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

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.

SUBMITTER: Liu B

PROVIDER: S-EPMC2810552 | biostudies-literature | 2009 Aug

REPOSITORIES: biostudies-literature

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

Liu Bo B Kodadek Thomas T

Journal of medicinal chemistry 20090801 15

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 permeabilit ...[more]

PMID: 19610652

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2023-04-25 | GSE208243 | GEO

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