Conjugation of spermine enhances cellular uptake of the stapled peptide-based inhibitors of p53-Mdm2 interaction
Open accessAbstract
We report the first synthesis of the C-terminally spermine-conjugated stapled peptide-based inhibitors of the p53-Mdm2 interaction. Subsequent biological, biophysical and cellular uptake assays with the spermine-conjugated stapled peptides revealed that spermine conjugation minimally affects biological activity while significantly increases peptide helicity and cellular uptake without apparent cytotoxicity.
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Research works printed but not linked: 1
- [5](a) Bracken C Gulyas J Taylor JW Baum J J Am Chem Soc 1994 116 6431 (b) Phelan CJ Skelton NJ Braisted AC McDowell RS J Am Chem Soc 1997 119 455 (c) Harrison RS Shepherd NE Hoang HN Ruiz-Gomez G Hill TA Driver RW Desai VS Young PR Abbenante G Fairlie DP Proc Natl Acad Sci USA 2010 107 11686 20543141 PMC2900680
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Modulators of Protein–Protein Interactions
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- Authors
- Muppidi, A., Li, X., Chen, J., & Lin, Q.
- Affiliations
- University at Buffalo, State University of New York (US)
- Moffitt Cancer Center (US)
- University of South Florida (US)
- Corresponding author
- Lin, Qing
- Venue
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier BV
- Published
- 2011-12
- Volume
- 21
- Issue
- 24
- Pages
- 7412-7415
- ISSN
- 0960-894X (ISSN-L)
- PMC
- PMC3569039
- OpenAlex
- W2018227338
- Cited by
- 16
- References
- 30
- Citations by year
- 2026: 1 · 2024: 1 · 2023: 1 · 2021: 1 · 2018: 2 · 2016: 1 · 2015: 2 · 2014: 5 · 2013: 1 · 2012: 1
- FWCI
- 0.91
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Bioorganic & Medicinal Chemistry Letters (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- Elsa U. Pardee Foundation
- National Cancer Institute (R01CA109636, CA 109636, CA 118210, P01CA118210)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- stapled peptides, p53-MDM2 interaction, peptide inhibitors, cellular uptake, peptide helicity, p53
- MeSH terms
- Amino Acid Sequence, Cell Survival, Cells, Circular Dichroism, HeLa Cells, Humans, Microscopy, Fluorescence, Peptides, Spermine, Tumor Suppressor Protein p53, Fluorescein, Proto-Oncogene Proteins c-mdm2
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