title: Case Study: discovery of inhibitors of the MDM2-p53 protein-protein interaction.
abstract: The p53 protein, a tumor suppressor, is inactivated in many human cancers through mutations or by its interaction with an oncoprotein, MDM2. Blocking the MDM2-p53 protein-protein interaction has the effect of activating wild-type p53 and has been pursued as a novel anticancer strategy. Small-molecule inhibitors of the MDM2-p53 interaction have been discovered through various approaches, and a number of them have progressed into clinical trials for cancer treatment. Here, we describe the methods and techniques used in the discovery of small-molecule inhibitors of the MDM2-p53 interaction.
authors: Comprehensive Cancer Center and Departments of Internal Medicine, University of Michigan, 1500 E. Medical Center Drive, Ann Arbor, MI, 48109, USA.
authors: Liu
authors: L
authors: Liu
authors: Denzil
authors: D
authors: Bernard
authors: Shaomeng
authors: S
authors: Wang
mesh_terms: D003593:Cytoplasm / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D025941:Protein Interaction Mapping / Q000379:methods*; D060066:Protein Interaction Maps / Q000187:drug effects*; D016601:RNA-Binding Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000494:pharmacology; D016159:Tumor Suppressor Protein p53 / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: C433227:CNBP protein, human; D016601:RNA-Binding Proteins; D054852:Small Molecule Libraries; C495901:TP53 protein, human; D016159:Tumor Suppressor Protein p53