Targeting MDM2 by the small molecule RITA: towards the development of new multi-target drugs against cancer |
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Authors: | Email author" target="_blank">L?Michel?Espinoza-FonsecaEmail author |
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Institution: | (1) Department of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, Minneapolis 55455, MN, USA |
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Abstract: | Background The use of low-molecular-weight, non-peptidic molecules that disrupt the interaction between the p53 tumor suppressor and
its negative regulator MDM2 has provided a promising alternative for the treatment of different types of cancer. Among these
compounds, RITA (reactivation of p53 and induction of tumor cell apoptosis) has been shown to be effective in the selective
induction of apoptosis, and this effect is due to its binding to the p53 tumor suppressor. Since biological systems are highly
dynamic and MDM2 may bind to different regions of p53, new alternatives should be explored. On this basis, the computational
"blind docking" approach was employed in this study to see whether RITA would bind to MDM2. |
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