ArticleProceedings of the National Academy of Sciences of the United States of America2016
Suramin inhibits cullin-RING E3 ubiquitin ligases.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 53 citations in OpenAlex.
- Repurposing drug screen for the identification of helicase inhibitors from viruses of pandemic concern.SLAS discovery : advancing life sciences R & D · 2026Article
- Suramin Interactions Across Biological Systems: From Molecular Targets to Therapeutic Implications.Biomolecules · 2026Review
- LOPAC library screening identifies suramin as a TRIM21 binder with a unique binding mode revealed by crystal structure.Acta crystallographica. Section F, Structural biology communications · 2025Article
- Binding to the Other Side: The AT-Hook DNA-Binding Domain Allows Nuclear Factors to Exploit the DNA Minor Groove.International journal of molecular sciences · 2024Review
- Coronaviruses SARS-CoV, MERS-CoV, and SARS-CoV-2 helicase inhibitors: a systematic review ofJournal of virus eradication · 2023Review
- An update on inhibitors targeting RNA-dependent RNA polymerase for COVID-19 treatment: Promises and challenges.Biochemical pharmacology · 2022Review
- Genetic and Epigenetic Mechanisms Deregulate the CRL2Frontiers in genetics · 2022Article
- Discovery of a small molecule inhibitor of cullin neddylation that triggers ER stress to induce autophagy.Acta pharmaceutica Sinica. B · 2021Article
- Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of nsp13 helicase.The Biochemical journal · 2021Article
- Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of nsp12/7/8 RNA-dependent RNA polymerase.The Biochemical journal · 2021Article
- Improvement of Oral Bioavailability of Pyrazolo-Pyridone Inhibitors of the Interaction of DCN1/2 and UBE2M.Journal of medicinal chemistry · 2021Article
- Inhibitors of cullin-RING E3 ubiquitin ligase 4 with antitumor potential.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Targeting Protein Neddylation to Inactivate Cullin-RING Ligases by Gossypol: A Lucky Hit or a New Start?Drug design, development and therapy · 2021Review
- Repurposing old drugs as new inhibitors of the ubiquitin-proteasome pathway for cancer treatment.Seminars in cancer biology · 2021Review
- A Novel Strategy to Track Lysine-48 Ubiquitination by Fluorescence Resonance Energy Transfer.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Targeting Cullin-RING E3 Ubiquitin Ligase 4 by Small Molecule Modulators.Journal of cellular signaling · 2021Article
- Identification of HMGA2 inhibitors by AlphaScreen-based ultra-high-throughput screening assays.Scientific reports · 2020Article
- The Effect of Dysfunctional Ubiquitin Enzymes in the Pathogenesis of Most Common Diseases.International journal of molecular sciences · 2020Review
- Suramin and NF449 are IP5K inhibitors that disrupt inositol hexakisphosphate-mediated regulation of cullin-RING ligase and sensitize cancer cells to MLN4924/pevonedistat.The Journal of biological chemistry · 2020Article
- Suramin exposure alters cellular metabolism and mitochondrial energy production in African trypanosomes.The Journal of biological chemistry · 2020Article
Corrections and comments
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Authors and funding
17 authors at 8 institutions in 3 countries.
Funding
Abstract
Cullin-RING E3 ubiquitin ligases (CRL) control a myriad of biological processes by directing numerous protein substrates for proteasomal degradation. Key to CRL activity is the recruitment of the E2 ubiquitin-conjugating enzyme Cdc34 through electrostatic interactions between E3's cullin conserved basic canyon and the acidic C terminus of the E2 enzyme. This report demonstrates that a small-molecule compound, suramin, can inhibit CRL activity by disrupting its ability to recruit Cdc34. Suramin, an antitrypansomal drug that also possesses antitumor activity, was identified here through a fluorescence-based high-throughput screen as an inhibitor of ubiquitination. Suramin was shown to target cullin 1's conserved basic canyon and to block its binding to Cdc34. Suramin inhibits the activity of a variety of CRL complexes containing cullin 2, 3, and 4A. When introduced into cells, suramin induced accumulation of CRL substrates. These observations help develop a strategy of regulating ubiquitination by targeting an E2-E3 interface through small-molecule modulators.
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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.