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Pharmaceuticals 2016, 9(2), 25; doi:10.3390/ph9020025

Chemical Variations on the p53 Reactivation Theme

Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, 1649-003 Lisboa, Portugal
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Academic Editors: Victor Freitas and Maria Emília de Sousa
Received: 13 April 2016 / Revised: 6 May 2016 / Accepted: 9 May 2016 / Published: 13 May 2016

Abstract

Among the tumor suppressor genes, p53 is one of the most studied. It is widely regarded as the “guardian of the genome”, playing a major role in carcinogenesis. In fact, direct inactivation of the TP53 gene occurs in more than 50% of malignancies, and in tumors that retain wild-type p53 status, its function is usually inactivated by overexpression of negative regulators (e.g., MDM2 and MDMX). Hence, restoring p53 function in cancer cells represents a valuable anticancer approach. In this review, we will present an updated overview of the most relevant small molecules developed to restore p53 function in cancer cells through inhibition of the p53-MDMs interaction, or direct targeting of wild-type p53 or mutated p53. In addition, optimization approaches used for the development of small molecules that have entered clinical trials will be presented. View Full-Text
Keywords: small molecules; MDM2 inhibitors; MDMX inhibitors; p53 activators; p53-MDM2 interaction inhibitors; p53-MDMX interaction inhibitors; mutant p53; wild-type p53 small molecules; MDM2 inhibitors; MDMX inhibitors; p53 activators; p53-MDM2 interaction inhibitors; p53-MDMX interaction inhibitors; mutant p53; wild-type p53
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Ribeiro, C.J.A.; Rodrigues, C.M.P.; Moreira, R.; Santos, M.M.M. Chemical Variations on the p53 Reactivation Theme. Pharmaceuticals 2016, 9, 25.

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