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Cited by 285

The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.

A Stapled p53 Helix Overcomes HDMX-Mediated Suppression of p53

Open access
Bernal, Federico, Wade, Mark, Godes, Marina, Davis, Tina N., Whitehead, David G., Kung, Andrew L., Wahl, Geoffrey M., Walensky, Loren D.·2010·Cancer Cell

Abstract

Summary Cancer cells neutralize p53 by deletion, mutation, proteasomal degradation, or sequestration to achieve a pathologic survival advantage. Targeting the E3 ubiquitin ligase HDM2 can lead to a therapeutic surge in p53 levels. However, the efficacy of HDM2 inhibition can be compromised by overexpression of HDMX, an HDM2 homologue that binds and sequesters p53. Here we report that a stapled p53 helix preferentially targets HDMX, blocks the formation of inhibitory p53-HDMX complexes, induces p53-dependent transcriptional upregulation, and thereby overcomes HDMX-mediated cancer resistance in vitro and in vivo. Importantly, our analysis of p53 interaction dynamics provides a blueprint for reactivating the p53 pathway in cancer by matching HDM2, HDMX, or dual inhibitors to the appropriate cellular context.

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Metadata

Authors
Bernal, F., Wade, M., Godes, M., Davis, T. N., Whitehead, D. G., Kung, A. L., Wahl, G. M., & Walensky, L. D.
Venue
Cancer Cell
Publisher
Elsevier BV
Published
2010-11
Volume
18
Issue
5
Pages
411-422
ISSN
1535-6108 (ISSN-L)
OpenAlex
W2171033030
Cited by
285
References
33
FWCI
9.83
Type
journal article
Language
en
Open access
bronze

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CoChat. (2026). Citation check: A Stapled p53 Helix Overcomes HDMX-Mediated Suppression of p53. https://app.cochat.ai/papers/10.1016/j.ccr.2010.10.024
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Bernal, F., Wade, M., Godes, M., Davis, T. N., Whitehead, D. G., Kung, A. L., Wahl, G. M., & Walensky, L. D. (2010). A Stapled p53 Helix Overcomes HDMX-Mediated Suppression of p53. Cancer Cell. https://doi.org/10.1016/j.ccr.2010.10.024

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Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.