Recent Advances of p53-MDM2 Small Molecule Inhibitors (2011-Present)

Author(s): Peng-Cheng Lv, Juan Sun, Hai-Liang Zhu

Journal Name: Current Medicinal Chemistry

Volume 22 , Issue 5 , 2015

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P53 is an important transcriptional factor that plays a pivotal role in different biological process (cell cycle, apoptosis, DNA repair, angiogenesis and cellular metabolism). While p53 binds to the promoter and increases the gene expression of Mdm2, MDM2 protein directly binds to p53 and inhibits its activity. Therefore, inhibitor of p53 and MDM2 has been considered as a potential cancer therapeutic agent due to the critical inhibitory role of MDM2 on p53. Small-molecule inhibitor of p53-MDM2 has been designed to serve as an effective way to treat cancer. Several compounds have moved into different phase of clinical trials based on major advances in the development of small-molecule inhibitors in recent years. Since there are few reviews covering the structure- activity relationship analysis of recent p53-MDM2 inhibitors reported from 2011 to the present time, in this review, attentions are focused on the development of p53-MDM2 inhibitors published from 2011 to the present time.

Keywords: Anticancer drug candidates, Crystal structures, p53-MDM2 inhibitors, Protein-protein interaction, Structure activity relationship analysis, Structure-based drug design, Xenograft model.

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Article Details

Year: 2015
Published on: 12 January, 2015
Page: [618 - 626]
Pages: 9
DOI: 10.2174/0929867322666141128162557
Price: $65

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PDF: 65