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PDBsum entry 1wum
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References listed in PDB file
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Key reference
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Title
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Selective small molecules blocking HIV-1 tat and coactivator pcaf association.
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Authors
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L.Zeng,
J.Li,
M.Muller,
S.Yan,
S.Mujtaba,
C.Pan,
Z.Wang,
M.M.Zhou.
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Ref.
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J Am Chem Soc, 2005,
127,
2376-2377.
[DOI no: ]
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PubMed id
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Abstract
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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.
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