Assay for Ubiquitin Ligase Activity: High-Throughput Screen for Inhibitors of HDM2

An assay for the autoubiquitination activity of the E3 ligaseHDM2 (Mdm2) was developed and adapted to a high-throughput format to identify inhibitors of this activity. The assay can also be used tomeasure the activity of other E3s andmay be useful in finding both inhibitors and activators of a wide...

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Veröffentlicht in:	Journal of biomolecular screening 2004-12, Vol.9 (8), p.695-703
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Zusammenfassung:	An assay for the autoubiquitination activity of the E3 ligaseHDM2 (Mdm2) was developed and adapted to a high-throughput format to identify inhibitors of this activity. The assay can also be used tomeasure the activity of other E3s andmay be useful in finding both inhibitors and activators of a wide range of different ubiquitin ligases.
ISSN:	1087-0571 2472-5552 1552-454X
DOI:	10.1177/1087057104267956