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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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The initial evaluation of non-peptidic small-molecule HDM2 inhibitors based on p53-HDM2 complex structure.

Peptidic Mouse Double Minute (MDM2) inhibitors have been demonstrated to effectively inhibit the interaction between p53 and MDM2, thus providing a therapeutic strategy for some tumors. However, there is no report on non-peptidic inhibitors. In this study non-peptidic HDM2 (the human homologue of MDM2) inhibitors were obtained by computer-aided design and subsequently synthesized by chemical method. Bio-evaluation showed that some of these inhibitors have affinity with HDM2, and can cause death of some tumor cells which express wild-type p53. Cellular assays showed that one of these compounds, syc-7, can activate the p53 pathway in some of these tumor cell lines, and further induce apoptosis. The results suggest that developing non-peptidic small-molecule HDM2 inhibitors is a promising way for new antitumor drug discovery.[1]

References

  1. The initial evaluation of non-peptidic small-molecule HDM2 inhibitors based on p53-HDM2 complex structure. Zhao, J., Wang, M., Chen, J., Luo, A., Wang, X., Wu, M., Yin, D., Liu, Z. Cancer Lett. (2002) [Pubmed]
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