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

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

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

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.

Original languageEnglish
Pages (from-to)9795-9798
Number of pages4
JournalChemical Communications
Volume56
Issue number68
DOIs
StatePublished - 4 Sep 2020

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