Issue 4, 2013
From the journal:

MedChemComm

Small organic molecules targeting PCAF bromodomain as potent inhibitors of HIV-1 replication†

Qiang Wang,a   Ruirui Wang,b   Baiqun Zhang,a   Shuai Zhang,a   Yongtang Zheng*b  and  Zhiyong Wang*a  

* Corresponding authors

a Hefei National Laboratory for Physical Sciences at Microscale, CAS Key Laboratory of Soft Matter Chemistry and Department of Chemistry, University of Science and Technology of China, Hefei, Anhui, P. R. China
E-mail: zwang3@ustc.edu.cn
Fax: +86 551-360-3185
Tel: +86 551-360-3185

b Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, P. R. China
E-mail: zhengyt@mail.kiz.ac.cn
Fax: +86 871-5195684
Tel: +86 871-5195684

Abstract

Human p300/CBP associated factor bromodomain (PCAF BRD), a relatively conserved host cell protein, can selectively bind with Tat-AcK50 (tat acetylated lys50). This interaction is essential for the transcription activation of HIV-1 viral gene, therefore PCAF BRD provides a potential targeting protein to inhibit the transcription. We synthesized a series of N1-aryl-propane-1,3-diamine compounds to bind to PCAF BRD. And cellular level anti-HIV-1 assay showed that these small molecules had good inhibitory potency on HIV-1 replication, which was consistent with the molecular assay. Also, it was found that 3-(2-nitrophenoxy) propan-1-amine derivatives had strong bioactivity against HIV-1 replication.

Graphical abstract: Small organic molecules targeting PCAF bromodomain as potent inhibitors of HIV-1 replication

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Article information

DOI
https://doi.org/10.1039/C3MD20376J
Article type
Concise Article
Submitted
20 Sep 2012
Accepted
26 Feb 2013
First published
28 Feb 2013

Med. Chem. Commun., 2013,4, 737-740

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Small organic molecules targeting PCAF bromodomain as potent inhibitors of HIV-1 replication

Q. Wang, R. Wang, B. Zhang, S. Zhang, Y. Zheng and Z. Wang, Med. Chem. Commun., 2013, 4, 737 DOI: 10.1039/C3MD20376J

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