1wug

From Proteopedia

Revision as of 17:48, 12 November 2007

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 with NP1 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

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