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Cancers 2017, 9(12), 172; doi:10.3390/cancers9120172

PRIMA-1 and PRIMA-1Met (APR-246): From Mutant/Wild Type p53 Reactivation to Unexpected Mechanisms Underlying Their Potent Anti-Tumor Effect in Combinatorial Therapies

1
Laboratory of Oncology and Experimental Surgery, Institut Jules Bordet, Université Libre de Bruxelles, 1 rue Heger-Bordet, 1000 Brussels, Belgium
2
Clinical Laboratory, Department of Biopathology, Henri Becquerel Centre, 76038 Rouen, France
3
Equipe de Recherche en Oncologie (IRON), Inserm U1245, Rouen University Hospital, 76000 Rouen, France
4
Laboratory of Human Anatomy and Experimental Oncology, Research Institute for Health Sciences and Technology, University of Mons (UMONS), 7000 Mons, Belgium
5
Department of Medicine, Institut Jules Bordet, Université Libre de Bruxelles, 1000 Brussels, Belgium
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 1 November 2017 / Revised: 6 December 2017 / Accepted: 13 December 2017 / Published: 16 December 2017
(This article belongs to the Special Issue p53 Signaling in Cancers)
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Abstract

p53 protects cells from genetic assaults by triggering cell-cycle arrest and apoptosis. Inactivation of p53 pathway is found in the vast majority of human cancers often due to somatic missense mutations in TP53 or to an excessive degradation of the protein. Accordingly, reactivation of p53 appears as a quite promising pharmacological approach and, effectively, several attempts have been made in that sense. The most widely investigated compounds for this purpose are PRIMA-1 (p53 reactivation and induction of massive apoptosis )and PRIMA-1Met (APR-246), that are at an advanced stage of development, with several clinical trials in progress. Based on publications referenced in PubMed since 2002, here we review the reported effects of these compounds on cancer cells, with a specific focus on their ability of p53 reactivation, an overview of their unexpected anti-cancer effects, and a presentation of the investigated drug combinations. View Full-Text
Keywords: p53; p53 reactivation; PRIMA-1; PRIMA-1Met; APR-246; drug combination; cancer p53; p53 reactivation; PRIMA-1; PRIMA-1Met; APR-246; drug combination; cancer
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MDPI and ACS Style

Perdrix, A.; Najem, A.; Saussez, S.; Awada, A.; Journe, F.; Ghanem, G.; Krayem, M. PRIMA-1 and PRIMA-1Met (APR-246): From Mutant/Wild Type p53 Reactivation to Unexpected Mechanisms Underlying Their Potent Anti-Tumor Effect in Combinatorial Therapies. Cancers 2017, 9, 172.

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