Enhanced nuclear accumulation of pyrrole-imidazole polyamides by incorporation of the tri-arginine vector

The tri-arginine moiety enhanced nuclear accumulation of a 12-ring pyrrole-imidazole polyamide (PIP) without compromising sequence-selectivity and achieved efficient repression of SOX2-downstream genes and HER2 transcription in live cells. This simple vector expands the application of long PIPs in l...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2020-10, Vol.56 (82), p.12371-12374
Hauptverfasser: Hidaka, Takuya, Tsubono, Yutaro, Hashiya, Kaori, Bando, Toshikazu, Pandian, Ganesh N, Sugiyama, Hiroshi
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Sprache:eng
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Zusammenfassung:The tri-arginine moiety enhanced nuclear accumulation of a 12-ring pyrrole-imidazole polyamide (PIP) without compromising sequence-selectivity and achieved efficient repression of SOX2-downstream genes and HER2 transcription in live cells. This simple vector expands the application of long PIPs in live cells by overcoming the compound delivery problems associated with them. The tri-arginine vector enhanced cellular uptake of a 12-ring pyrrole-imidazole polyamide and significantly reduced the concentration of compound required for transcriptional repression of SOX2 .
ISSN:1359-7345
1364-548X
DOI:10.1039/d0cc05158f