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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p53, the cellular gatekeeper for growth and division
Levine, A. J. (1997) · Cell · doi:10.1016/s0092-8674(00)81871-1 · Cited by 7,693
Crystal Structure of a p53 Tumor Suppressor-DNA Complex: Understanding Tumorigenic Mutations
Cho, Y., Gorina, S., Jeffrey, P. D., & Pavletich, N. P. (1994) · Science · doi:10.1126/science.8023157 · Cited by 2,559 · cited 1×
“It is particularly noteworthy that PRIMA-1 can reactivate His-175 mutant p53, which has extensive structural defect”
Background
p53: puzzle and paradigm.Preprint
Ko, L. J., & Prives, C. L. (1996) · Genes & Development · doi:10.1101/gad.10.9.1054 · Cited by 2,346
A Matter of Life and Cell Death
Evan, G. I., & Littlewood, T. D. (1998) · Science · doi:10.1126/science.281.5381.1317 · Cited by 1,528
p53 Status and the Efficacy of Cancer Therapy in Vivo
Lowe, S. W., Bodis, S. B., McClatchey, A. I., Remington, L., Ruley, H. E., Fisher, D. E., Housman, D. E., & Jacks, T. (1994) · Science · doi:10.1126/science.7973635 · Cited by 1,468
The complexity of p53 modulation: emerging patterns from divergent signalsPreprint
Giaccia, A. J., & Kastan, M. B. (1998) · Genes & Development · doi:10.1101/gad.12.19.2973 · Cited by 1,315
Disruption of p53 in human cancer cells alters the responses to therapeutic agents.
Bunz, F., Hwang, P. M., Torrance, C., Waldman, T., Zhang, Y., Dillehay, L., Williams, J., Lengauer, C., Kinzler, K. W., & Vogelstein, B. (1999) · Journal of Clinical Investigation · doi:10.1172/jci6863 · Cited by 1,044
Regulation of the specific DNA binding function of p53
Hupp, T. R., Meek, D. W., Midgley, C., & Lane, D. P. (1992) · Cell · doi:10.1016/0092-8674(92)90562-q · Cited by 916
Pharmacological Rescue of Mutant p53 Conformation and Function
Foster, B. A., Coffey, H. A., Morin, M. J., & Rastinejad, F. (1999) · Science · doi:10.1126/science.286.5449.2507 · Cited by 802
Tumor surveillance via the ARF–p53 pathwayPreprint
Sherr, C. J. (1998) · Genes & Development · doi:10.1101/gad.12.19.2984 · Cited by 718

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Proteasome inhibitors suppress the protein expression of mutant p53
Halasi, M., Pandit, B., & Gartel, A. L. (2014) · Cell Cycle · doi:10.4161/15384101.2014.950132 · Cited by 24
DNA-damage sensitizers: Potential new therapeutical tools to improve chemotherapy
Michod, D., & Widmann, C. (2007) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2007.04.003 · Cited by 24
Molecular therapeutics: promise and challenges
Kohn, E. C., Lu, Y., Wang, H., Yu, Q., Yu, S., Hall, H. S., Smith, D. L., Meric‐Bernstam, F., Hortobágyi, G. N., & Mills, G. B. (2004) · Seminars in Oncology · doi:10.1053/j.seminoncol.2004.01.009 · Cited by 24
p53 in breast cancer: mutation and countermeasures
Kumar, S. R. (2007) · Frontiers in bioscience · doi:10.2741/2378 · Cited by 24
Harmonized microarray/mutation scanning analysis of TP53 mutations in undissected colorectal tumors
Favis, R., Huang, J., Gerry, N. P., Culliford, A. T., Paty, P. B., Soussi, T., & Barany, F. (2004) · Human Mutation · doi:10.1002/humu.20069 · Cited by 24
Induction of apoptosis in cancer cells through N-acetyl-l-leucine-modified polyethylenimine-mediated p53 gene delivery
Li, Z., Zhang, L., & Li, Q. (2015) · Colloids and Surfaces B Biointerfaces · doi:10.1016/j.colsurfb.2015.08.024 · Cited by 23
PRIMA-1 increases cisplatin sensitivity in chemoresistant ovarian cancer cells with p53 mutation: a requirement for Akt down-regulation
Kobayashi, N., Abedini, M. R., Sakuragi, N., & Tsang, B. K. (2013) · Journal of Ovarian Research · doi:10.1186/1757-2215-6-7 · Cited by 24
