A Genetically Encoded FRET Probe to Detect Intranucleosomal Histone H3K9 or H3K14 Acetylation Using BRD4, a BET Family Member

Shiho Nakaoka, Kazuki Sasaki, Akihiro Ito, Yoichi Nakao, Minoru Yoshida

研究成果: Article査読

16 被引用数 (Scopus)

抄録

Acetylation is a well-characterized histone modification, which plays important roles in controlling epigenetic gene expression, and its malfunction is tightly associated with cancer. By taking advantage of the specific binding of BRD4 to acetylated lysine residues, we developed a FRET-based probe for visualizing histone H3 acetylation in living cells. BRD4, a protein known to be involved in acute myeloid leukemia and nuclear protein in testis midline carcinoma, recognizes the acetylation of histone H3 via its bromodomains. The probe exhibited a significant change in FRET signaling that was dependent on histone H3 acetylation. Mutagenesis studies revealed that an increase in the emission ratio reflected the acetylation of either K9 or K14 of histone H3 within the probe. Since BRD4 has increasingly drawn attention as a new anticancer drug target, we demonstrated that the developed fluorescent probe will also serve as a powerful tool to evaluate BRD4 inhibitors in living cells.

本文言語English
ページ(範囲)729-733
ページ数5
ジャーナルACS Chemical Biology
11
3
DOI
出版ステータスPublished - 2016 3 18

ASJC Scopus subject areas

  • 生化学
  • 分子医療

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