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Investigation of the relative cellular permeability of DNA-binding pyrrole-imidazole polyamides

Academic Article
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Overview

authors

  • Liu, B.
  • Kodadek, Thomas

publication date

  • August 2009

journal

  • Journal of Medicinal Chemistry  Journal

abstract

  • Pyrrole-imidazole (Py-Im) polyamides are a group of chemicals that are able to bind specifically to DNA sequences in vitro and in mammalian cells. Using a cell based reporter assay, we investigated the size and linker affects on the cellular permeability of polyamides. We found that the conventional beta-alanine-3,3'-diamino-N-methyldipropylamine (betaDa) linker strongly limited the cellular permeability. We discovered that a short ethylene diamine (Et) linker displayed high cellular permeability. With the improved Et linker, we found that the cellular permeability of polyamides was size-dependent.

subject areas

  • DNA
  • Dexamethasone
  • Female
  • HeLa Cells
  • Humans
  • Imidazoles
  • Nylons
  • Permeability
  • Pyrroles
  • Receptors, Glucocorticoid
  • Structure-Activity Relationship
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Identity

PubMed Central ID

  • PMC2810552

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm9002999

PubMed ID

  • 19610652
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Additional Document Info

start page

  • 4604

end page

  • 4612

volume

  • 52

issue

  • 15

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