Achieving cell penetration with distance-matching cysteine cross-linkers: a facile route to cell-permeable peptide dual inhibitors of Mdm2/Mdmx
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We report the design of bisarylmethylene bromides as a new class of rigid, distance-matching cysteine cross-linkers. By cross-linking a peptide dual inhibitor of Mdm2/Mdmx containing cysteines at i,i+7 positions, dramatic enhancement in cell permeability was achieved, along with increased helicity and biological activity.
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- Authors
- Muppidi, A., Wang, Z., 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
- Chemical Communications
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2011
- Volume
- 47
- Issue
- 33
- Pages
- 9396
- ISSN
- 1359-7345 (ISSN-L)
- 1364-548X
- PMC
- PMC5428881
- OpenAlex
- W2084214674
- Cited by
- 87
- References
- 29
- Citations by year
- 2025: 3 · 2024: 4 · 2023: 6 · 2022: 3 · 2021: 8 · 2020: 5 · 2019: 7 · 2018: 7 · 2017: 6 · 2016: 9 · 2015: 11 · 2014: 13 · 2013: 2 · 2012: 2
- FWCI
- 2.34
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Chemical Communications (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Cancer Institute (CA 118210, P01CA118210)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Health Sciences › Medicine › Oncology › Cancer-related Molecular Pathways
- Keywords
- cell penetration, MDM2, MDMX, cell-permeable peptide, peptide helicity, p53 pathway
- MeSH terms
- Amino Acid Sequence, Cell Membrane Permeability, Cysteine, Enzyme Inhibitors, HeLa Cells, Humans, Nuclear Proteins, Peptides, Proto-Oncogene Proteins, Microscopy, Confocal, Cell Cycle Proteins, Proto-Oncogene Proteins c-mdm2
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