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Field-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent

Authors
 Soo-Yeon Hwang  ;  Soo-Yeon Park  ;  Jung Yeon Hong  ;  Soo Yeon Lee  ;  Jae-Ho Shin  ;  Younghwa Na  ;  Myung Hyun Sohn  ;  Ho-Geun Yoon  ;  Youngjoo Kwon 
Citation
 CHEMICAL COMMUNICATIONS, Vol.56(68) : 9795-9798, 2020-08 
Journal Title
 CHEMICAL COMMUNICATIONS 
ISSN
 1359-7345 
Issue Date
2020-08
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-β1-stimulated lung fibroblast cells and bleomycin-induced in vivo lung fibrosis mice.
Full Text
https://pubs.rsc.org/en/content/articlelanding/2020/CC/D0CC03553J#!divAbstract
DOI
10.1039/d0cc03553j
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Biochemistry and Molecular Biology (생화학-분자생물학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Pediatrics (소아과학교실) > 1. Journal Papers
1. College of Medicine (의과대학) > Yonsei Biomedical Research Center (연세의생명연구원) > 1. Journal Papers
Yonsei Authors
Park, Soo Yeon(박수연) ORCID logo https://orcid.org/0000-0003-3743-9554
Sohn, Myung Hyun(손명현) ORCID logo https://orcid.org/0000-0002-2478-487X
Yoon, Ho Geun(윤호근) ORCID logo https://orcid.org/0000-0003-2718-3372
Hong, Jung Yeon(홍정연) ORCID logo https://orcid.org/0000-0003-0406-9956
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/180057
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