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

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Liu B, Kodadek T

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

J Med Chem. 2009 Aug 13;52(15):4604-12. doi: 10.1021/jm9002999.

PubMed ID
19610652 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DexamethasoneGlucocorticoid receptorIC 50 (nM)5N/AN/ADetails