Field-based rational design of p300 histone acetyltransferase inhibitor and systematic evaluation as an anti-fibrotic agent. Academic Article uri icon

Overview

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.

authors

  • Hwang, Soo Yeon
  • Park, Soo-Yeon
  • Hong, Jung Yeon
  • Lee, Soo Yeon
  • Shin, Jae-Ho
  • Na, Younghwa
  • Sohn, Myung Hyun
  • Yoon, Ho-Geun
  • Kwon, Youngjoo

publication date

  • August 25, 2020

Research

keywords

  • Antifibrinolytic Agents
  • Drug Design
  • E1A-Associated p300 Protein

Identity

Scopus Document Identifier

  • 85090076278

Digital Object Identifier (DOI)

  • 10.1039/d0cc03553j

PubMed ID

  • 32701101

Additional Document Info

volume

  • 56

issue

  • 68