In vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2

MDM2 binds the p53 tumor suppressor protein with high affinity and negatively modulates its transcriptional activity and stability. Overexpression of MDM2, found in many human tumors, effectively impairs p53 function. Inhibition of MDM2-p53 interaction can stabilize p53 and may offer a novel strateg...

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Veröffentlicht in:	Science (American Association for the Advancement of Science) 2004-02, Vol.303 (5659), p.844-848
Hauptverfasser:	Vassilev, Lyubomir T., Vu, Binh T., Graves, Bradford, Carvajal, Daisy, Podlaski, Frank, Filipovic, Zoran, Kong, Norman, Kammlott, Ursula, Lukacs, Christine, Klein, Christian, Fotouhi, Nader, Liu, Emily A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Apoptosis Apoptosis - drug effects BASIC BIOLOGICAL SCIENCES Binding Sites Biological and medical sciences BIOLOGICAL PATHWAYS Cancer Cell cycle Cell Cycle - drug effects Cell Division - drug effects Cell growth Cell Line Cell Line, Tumor Cell lines Cell Survival - drug effects CHEMICAL ACTIVATION Crystallization Crystallography, X-Ray Cyclin-Dependent Kinase Inhibitor p21 Cyclins - metabolism Dose-Response Relationship, Drug Enantiomers Feedback (Response) Gene Expression General aspects (metabolism, cell proliferation, established cell line...) Genes, p53 HCT116 cells Heterologous transplantation Human growth Humans Hydrophobic and Hydrophilic Interactions Imidazoles - chemistry Imidazoles - metabolism Imidazoles - pharmacology IN VIVO Inhibition MDM2 protein Medical sciences Mice Mice, Nude Models, Molecular Molecular Weight MOLECULES NATIONAL SYNCHROTRON LIGHT SOURCE Neoplasm Transplantation Neoplasms, Experimental - drug therapy Neoplasms, Experimental - metabolism Neoplasms, Experimental - pathology NIH 3T3 Cells Nuclear Proteins Phosphorylation Physiological aspects Piperazines - chemistry Piperazines - metabolism Piperazines - pharmacology Protein Conformation Proteins Proto-Oncogene Proteins - antagonists & inhibitors Proto-Oncogene Proteins - chemistry Proto-Oncogene Proteins - metabolism Proto-Oncogene Proteins c-mdm2 Rodents Stereoisomerism Transplantation, Heterologous Tumor antigens Tumor cell Tumor Suppressor Protein p53 - metabolism Tumors Tumour antigens Viability
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