1wum
From Proteopedia
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| - | [[Image:1wum.gif|left|200px]]<br /> | + | [[Image:1wum.gif|left|200px]]<br /><applet load="1wum" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1wum" size=" | + | |
caption="1wum" /> | caption="1wum" /> | ||
'''Complex structure of PCAF bromodomain with small chemical ligand NP2'''<br /> | '''Complex structure of PCAF bromodomain with small chemical ligand NP2'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1WUM is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with NP2 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http:// | + | 1WUM is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=NP2:'>NP2</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1WUM OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Yan, S.]] | [[Category: Yan, S.]] | ||
[[Category: Zeng, L.]] | [[Category: Zeng, L.]] | ||
| - | [[Category: Zhou, M | + | [[Category: Zhou, M M.]] |
[[Category: NP2]] | [[Category: NP2]] | ||
[[Category: bromodomain]] | [[Category: bromodomain]] | ||
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[[Category: np2]] | [[Category: np2]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:48:25 2008'' |
Revision as of 13:48, 21 February 2008
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Complex structure of PCAF bromodomain with small chemical ligand NP2
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
1WUM is a Single protein structure of sequence from Homo sapiens with as ligand. Active as Histone acetyltransferase, with EC number 2.3.1.48 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 Thu Feb 21 15:48:25 2008
Categories: Histone acetyltransferase | Homo sapiens | Single protein | Li, J. | Mujtaba, S. | Muller, M. | Pan, C. | Wang, Z. | Yan, S. | Zeng, L. | Zhou, M M. | NP2 | Bromodomain | Chemical ligand | Histone-acetyltransferase | Nmr-structure | Np1 | Np2
