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ChemMedChem. 2011 Jul 4;6(7):1184-91. doi: 10.1002/cmdc.201100071. Epub 2011 Apr 19.

Inhibitors of the interactions between HIV-1 IN and the cofactor LEDGF/p75.

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1
Dipartimento Farmaco-Chimico, Università degli Studi di Messina, Viale Annunziata, 98168 Messina, Italy.

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.

PMID:
21506277
DOI:
10.1002/cmdc.201100071
[Indexed for MEDLINE]
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