P63 and P73 Activation in Cancers with p53 Mutation
Cai, B., Hsu, Y.-C., Yeh, F.-Y., Lin, Y.-R., Lu, R.-Y., Yu, S.-J., Shaw, J., Wu, M.-H., Tsai, Y.-Z., Lin, Y.-C., et al. (2022) · Biomedicines · doi:10.3390/biomedicines10071490 · Cited by 24
Anticancer Therapeutic Strategies Targeting p53 Aggregation
Ferretti, G. D. S., Quarti, J., dos Santos, G., Rangel, L. P., & Silva, J. L. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms231911023 · Cited by 23
PRIMA-1 cytotoxicity correlates with nucleolar localization and degradation of mutant p53 in breast cancer cells
Russo, D., Ottaggio, L., Penna, I., Foggetti, G., Fronza, G., Inga, A., & Menichini, P. (2010) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2010.10.031 · Cited by 23
PRIMA‐1 induces p53‐mediated apoptosis by upregulating Noxa in esophageal squamous cell carcinoma with TP53 missense mutation
FURUKAWA, H., Makino, T., Yamasaki, M., Tanaka, K., Miyazaki, Y., Takahashi, T., Kurokawa, Y., Nakajima, K., Takiguchi, S., Mori, M., et al. (2017) · Cancer Science · doi:10.1111/cas.13454 · Cited by 23
Re-activation of the p53 pathway inhibits in vivo and in vitro growth of hormone-dependent human breast cancer cells
Liang, Y., Besch-Williford, C. L., Benakanakere, I., & Hyder, S. M. (2007) · International Journal of Oncology · doi:10.3892/ijo.31.4.777 · Cited by 23
Missense mutations in the TP53 DNA-binding domain predict outcomes in patients with advanced oral cavity squamous cell carcinoma
Lapke, N., Lu, Y., Liao, C., Lee, L., Lin, C., Wang, H., Ng, S., Chen, S., & Yen, T. (2016) · Oncotarget · doi:10.18632/oncotarget.9925 · Cited by 23
Exploring the Role of p53 in Radiosensitivity: A Key Player in Cancer Therapy
Al-Arafat, T., Mao, A., Katsube, T., & Wang, B. (2024) · Radiation · doi:10.3390/radiation4040023 · Cited by 23
p53: from understanding its structure to advances in therapeutic targeting
Wang, W., Liu, X., Liu, H., Abolhassani, H., Yan, H., Zhang, H., & Wang, X. (2026) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-025-02549-5 · Cited by 29
Disarming mutant p53 oncogenic function
Girardini, J. E., Marotta, C., & Sal, G. D. (2013) · Pharmacological Research · doi:10.1016/j.phrs.2013.11.003 · Cited by 23
Novel Isatin-based activator of p53 transcriptional functions in tumor cells.
Mirgayazova, R., Khadiullina, R., Mingaleeva, R. N., Chasov, V. V., Gomzikova, M. O., Garanina, E. E., Rizvanov, A. A., & Bulatov, E. (2019) · PubMed Central · doi:10.22099/mbrc.2019.34179.1419 · Cited by 22
BMI1-Inhibitor PTC596 in Combination with MCL1 Inhibitor S63845 or MEK Inhibitor Trametinib in the Treatment of Acute Leukemia
Seipel, K., Kopp, B., Bacher, U., & Pabst, T. (2021) · Cancers · doi:10.3390/cancers13030581 · Cited by 22
Involvement of p53 in insulin-like growth factor binding protein-3 regulation in the breast cancer cell response to DNA damage
Marzec, K. A., Lin, M. Z., Martin, J. L., & Baxter, R. C. (2015) · Oncotarget · doi:10.18632/oncotarget.5612 · Cited by 22
PRIMA-1Met suppresses colorectal cancer independent of p53 by targeting MEK
Lu, T., Zou, Y., Xu, G., Potter, J. A., Taylor, G. L., Duan, Q., Yang, Q., Xiong, H., Qiu, H., Ye, D., et al. (2016) · Oncotarget · doi:10.18632/oncotarget.12940 · Cited by 20
Use of p53 for therapy of human cancer
Almazov, V. P., Кочетков, Д. В., & Chumakov, P. M. (2007) · Molecular Biology · doi:10.1134/s0026893307060015 · Cited by 22
Self-citation
Mutant p53 melanoma cell lines respond differently to CP-31398-induced apoptosis
Ho, C. K., & Li, G. (2005) · British Journal of Dermatology · doi:10.1111/j.1365-2133.2005.06810.x · Cited by 22

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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