Inhibitors of the Interactions between HIV-1 IN and the Cofactor LEDGF/p75

被引：35

作者：

De Luca, Laura ^{[1
]}

Ferro, Stefania ^{[1
]}

Morreale, Francesca ^{[1
]}

De Grazia, Sara ^{[1
]}

Chimirri, Alba ^{[1
]}

机构：

[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy

来源：

CHEMMEDCHEM | 2011年 / 6卷 / 07期

关键词：

antiviral agents; CHIBA-3053; CX04328; D77; LEDGF/p75; protein-protein interactions; PROTEIN-PROTEIN INTERACTIONS; SMALL-MOLECULE INHIBITORS; INTEGRASE-BINDING DOMAIN; AT-HOOK MOTIFS; COMPLEX-FORMATION; N-METHYLATION; IDENTIFICATION; DESIGN; PEPTIDE; REVEALS;

D O I：

10.1002/cmdc.201100071

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

收藏

页码：1184 / 1191

页数：8

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