A Left‐Handed Solution to Peptide Inhibition of the p53–MDM2 Interaction
Open accessAbstract
Throwing tumors a left-hook punch: The oncoprotein MDM2 negatively regulates the activity and stability of the tumor suppressor protein p53, and is an important molecular target for anticancer therapy. Mirror-image phage display identified a high-affinity D-peptide ligand of MDM2 (see structure) that could be developed into a potent and protease-resistant p53 activator with potential antitumor activity.
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- Authors
- Liu, M., Pazgier, M., Li, C., Yuan, W., Li, C., & Lu, W.
- Affiliations
- University of Maryland, Baltimore (US)
- Corresponding author
- Lu, Wuyuan
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2010-05-06
- Volume
- 49
- Issue
- 21
- Pages
- 3649-3652
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- PMC
- PMC3359147
- OpenAlex
- W2107850581
- Cited by
- 115
- References
- 31
- Citations by year
- 2026: 4 · 2025: 10 · 2024: 11 · 2023: 6 · 2022: 4 · 2021: 7 · 2020: 6 · 2019: 8 · 2018: 9 · 2017: 9 · 2016: 8 · 2015: 10 · 2014: 6 · 2013: 4 · 2012: 8
- FWCI
- 2.84
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Angewandte Chemie International Edition (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of Allergy and Infectious Diseases (AI 061482, AI-072732, R01AI072732, R01AI061482)
- Topics
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Structure and Dynamics
- Keywords
- p53-MDM2 interaction, MDM2, p53 activation, peptide inhibitors, protease resistance, tumor suppressor, cancer therapy, protein-protein interaction inhibition
- MeSH terms
- Amino Acid Sequence, Enzyme Inhibitors, Humans, Ligands, Molecular Sequence Data, Peptides, Stereoisomerism, Drug Design, Proto-Oncogene Proteins c-mdm2
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