Assay for ubiquitin ligase activity: high-throughput screen for inhibitors of HDM2

An assay for the autoubiquitination activity of the E3 ligase HDM2 (Mdm2) was developed and adapted to a high-throughput format to identify inhibitors of this activity. The assay can also be used to measure the activity of other E3s and may be useful in finding both inhibitors and activators of a wi...

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Bibliographic Details
Published inJournal of biomolecular screening Vol. 9; no. 8; pp. 695 - 703
Main Authors Davydov, I V, Woods, D, Safiran, Y J, Oberoi, P, Fearnhead, H O, Fang, S, Jensen, J P, Weissman, A M, Kenten, J H, Vousden, K H
Format Journal Article
LanguageEnglish
Published United States 01.12.2004
Subjects
Animals
Biological Assay
Combinatorial Chemistry Techniques
Drug Evaluation, Preclinical - methods
Enzyme Inhibitors - pharmacology
Humans
Mice
Nuclear Proteins - agonists
Nuclear Proteins - antagonists & inhibitors
Protein Structure, Tertiary
Proto-Oncogene Proteins - agonists
Proto-Oncogene Proteins - antagonists & inhibitors
Proto-Oncogene Proteins c-mdm2
Spectrometry, Fluorescence
Ubiquitin-Protein Ligases - antagonists & inhibitors
Ubiquitins - metabolism
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Summary:An assay for the autoubiquitination activity of the E3 ligase HDM2 (Mdm2) was developed and adapted to a high-throughput format to identify inhibitors of this activity. The assay can also be used to measure the activity of other E3s and may be useful in finding both inhibitors and activators of a wide range of different ubiquitin ligases.
ISSN:1087-0571
2472-5552
DOI:10.1177/1087057104267956