Cited by 88Chemical Synthesis and AnalysisRNA Interference and Gene DeliveryCancer-related Molecular Pathways

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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Muppidi, Avinash, Wang, Zhiyong, Li, Xiaolong, Chen, Jiandong, Lin, Qing·2011·Chemical Communications

Abstract

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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  1. [3](a) Balaram P Curr Opin Struct Biol 1992 2 845 (b) Roy RS Karle IL Raghothama S Balaram P Proc Natl Acad Sci U S A 2004 101 16478 15546995 PMC534522

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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
Published
2011
Volume
47
Issue
33
Pages
9396
ISSN
  • 1359-7345 (ISSN-L)
  • 1364-548X
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
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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