ArticleACS chemical biology2018
Photochemical Control of Protein Arginine Deiminase (PAD) Activity.
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 15 papers.
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The trial behind it
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Who cites it
15 citing papers in PubMed, 35 citations in OpenAlex.
- Recent Progress in Regulating the Activity of Enzymes with Photoswitchable Inhibitors.Molecules (Basel, Switzerland) · 2024Review
- Spatiotemporally Precise Optical Manipulation of Intracellular Molecular Activities.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Structure-Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy.Pharmaceutics · 2024Review
- Development of LB244, an Irreversible STING Antagonist.Journal of the American Chemical Society · 2023Article
- Current insights into the role of citrullination in thrombosis.Current opinion in chemical biology · 2023Review
- Real-time precision opto-control of chemical processes in live cells.Nature communications · 2022Article
- Chemical biology of protein citrullination by the protein A arginine deiminases.Current opinion in chemical biology · 2021Review
- Review
- Site-specific incorporation of citrulline into proteins in mammalian cells.Nature communications · 2021Article
- 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
- Progression on Citrullination of Proteins in Gastrointestinal Cancers.Frontiers in oncology · 2019Review
- Thioredoxin Modulates Protein Arginine Deiminase 4 (PAD4)-Catalyzed Citrullination.Frontiers in immunology · 2019Article
- Peptidylarginine Deiminases Post-Translationally Deiminate Prohibitin and Modulate Extracellular Vesicle Release and MicroRNAs in Glioblastoma Multiforme.International journal of molecular sciences · 2018Article
- Citrullination Inactivates Nicotinamide- N-methyltransferase.ACS chemical biology · 2018Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Protein arginine deiminases (PADs) play an important role in the pathogenesis of various diseases, including rheumatoid arthritis, multiple sclerosis, lupus, ulcerative colitis, and breast cancer. Therefore, the development of PAD inhibitors has drawn significant research interest in recent years. Herein, we describe the development of the first photoswitchable PAD inhibitors. These compounds possess an azobenzene photoswitch to optically control PAD activity. Screening of a series of inhibitors structurally similar to BB-Cl-amidine afforded compounds 1 and 2 as the most promising candidates for the light-controlled inhibition of PAD2; the cis isomer of 1 is 10-fold more potent than its trans isomer, whereas the trans isomer of 2 is 45-fold more potent than the corresponding cis isomer. The altered inhibitory potency upon photoisomerization has been confirmed in a competitive activity-based protein profiling (ABPP) assay. Further investigations indicate that the trans isomer of 2 is an irreversible inhibitor, whereas the cis isomer acts as a competitive inhibitor. In cells, the trans isomer of compound 1 is completely inactive, whereas the cis isomer inhibits histone H3-citrullination in a dose-dependent manner. Taken together, 1 serves as the foundation for developing photopharmaceuticals that can be activated at the desired tissue, using light, to treat diseases where PAD activity is dysregulated.
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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.