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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