1wug

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[[Image:1wug.gif|left|200px]]
[[Image:1wug.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1wug |SIZE=350|CAPTION= <scene name='initialview01'>1wug</scene>
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The line below this paragraph, containing "STRUCTURE_1wug", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=NP1:N-(3-AMINOPROPYL)-4-METHYL-2-NITROBENZENAMINE'>NP1</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= PCAF ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1wug| PDB=1wug | SCENE= }}
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|RELATEDENTRY=[[1b91|1B91]], [[1jm4|1JM4]], [[1wum|1WUM]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1wug FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1wug OCA], [http://www.ebi.ac.uk/pdbsum/1wug PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1wug RCSB]</span>
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}}
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'''complex structure of PCAF bromodomain with small chemical ligand NP1'''
'''complex structure of PCAF bromodomain with small chemical ligand NP1'''
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[[Category: Zeng, L.]]
[[Category: Zeng, L.]]
[[Category: Zhou, M M.]]
[[Category: Zhou, M M.]]
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[[Category: bromodomain]]
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[[Category: Bromodomain]]
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[[Category: chemical ligand]]
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[[Category: Chemical ligand]]
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[[Category: histone-acetyltransferase]]
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[[Category: Histone-acetyltransferase]]
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[[Category: nmr-structure]]
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[[Category: Nmr-structure]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:09:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:41:08 2008''
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Revision as of 11:09, 3 May 2008

Image:1wug.gif

Template:STRUCTURE 1wug

complex structure of PCAF bromodomain with small chemical ligand NP1


Overview

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.

About this Structure

1WUG is a Single protein structure of sequence from Homo sapiens. Full crystallographic 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 Sat May 3 14:09:01 2008

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OCA

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