Abstract
Lens epithelium-derived growth factor (LEDGF/p75) plays an essential role in the HIV-1 replication. It acts by tethering integrase (IN) into the host cellular chromatin. Due to its significance of the IN-LEDGF/p75 interaction affords a novel therapeutic approach for the design of new classes of antiretroviral agents. To date, many small molecules have been found to be the inhibitors of INLEDGF/ p75 interaction. This review summarizes recent advances in the development of potential structure-based IN-LEDGF/p75 interaction inhibitors. The work will be helpful to shed light on the antiretroviral drug development pipeline in the next future.
Keywords: HIV-1; integrase; LEDGF/p75; integrase-LEDGF/p75 interaction inhibitors .
Mini-Reviews in Medicinal Chemistry
Title:Recent Advances in the Development of Small-Molecular Inhibitors Target HIV Integrase-LEDGF/p75 Interaction
Volume: 15 Issue: 14
Author(s): Yu Zhao and Zaigang Luo
Affiliation:
Keywords: HIV-1; integrase; LEDGF/p75; integrase-LEDGF/p75 interaction inhibitors .
Abstract: Lens epithelium-derived growth factor (LEDGF/p75) plays an essential role in the HIV-1 replication. It acts by tethering integrase (IN) into the host cellular chromatin. Due to its significance of the IN-LEDGF/p75 interaction affords a novel therapeutic approach for the design of new classes of antiretroviral agents. To date, many small molecules have been found to be the inhibitors of INLEDGF/ p75 interaction. This review summarizes recent advances in the development of potential structure-based IN-LEDGF/p75 interaction inhibitors. The work will be helpful to shed light on the antiretroviral drug development pipeline in the next future.
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Cite this article as:
Zhao Yu and Luo Zaigang, Recent Advances in the Development of Small-Molecular Inhibitors Target HIV Integrase-LEDGF/p75 Interaction, Mini-Reviews in Medicinal Chemistry 2015; 15 (14) . https://dx.doi.org/10.2174/1389557515666150709114917
DOI https://dx.doi.org/10.2174/1389557515666150709114917 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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