ArticleJournal of biomolecular screening2012
TR-FRET-based high-throughput screening assay for identification of UBC13 inhibitors.
Article in Journal of biomolecular screening, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
16 citing papers in PubMed, 38 citations in OpenAlex.
- Emerging Role and Potential Therapeutic Application of TRIM Proteins in Cardiovascular Diseases.Biomolecules · 2026Review
- Targeting TRIM Proteins: A Quest towards Drugging an Emerging Protein Class.Chembiochem : a European journal of chemical biology · 2021Review
- A Novel Strategy to Track Lysine-48 Ubiquitination by Fluorescence Resonance Energy Transfer.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Assays and technologies for developing proteolysis targeting chimera degraders.Future medicinal chemistry · 2020Review
- Application of FRET Biosensors in Mechanobiology and Mechanopharmacological Screening.Frontiers in bioengineering and biotechnology · 2020Review
- Label-Free and Real-Time Detection of Protein Ubiquitination with a Biological Nanopore.ACS nano · 2017Article
- Ubc13 haploinsufficiency protects against age-related insulin resistance and high-fat diet-induced obesity.Scientific reports · 2016Article
- Suramin inhibits cullin-RING E3 ubiquitin ligases.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- A novel small-molecule inhibitor of influenza A virus acts by suppressing PA endonuclease activity of the viral polymerase.Scientific reports · 2016Article
- A time-resolved Förster resonance energy transfer assay to measure activity of the deamidase of the prokaryotic ubiquitin-like protein.Analytical biochemistry · 2015Article
- Polypharmacology of small molecules targeting the ubiquitin-proteasome and ubiquitin-like systems.Oncotarget · 2015Review
- Design, development, and validation of a high-throughput drug-screening assay for targeting of human leukemia.Cancer · 2014Article
- Biophysical Detection of Diversity and Bias in GPCR Function.Frontiers in endocrinology · 2014Review
- Article
- How to Target Viral and Bacterial Effector Proteins Interfering with Ubiquitin Signaling.Current topics in microbiology and immunologyReview
- A new FRET-based platform to track substrate ubiquitination by fluorescence.The Journal of biological chemistryArticle
Corrections and comments
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
Abstract
UBC13 is a noncanonical ubiquitin conjugating enzyme (E2) that has been implicated in a variety of cellular signaling processes due to its ability to catalyze formation of lysine 63-linked polyubiquitin chains on various substrates. In particular, UBC13 is required for signaling by a variety of receptors important in immune regulation, making it a candidate target for inflammatory diseases. UBC13 is also critical for double-strand DNA repair and thus a potential radiosensitizer and chemosensitizer target for oncology. The authors developed a high-throughput screening (HTS) assay for UBC13 based on the method of time-resolved fluorescence resonance energy transfer (TR-FRET). The TR-FRET assay combines fluorochrome (Fl)-conjugated ubiquitin (fluorescence acceptor) with terbium (Tb)-conjugated ubiquitin (fluorescence donor), such that the assembly of mixed chains of Fl- and Tb-ubiquitin creates a robust TR-FRET signal. The authors defined conditions for optimized performance of the TR-FRET assay in both 384- and 1536-well formats. Chemical library screens (total 456 865 compounds) were conducted in high-throughput mode using various compound collections, affording superb Z' scores (typically >0.7) and thus validating the performance of the assays. Altogether, the HTS assays described here are suitable for large-scale, automated screening of chemical libraries in search of compounds with inhibitory activity against UBC13.
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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.