Cited by 1,067Cancer-related Molecular PathwaysCell death mechanisms and regulationPI3K/AKT/mTOR signaling in cancer

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

Bykov, Vladimir J.N., Issaeva, Natalia, Shilov, Alexandre, Hultcrantz, Monica, Pugacheva, Elena, Chumakov, Peter, Bergman, Jan, Wiman, Klas G., Selivanova, Galina·2002·Nature Medicine

DOI 10.1038/nm0302-282

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Abstract

The tumor suppressor p53 inhibits tumor growth primarily through its ability to induce apoptosis. Mutations in p53 occur in at least 50% of human tumors. We hypothesized that reactivation of mutant p53 in such tumors should trigger massive apoptosis and eliminate the tumor cells. To test this, we screened a library of low-molecular-weight compounds in order to identify compounds that can restore wild-type function to mutant p53. We found one compound capable of inducing apoptosis in human tumor cells through restoration of the transcriptional transactivation function to mutant p53. This molecule, named PRIMA-1, restored sequence-specific DNA binding and the active conformation to mutant p53 proteins in vitro and in living cells. PRIMA-1 rescued both DNA contact and structural p53 mutants. In vivo studies in mice revealed an antitumor effect with no apparent toxicity. This molecule may serve as a lead compound for the development of anticancer drugs targeting mutant p53.

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Authors: Bykov, V. J. N., Issaeva, N., Shilov, A., Hultcrantz, M., Pugacheva, E., Chumakov, P., Bergman, J., Wiman, K. G., & Selivanova, G.
Affiliations: Karolinska University Hospital (SE)
Engelhardt Institute of Molecular Biology (RU)
Karolinska Institutet (SE)
Corresponding author: Wiman, Klas G.
ORCID: Bykov, Vladimir J.N.
Issaeva, Natalia
Hultcrantz, Monica
Pugacheva, Elena
Chumakov, Peter
Bergman, Jan
Wiman, Klas G.
Selivanova, Galina
Venue: Nature Medicine
Publisher: Springer Science and Business Media LLC
Published: 2002-03
Volume: 8
Issue: 3
Pages: 282-288
ISSN: 1078-8956 (ISSN-L)
1546-170X
DOI: 10.1038/nm0302-282
OpenAlex: W2092902276
Cited by: 1,067
References: 32
Citations by year: 2026: 22 · 2025: 29 · 2024: 42 · 2023: 51 · 2022: 49 · 2021: 58 · 2020: 55 · 2019: 53 · 2018: 51 · 2017: 34 · 2016: 53 · 2015: 42 · 2014: 51 · 2013: 38 · 2012: 37
FWCI: 18.33
Type: journal article
Language: en
Open access: closed
Licence: www.springer.com/tdm (tdm)
Locations: Nature Medicine (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Cell death mechanisms and regulation
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › PI3K/AKT/mTOR signaling in cancer
Keywords: mutant p53, PRIMA-1, p53 reactivation, tumor suppressor function, apoptosis, transcriptional activation, small molecules, anticancer drug development, DNA binding, p53 conformation, anticancer activity
MeSH terms: Animals, Antineoplastic Agents, Aza Compounds, Cell Separation, Flow Cytometry, Humans, Molecular Weight, Mutation, Neoplasms, Organic Chemicals, Protein Conformation, Transplantation, Heterologous, Tumor Cells, Cultured, Molecular Structure, Transcriptional Activation, Tumor Suppressor Protein p53, Apoptosis, Genes, Reporter, Bridged Bicyclo Compounds, Heterocyclic, In Situ Nick-End Labeling, Mice

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

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