Abstract
The replication cycle of human immunodeficiency virus type 1 (HIV-1) is a complex multistep process that depends on both viral and host cell factors. The nuclear protein lens epithelium-derived growth factor (LEDGF/p75) is a multidomain protein, present in host cells, which plays an important role in the integration process. LEDGF/p75 not only binds HIV-1 integrase (IN) at its IN binding domain (IBD) but also contains several motifs that function in DNA and chromatin binding. The demonstrated importance of the association between IN and LEDGF/p75 in HIV-1 integration suggests the possibility that this protein-protein interaction (PPI) could be exploited as an antiviral target. We describe herein the progress to date in developing inhibitors of this promising target.
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Benzoates / chemistry
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Benzoates / pharmacology
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HIV Integrase / chemistry*
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HIV Integrase / metabolism
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HIV Integrase Inhibitors / chemistry
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HIV Integrase Inhibitors / pharmacology
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HIV-1 / enzymology
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Humans
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Indoles / chemistry
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Indoles / pharmacology
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Intercellular Signaling Peptides and Proteins / chemistry*
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Intercellular Signaling Peptides and Proteins / metabolism
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Peptides / chemistry
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Peptides / pharmacology
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Protein Interaction Domains and Motifs / drug effects
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Quinolines / chemistry
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Quinolines / pharmacology
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Thiazolidinediones / chemistry
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Thiazolidinediones / pharmacology
Substances
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4-((5-bromo-4-((2,4-dioxo-3-(2-oxo-2-phenylethyl)-1,3-thiazolidin-5-ylidene)methyl)-2-ethoxyphenoxy)methyl)benzoic acid
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Benzoates
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HIV Integrase Inhibitors
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Indoles
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Intercellular Signaling Peptides and Proteins
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Peptides
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Quinolines
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Thiazolidinediones
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lens epithelium-derived growth factor
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HIV Integrase
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p31 integrase protein, Human immunodeficiency virus 1