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Synthesis and evaluation of a potent and selective cell-permeable p300 histone acetyltransferase inhibitor.
Autorzy
Rok wydania
2005
Czasopismo
Journal of the American Chemical Society
Numer woluminu
127
Strony
17182-17183
DOI
10.1021/ja0558544
Kolekcja
Język
Angielski
Typ publikacji
Artykuł
This paper describes the first potent and selective p300 histone acetyltransferase (HAT) inhibitor which is effective in live cells. This compound 7 is a coenzyme A analogue conjugated to a cell permeabilizing oligoArg peptide via disulfide linkage. This compound was shown to block cellular histone acetylation and transcription using a p300-sensitive reporter. It should thus be broadly useful for dissecting the role of p300 HAT activity in physiologic and disease states.
Słowa kluczowe
Disulfides, Peptides and proteins, Organic reactions, Assays, Inhibitors
Adres publiczny
https://doi.org/10.1021/ja0558544
Strona internetowa wydawcy
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