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 wide range of different ubiquitin ligases.
Davydov
I V
IV
Meso-Scale Discovery, Meso-Scale Diagnostics, LLC, Gaithersburg, MD, USA.
Woods
D
D
Safiran
Y J
YJ
Oberoi
P
P
Fearnhead
H O
HO
Fang
S
S
Jensen
J P
JP
Weissman
A M
AM
Kenten
J H
JH
Vousden
K H
KH
D000818:Animals; D001681:Biological Assay; D020650:Combinatorial Chemistry Techniques; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D009687:Nuclear Proteins / Q000819:agonists / Q000037:antagonists & inhibitors*; D017434:Protein Structure, Tertiary; D011518:Proto-Oncogene Proteins / Q000819:agonists / Q000037:antagonists & inhibitors*; D051736:Proto-Oncogene Proteins c-mdm2; D013050:Spectrometry, Fluorescence; D044767:Ubiquitin-Protein Ligases / Q000037:antagonists & inhibitors*; D014452:Ubiquitins / Q000378:metabolism*
D004791:Enzyme Inhibitors; D009687:Nuclear Proteins; D011518:Proto-Oncogene Proteins; D014452:Ubiquitins; C497206:MDM2 protein, human; C497207:Mdm2 protein, mouse; D051736:Proto-Oncogene Proteins c-mdm2; D044767:Ubiquitin-Protein Ligases