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Field-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent
- Title
- Field-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent
- Authors
- Hwang, Soo-Yeon; Park, Soo-Yeon; Hong, Jung Yeon; Lee, Soo Yeon; Shin, Jae-Ho; Na, Younghwa; Sohn, Myung Hyun; Yoon, Ho-Geun; Kwon, Youngjoo
- Ewha Authors
- 권영주
- SCOPUS Author ID
- 권영주
- Issue Date
- 2020
- Journal Title
- CHEMICAL COMMUNICATIONS
- ISSN
- 1359-7345
1364-548X
- Citation
- CHEMICAL COMMUNICATIONS vol. 56, no. 68, pp. 9795 - 9798
- Publisher
- ROYAL SOC CHEMISTRY
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- Abstract
- (E)-3-(3-(4-((3-Carbamoylbenzyl)oxy)-3-iodo-5-methoxyphenyl) acryloyl)benzamide (A6) was found to be a potent p300 inhibitor (IC50= 870 nM) showing a similar binding mode to that of acetyl-CoA, a p300 substrate, and effective anti-fibrotic activity in both TGF-beta 1-stimulated lung fibroblast cells and bleomycin-inducedin vivolung fibrosis mice.
- DOI
- 10.1039/d0cc03553j
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
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