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Assay Method Information

Assay Name:  E3 Ligase dose-response_384
Description:  Molecular Library Screening Center Network (MLSCN) Penn Center for Molecular Discovery (PCMD) Assay Provider: Brent Stockwell, Columbia University MLSCN Grant: R03MH082369-01 The E3 ligases are involved in regulating other proteins by covalent ligation to the 76 amino acid protein ubiquitin. This post-translational modification can result in altered conformation, altered activity, or degradation of the substrate protein. Thus, E3 ligases are effectors of a major means of post-translational modification of proteins in many species, including mammals. The dipeptide boronic acid bortezomib is a potent proteasome inhibitor, has selective anticancer activity in tumor cells and in mice and was recently approved for clinical use in multiple myeloma. MDM2 E3 ligase is involved in numerous types of human cancer. Selective E3 ligase inhibitors would be preferable as they would be more selective and less toxic. Inhibitors of the MDM2-UBCH5 interaction should disrupt the E3 ligase activity of M
Affinity data for this assay
 

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Last update November 1, 2007
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