Field-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent
- 주제(기타) Chemistry, Multidisciplinary
- 설명문(일반) [Hwang, Soo-Yeon; Kwon, Youngjoo] Ewha Womans Univ, Coll Pharm, Seoul 03760, South Korea; [Hwang, Soo-Yeon; Kwon, Youngjoo] Ewha Womans Univ, Grad Sch Pharmaceut Sci, Seoul 03760, South Korea; [Park, Soo-Yeon; Lee, Soo Yeon; Yoon, Ho-Geun] Yonsei Univ, Severance Med Res Inst, Dept Biochem & Mol Biol, Brain Korea 21 PLUS Project Med Sci,Coll Med, Seoul 03722, South Korea; [Hong, Jung Yeon; Sohn, Myung Hyun] Yonsei Univ, Inst Allergy, Dept Pediat, Brain Korea 21 PLUS Project Med Sci,Coll Med, Seoul 03722, South Korea; [Shin, Jae-Ho; Na, Younghwa] CHA Univ, Coll Pharm, Pochon 11160, South Korea
- 등재 SCIE, SCOPUS
- 발행기관 ROYAL SOC CHEMISTRY
- 발행년도 2020
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000174509
- 본문언어 영어
- Published As http://dx.doi.org/10.1039/d0cc03553j
- PubMed https://pubmed.ncbi.nlm.nih.gov/32701101
초록/요약
(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.
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