Issue 68, 2020
From the journal:

Chemical Communications

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

Soo-Yeon Hwang,‡a   Soo-Yeon Park,‡b   Jung Yeon Hong,‡c   Soo Yeon Lee,b   Jae-Ho Shin,d   Younghwa Na,d   Myung Hyun Sohn,*c   Ho-Geun Yoon*b  and  Youngjoo Kwon ORCID logo *a  

* Corresponding authors

a College of Pharmacy & Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul, Korea
E-mail: ykwon@ewha.ac.kr

b Department of Biochemistry and Molecular Biology, Severance Medical Research Institute, Brain Korea 21 PLUS Project for Medical Sciences, Yonsei University College of Medicine, Seoul, Korea
E-mail: YHGEUN@yuhs.ac

c Department of Pediatrics, Institute of Allergy, Brain Korea 21 PLUS Project for Medical Science, Yonsei University College of Medicine, Seoul, Korea
E-mail: mhsohn@yuhs.ac

d College of Pharmacy, CHA University, Pocheon, Korea
E-mail: yna7315@cha.ac.kr

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.

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

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Article information

DOI
https://doi.org/10.1039/D0CC03553J
Article type
Communication
Submitted
18 May 2020
Accepted
13 Jul 2020
First published
15 Jul 2020

Chem. Commun., 2020,56, 9795-9798

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

S. Hwang, S. Park, J. Y. Hong, S. Y. Lee, J. Shin, Y. Na, M. H. Sohn, H. Yoon and Y. Kwon, Chem. Commun., 2020, 56, 9795 DOI: 10.1039/D0CC03553J

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