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

doi:10.1039/d0cc03553j

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

Department of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

8 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 language	English
Pages (from-to)	9795-9798
Number of pages	4
Journal	Chemical Communications
Volume	56
Issue number	68
DOIs	https://doi.org/10.1039/d0cc03553j
State	Published - 4 Sep 2020

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© 2020 The Royal Society of Chemistry.

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

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.",

author = "Hwang, {Soo Yeon} and Park, {Soo Yeon} and Hong, {Jung Yeon} and Lee, {Soo Yeon} and Shin, {Jae Ho} and Younghwa Na and Sohn, {Myung Hyun} and Yoon, {Ho Geun} and Youngjoo Kwon",

note = "Publisher Copyright: {\textcopyright} 2020 The Royal Society of Chemistry.",

year = "2020",

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doi = "10.1039/d0cc03553j",

language = "English",

volume = "56",

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T1 - Field-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent

AU - Hwang, Soo Yeon

AU - Park, Soo Yeon

AU - Hong, Jung Yeon

AU - Lee, Soo Yeon

AU - Shin, Jae Ho

AU - Na, Younghwa

AU - Sohn, Myung Hyun

AU - Yoon, Ho Geun

AU - Kwon, Youngjoo

PY - 2020/9/4

Y1 - 2020/9/4

N2 - (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.

AB - (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.

UR - http://www.scopus.com/inward/record.url?scp=85090076278&partnerID=8YFLogxK

U2 - 10.1039/d0cc03553j

DO - 10.1039/d0cc03553j

M3 - Article

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AN - SCOPUS:85090076278

SN - 1359-7345

VL - 56

SP - 9795

EP - 9798

JO - Chemical Communications

JF - Chemical Communications

IS - 68

ER -

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

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