the clear link between increased PAD activity and human disease, the PADs are therapeutically relevant targets. Herein, we report the development of next generation cell permeable and "clickable" probes (BB-Cl-Yne and BB-F-Yne) for covalent labeling of the PADs both in vitro and in cell-based systems. Using advanced chemoproteomic technologies, we also report the off targets of both BB-Cl-Yne and BB-F-Yne. The probes are highly specific for the PADs, with relatively few off targets, especially BB-F-Yne, suggesting the preferential use of the fluoroacetamidine warhead in next generation irreversible PAD inhibitors. Notably, these compounds can be used in a variety of modalities, including the identification of off targets of the parent compounds and as activity-based protein profiling probes in target engagement assays to demonstrate the efficacy of PAD inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.