1wum | pdb_00001wum
Complex structure of PCAF bromodomain with small chemical ligand NP2
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| 1wum | |||||||||||||
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| Ligands: | NP2 | ||||||||||||
| Activity: | Histone acetyltransferase, with EC number 2.3.1.48 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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. 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
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