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Selective small molecules blocking HIV-1 Tat and coactivator PCAF association

Development of drug resistance from mutations in the targeted viral proteins leads to continuation of viral production by chronically infected cells, contributing to HIV-mediated immune dysfunction. Targeting a host cell protein essential for viral reproduction, rather than a viral protein, may mini... Full description

Journal Title: Journal of the American Chemical Society 02 March 2005, Vol.127(8), pp.2376-7
Main Author: Zeng, Lei
Other Authors: Li, Jiaming , Muller, Michaela , Yan, Sherry , Mujtaba, Shiraz , Pan, Chongfeng , Wang, Zhiyong , Zhou, Ming-Ming
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: ISSN: 0002-7863 ; PMID: 15724976 Version:1
Link: http://pubmed.gov/15724976
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recordid: medline15724976
title: Selective small molecules blocking HIV-1 Tat and coactivator PCAF association
format: Article
creator:
  • Zeng, Lei
  • Li, Jiaming
  • Muller, Michaela
  • Yan, Sherry
  • Mujtaba, Shiraz
  • Pan, Chongfeng
  • Wang, Zhiyong
  • Zhou, Ming-Ming
subjects:
  • Acetyltransferases -- Antagonists & Inhibitors
  • Anti-HIV Agents -- Pharmacology
  • Cell Cycle Proteins -- Antagonists & Inhibitors
  • Diamines -- Pharmacology
  • Gene Products, Tat -- Antagonists & Inhibitors
  • HIV-1 -- Metabolism
  • Propane -- Analogs & Derivatives
  • Transcription Factors -- Antagonists & Inhibitors
ispartof: Journal of the American Chemical Society, 02 March 2005, Vol.127(8), pp.2376-7
description: Development of drug resistance from mutations in the targeted viral proteins leads to continuation of viral production by chronically infected cells, contributing to HIV-mediated immune dysfunction. Targeting a host cell protein essential for viral reproduction, rather than a viral protein, may minimize the viral drug resistance problem as observed with HIV protease inhibitors. We report here the development of a novel class of N1-aryl-propane-1,3-diamine compounds using a structure-based approach that selectively inhibit the activity of the bromodomain of the human transcriptional co-activator PCAF, of which association with the HIV trans-activator Tat is essential for transcription and replication of the integrated HIV provirus.
language: eng
source:
identifier: ISSN: 0002-7863 ; PMID: 15724976 Version:1
fulltext: no_fulltext
issn:
  • 00027863
  • 0002-7863
url: Link


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titleSelective small molecules blocking HIV-1 Tat and coactivator PCAF association
creatorZeng, Lei ; Li, Jiaming ; Muller, Michaela ; Yan, Sherry ; Mujtaba, Shiraz ; Pan, Chongfeng ; Wang, Zhiyong ; Zhou, Ming-Ming
ispartofJournal of the American Chemical Society, 02 March 2005, Vol.127(8), pp.2376-7
identifierISSN: 0002-7863 ; PMID: 15724976 Version:1
subjectAcetyltransferases -- Antagonists & Inhibitors ; Anti-HIV Agents -- Pharmacology ; Cell Cycle Proteins -- Antagonists & Inhibitors ; Diamines -- Pharmacology ; Gene Products, Tat -- Antagonists & Inhibitors ; HIV-1 -- Metabolism ; Propane -- Analogs & Derivatives ; Transcription Factors -- Antagonists & Inhibitors
descriptionDevelopment of drug resistance from mutations in the targeted viral proteins leads to continuation of viral production by chronically infected cells, contributing to HIV-mediated immune dysfunction. Targeting a host cell protein essential for viral reproduction, rather than a viral protein, may minimize the viral drug resistance problem as observed with HIV protease inhibitors. We report here the development of a novel class of N1-aryl-propane-1,3-diamine compounds using a structure-based approach that selectively inhibit the activity of the bromodomain of the human transcriptional co-activator PCAF, of which association with the HIV trans-activator Tat is essential for transcription and replication of the integrated HIV provirus.
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titleSelective small molecules blocking HIV-1 Tat and coactivator PCAF association
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abstractDevelopment of drug resistance from mutations in the targeted viral proteins leads to continuation of viral production by chronically infected cells, contributing to HIV-mediated immune dysfunction. Targeting a host cell protein essential for viral reproduction, rather than a viral protein, may minimize the viral drug resistance problem as observed with HIV protease inhibitors. We report here the development of a novel class of N1-aryl-propane-1,3-diamine compounds using a structure-based approach that selectively inhibit the activity of the bromodomain of the human transcriptional co-activator PCAF, of which association with the HIV trans-activator Tat is essential for transcription and replication of the integrated HIV provirus.
pmid15724976
doi10.1021/ja044885g
eissn15205126
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date2005-03-02