1wum

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[[Image:1wum.gif|left|200px]]
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[[Image:1wum.png|left|200px]]
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{{STRUCTURE_1wum| PDB=1wum | SCENE= }}
{{STRUCTURE_1wum| PDB=1wum | SCENE= }}
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'''Complex structure of PCAF bromodomain with small chemical ligand NP2'''
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===Complex structure of PCAF bromodomain with small chemical ligand NP2===
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==Overview==
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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.
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The line below this paragraph, {{ABSTRACT_PUBMED_15724976}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15724976 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15724976}}
==About this Structure==
==About this Structure==
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1WUM is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WUM OCA].
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1WUM is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WUM OCA].
==Reference==
==Reference==
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[[Category: Np1]]
[[Category: Np1]]
[[Category: Np2]]
[[Category: Np2]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:09:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 10:30:28 2008''

Revision as of 07:30, 28 July 2008

Image:1wum.png

Template:STRUCTURE 1wum

Complex structure of PCAF bromodomain with small chemical ligand NP2

Template:ABSTRACT PUBMED 15724976

About this Structure

1WUM is a Single protein structure of sequence from Homo sapiens. Full experimental information is available from OCA.

Reference

Selective small molecules blocking HIV-1 Tat and coactivator PCAF association., Zeng L, Li J, Muller M, Yan S, Mujtaba S, Pan C, Wang Z, Zhou MM, J Am Chem Soc. 2005 Mar 2;127(8):2376-7. PMID:15724976

Page seeded by OCA on Mon Jul 28 10:30:28 2008

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