ArticleAngewandte Chemie (International ed. in English)2016
Insights Into the Allosteric Inhibition of the SUMO E2 Enzyme Ubc9.
Article in Angewandte Chemie (International ed. in English), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 22 citations in OpenAlex.
- Identification of the first peptide inhibitor of UBE2C enzymatic activity: insights from metadynamics-guided folding and binding studies.Journal of enzyme inhibition and medicinal chemistry · 2026Article
- Honokiol Suppresses Glioma Cell Proliferation by Disrupting SUMO1-YAP1 Conjugation and Promoting YAP1 Proteasomal Degradation.Biomolecules · 2026Article
- Ubc9-mediated SUMOylation of Ninj1 alleviates inflammatory responses in hepatic ischaemia/reperfusion injury.Clinical and translational medicine · 2026Article
- Unsupervised evolution of protein and antibody complexes with a structure-informed language model.Science (New York, N.Y.) · 2024Article
- Inverse folding of protein complexes with a structure-informed language model enables unsupervised antibody evolution.bioRxiv : the preprint server for biology · 2023Article
- Article
- Advancing large-scale production of TEV protease through an innovative NT* tag-based fusion construct.Current research in structural biology · 2023Article
- Identification and optimization of molecular glue compounds that inhibit a noncovalent E2 enzyme-ubiquitin complex.Science advances · 2021Article
- The Molecular Basis of Ubiquitin-Conjugating Enzymes (E2s) as a Potential Target for Cancer Therapy.International journal of molecular sciences · 2021Review
- Current Status of SUMOylation Inhibitors.Current medicinal chemistry · 2021Review
- Targeting SUMOylation inFrontiers in cellular and infection microbiology · 2021Review
- An in vitro Förster resonance energy transfer-based high-throughput screening assay identifies inhibitors of SUMOylation E2 Ubc9.Acta pharmacologica Sinica · 2020Article
- Allosteric mechanism for site-specific ubiquitination of FANCD2.Nature chemical biology · 2020Article
- Expression of SUMO associated proteins in the mouse endometrium is regulated by ovarian hormones throughout the estrous cycle.Experimental and therapeutic medicine · 2020Article
- A Small-Molecule Microarray Approach for the Identification of E2 Enzyme Inhibitors in Ubiquitin-Like Conjugation Pathways.SLAS discovery : advancing life sciences R & D · 2017Article
- Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.Journal of medicinal chemistry · 2017Article
- A dual protease approach for expression and affinity purification of recombinant proteins.Analytical biochemistry · 2016Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 3 countries.
Funding
Abstract
Conjugation of the small ubiquitin-like modifier (SUMO) to protein substrates is an important disease-associated posttranslational modification, although few inhibitors of this process are known. Herein, we report the discovery of an allosteric small-molecule binding site on Ubc9, the sole SUMO E2 enzyme. An X-ray crystallographic screen was used to identify two distinct small-molecule fragments that bind to Ubc9 at a site distal to its catalytic cysteine. These fragments and related compounds inhibit SUMO conjugation in biochemical assays with potencies of 1.9-5.8 mm. Mechanistic and biophysical analyses, coupled with molecular dynamics simulations, point toward ligand-induced rigidification of Ubc9 as a mechanism of inhibition.
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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.