科研之友
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摘要
The recovery of cellular tumor antigen p53 functionality has become an attractive target in cancer therapy. The transcriptional activity of p53, mainly regulating cell cycle, DNA damage repair and apoptosis induction, is deregulated in the majority of human tumors. Indeed, the TP53 gene constitutes the most frequent mutated gene in cancer. Furthermore, the upregulation of the main negative controller of p53, oncoprotein Mdm2, has also been well described in different tumor types. Recent advances in the design of small-molecule inhibitors have allowed the development of highly specific protein-protein modulators that block the interaction between p53 and Mdm2. In this review, we aim to highlight the cornerstones of the current knowledge of the Mdm2-p53 interaction and summarize the preclinical and clinical development of Mdm2-p53 inhibitors.
- 出版日期2012-4
