1WUM: Complex structure of PCAF bromodomain with small chemical ligand NP2

Citation:
Abstract
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.
PDB ID: 1WUMDownload
MMDB ID: 34589
PDB Deposition Date: 2004/12/8
Updated in MMDB: 2012/11
Experimental Method:
solution nmr
Source Organism:
Similar Structures:
Molecular Components in 1WUM
Label Count Molecule
Protein (1 molecule)
1
Histone Acetyltransferase Pcaf(Gene symbol: KAT2B)
Molecule annotation
Chemical (1 molecule)
1
1
* Click molecule labels to explore molecular sequence information.

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