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

11 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",

month = sep,

day = "4",

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 - https://www.scopus.com/pages/publications/85090076278

U2 - 10.1039/d0cc03553j

DO - 10.1039/d0cc03553j

M3 - Article

C2 - 32701101

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

Abstract

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