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Updated: Dec 28, 2025
14:57
Yeast As a Chassis for Developing Functional Assays to Study Human P53
Published on: August 4, 2019
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Small-molecule modulation of p53 protein-protein interactions
Ave Kuusk1,2, Helen Boyd3, Hongming Chen4
1Laboratory of Chemical Biology, Department of Biomedical Engineering and Institute for Complex Molecular Systems, Eindhoven University of Technology, NL-5600MB Eindhoven, The Netherlands.
Biological Chemistry
|February 13, 2020
Summary
Stabilizing protein-protein interactions (PPIs) with small molecules offers a novel therapeutic strategy for cancer. This review explores stabilizing the 14-3-3σ-p53 complex to enhance tumor suppressor activity.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Protein-protein interactions (PPIs) are crucial in cellular processes.
- The tumor suppressor p53 is frequently altered in human cancers.
- 14-3-3 proteins regulate p53 activity by preventing degradation and enhancing DNA binding.
Purpose of the Study:
- To review the interactions between 14-3-3 proteins and p53.
- To explore the potential of stabilizing the 14-3-3σ-p53 complex.
- To summarize small molecules targeting p53-MDM2 interactions.
Main Methods:
- Literature review of studies on p53-14-3-3 interactions.
- Analysis of small-molecule approaches for PPI modulation.
- Discussion of strategies for stabilizing the 14-3-3σ-p53 complex.
Main Results:
- 14-3-3 proteins positively regulate p53 function.
- Stabilizing PPIs is an underexploited therapeutic strategy.
- Small molecules targeting p53-MDM2 interactions show promise.
Conclusions:
- Modulating PPIs, particularly stabilizing the 14-3-3σ-p53 complex, represents a promising avenue for cancer therapy.
- Further research into PPI stabilization is warranted for drug development.
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