ArticleCell chemical biology2018
The MALDI-TOF E2/E3 Ligase Assay as Universal Tool for Drug Discovery in the Ubiquitin Pathway.
Article in Cell chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 67 citations in OpenAlex.
- Bendamustine switches TNF receptor superfamily signal from a survival to a death signal in B-cell lymphomas.Blood neoplasia · 2025Article
- Review
- Discovery and characterization of noncanonical E2-conjugating enzymes.Science advances · 2024Article
- Design and high-throughput implementation of MALDI-TOF/MS-based assays for Parkin E3 ligase activity.Cell reports methods · 2024Article
- An expanded lexicon for the ubiquitin code.Nature reviews. Molecular cell biology · 2023Review
- Advances in high-throughput mass spectrometry in drug discovery.EMBO molecular medicine · 2023Review
- MALDI-TOF Mass Spectrometry for interrogating ubiquitin enzymes.Frontiers in molecular biosciences · 2023Article
- A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia.Journal of medicinal chemistry · 2022Article
- The NF-κB Pharmacopeia: Novel Strategies to Subdue an Intractable Target.Biomedicines · 2022Review
- Targeting the ubiquitin system by fragment-based drug discovery.Frontiers in molecular biosciences · 2022Review
- Non-lysine ubiquitylation: Doing things differently.Frontiers in molecular biosciences · 2022Review
- Review
- LUBAC: a new player in polyglucosan body disease.Biochemical Society transactions · 2021Review
- Targeting the Ubiquitin-Proteasome System for Cancer Therapeutics by Small-Molecule Inhibitors.Cancers · 2021Review
- Deubiquitinating enzyme amino acid profiling reveals a class of ubiquitin esterases.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Characterization of Small-Molecule-Induced Changes in Parkinson's-Related Trafficking via the Nedd4 Ubiquitin Signaling Cascade.Cell chemical biology · 2021Article
- Exploration of Aberrant E3 Ligases Implicated in Alzheimer's Disease and Development of Chemical Tools to Modulate Their Function.Frontiers in cellular neuroscience · 2021Review
- High-throughput matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry-based deubiquitylating enzyme assay for drug discovery.Nature protocols · 2020Article
- Robust and facile purification of full-length, untagged human Nedd4 as a recombinant protein from Escherichia coli.Protein expression and purification · 2020Article
- The HECT E3 Ligase E6AP/UBE3A as a Therapeutic Target in Cancer and Neurological Disorders.Cancers · 2020Review
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6 authors at 1 institution in 1 country.
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Abstract
Due to their role in many diseases, enzymes of the ubiquitin system have recently become interesting drug targets. Despite efforts, primary screenings of compound libraries targeting E2 enzymes and E3 ligases have been strongly limited by the lack of robust and fast high-throughput assays. Here we report a label-free high-throughput screening assay for ubiquitin E2 conjugating enzymes and E3 ligases based on MALDI-TOF mass spectrometry. The MALDI-TOF E2/E3 assay allows testing E2 enzymes and E3 ligases for their ubiquitin transfer activity, identifying E2/E3 active pairs, inhibitor potency and specificity and screening compound libraries in vitro without chemical or fluorescent probes. We demonstrate that the MALDI-TOF E2/E3 assay is a universal tool for drug discovery screening in the ubiquitin pathway as it is suitable for working with all E3 ligase families and requires a reduced amount of reagents, compared with standard biochemical assays.
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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.