کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8292367 | 1536726 | 2018 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A natural compound, aristoyagonine, is identified as a potent bromodomain inhibitor by mid-throughput screening
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
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چکیده انگلیسی
Bromodomain-containing protein 4 (Brd4) is known to play a key role in tumorigenesis. It binds acetylated histones to regulate the expression of numerous genes. Because of the importance of brd4 in tumorigenesis, much research has been undertaken to develop brd4 inhibitors with therapeutic potential. As a result, various scaffolds for bromodomain inhibitors have been identified. To discover new scaffolds, we performed mid-throughput screening using two different enzyme assays, alpha-screen and ELISA. We found a novel bromodomain inhibitor with a unique scaffold, aristoyagonine. This natural compound showed inhibitory activity in vitro and tumor growth inhibition in a Ty82-xenograft mouse model. In addition, we tested Brd4 inhibitors in gastric cancer cell lines, and found that aristoyagonine exerted cytotoxicity not only in I-BET-762-sensitive cancer cells, but also in I-BET-762-resistant cancer cells. This is the first paper to describe a natural compound as a Brd4 bromodomain inhibitor.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 503, Issue 2, 5 September 2018, Pages 882-887
Journal: Biochemical and Biophysical Research Communications - Volume 503, Issue 2, 5 September 2018, Pages 882-887
نویسندگان
Young Hun Kim, Minsung Kim, Miyoun Yoo, Ji Eun Kim, Heung Kyoung Lee, Jung-Nyoung Heo, Chong Ock Lee, Minjin Yoo, Kwan-Young Jung, Chang-Soo Yun, Sung Woong Moon, Hye Kyung Chang, Chul-Woong Chung, Suhkneung Pyo, Sang Un Choi, Chi Hoon Park,