Abstract
Recent researches have discovered that MDM2 (murine double minute 2, or HDM2 for the human congener) protein is the main negative regulator of p53, which is an attractive therapeutic target in oncology because its tumor-suppressor activity which can be stimulated to eradicate tumor cells. Inhibiting the p53 – MDM2 interaction is a promising approach for activating p53, because this association is well characterized at the structural and biological levels. A number of drug screening approaches and technologies have been used to identity novel inhibitors of the p53-MDM2 interaction. This review will detail the development history of MDM2 protein and the p53-MDM2 interaction, the major classes of novel small-molecular p53-MDM2 binding inhibitors, key medicinal action with the protein-protein interaction and in vitro or in vivo biological activtiies.
Keywords: MDM2, p53-MDM2 interaction, SAR, small molecular inhibitors, therapeutics/drugs
Current Medicinal Chemistry
Title: Small Molecule Inhibitors of the p53-MDM2
Volume: 15 Issue: 17
Author(s): Chun-Qi Hu and Yong-Zhou Hu
Affiliation:
Keywords: MDM2, p53-MDM2 interaction, SAR, small molecular inhibitors, therapeutics/drugs
Abstract: Recent researches have discovered that MDM2 (murine double minute 2, or HDM2 for the human congener) protein is the main negative regulator of p53, which is an attractive therapeutic target in oncology because its tumor-suppressor activity which can be stimulated to eradicate tumor cells. Inhibiting the p53 – MDM2 interaction is a promising approach for activating p53, because this association is well characterized at the structural and biological levels. A number of drug screening approaches and technologies have been used to identity novel inhibitors of the p53-MDM2 interaction. This review will detail the development history of MDM2 protein and the p53-MDM2 interaction, the major classes of novel small-molecular p53-MDM2 binding inhibitors, key medicinal action with the protein-protein interaction and in vitro or in vivo biological activtiies.
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Cite this article as:
Hu Chun-Qi and Hu Yong-Zhou, Small Molecule Inhibitors of the p53-MDM2, Current Medicinal Chemistry 2008; 15 (17) . https://dx.doi.org/10.2174/092986708784872375
DOI https://dx.doi.org/10.2174/092986708784872375 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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