期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 15, 页码 4604-4612出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm9002999
关键词
-
资金
- National Institutes of Health [P01-DK58398]
- Welch Foundation [I-1299]
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 (beta Da) 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.
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