Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound

By V. Bykov, N. Issaeva, A. Shilov, Monica Hultcrantz, E. Pugacheva, P. Chumakov, J. Bergman, K. Wiman, G. Selivanova. Nature Medicine, 2002

1,113 citations recorded by the source corpus.

Subfields: Biotechnology, Molecular Biology, Oncology

View Paper: https://www.semanticscholar.org/paper/79b552c4d412bdc727b64202f76df24b9e3ce271

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Citations in the corpus

Targeting p53 pathways: mechanisms, structures and advances in therapy (2023, methodology): “After PRIMA1 treatment of SKOV-His-175 cells, a 46% increase in folded p53 protein was observed using the p53 conformation-specific monoclonal antibody PAb1620.(386) Further studies revealed that APR-246 (PRIMA-1, eprenetapopt), a methylated derivative of PRIMA-1,(389) has stronger antitumor activit”
MicroRNAs in development and disease. (2011, background): “In contrast to the above listed antiapoptotic miRNAs, p53 induces apoptosis via upregulation of miR-34a, following its reactivation by PRIMA-1 (150) [a small molecule that restores mutant p53’s transcriptional activity and apoptotic effects in lung cancer cell lines (64)].”
Mutant p53 gain-of-function in cancer. (2010, background): “A number of such molecules have already been identified and described, and shown to exert antitumor effects in experimental mouse models (Bykov et al. 2002; Bykov et al. 2005; Foster et al. 1999; Lambert et al. 2009).”
Mutant p53: one name, many proteins. (2012, background): “Of the small molecules that target mutant p53, the most welladvanced so far has been PRIMA-1 (also known as APR246), which has been shown to reactivate missense mutants of p53 to regain at least some functions of wild-type p53 and thus halt tumor growth and is currently in a phase I clinical trial (”
Role of p53 in Cell Death and Human Cancers (2011, background): “In contrast to wild-type p53, 53BP1 does not interact with cancer-derived p53 mutants (R175H and R273H).”
The first 30 years of p53: growing ever more complex (2009, positive): “In one approach, such molecules were developed to interact with mutant p53 proteins in tumour cells and thereby alter their conformation and restore their functio”