Rational design of LEDGINs as first allosteric integrase inhibitors for the treatment of HIV infection.

Abstract

The interaction between lens epithelium-derived growth factor (LEDGF/p75) and HIV-1 integrase (IN) is an attractive target for antiviral development because its inhibition blocks HIV replication. Developing novel small molecules that disrupt the LEDGF/p75-IN interaction constitutes a promising new therapeutic strategy for the treatment of HIV. Here we will highlight recent advances in the design and development of small-molecule inhibitors binding to the LEDGF/p75 binding pocket of IN, referred to as LEDGINs.

• Authors: Belete A Desimmie, Jonas Demeulemeester, Frauke Christ, Zeger Debyser
• Journal: Drug discovery today. Technologies (Drug Discov Today Technol) Vol. 10 Issue 4 Pg. e517-22 (Dec 2013) ISSN: 1740-6749 [Electronic] England
• PMID: 24451643 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Adaptor Proteins, Signal Transducing
• HIV Integrase Inhibitors
• PSIP1 protein, human
• Transcription Factors
• HIV Integrase

Topics

• Adaptor Proteins, Signal Transducing (metabolism)
• Drug Design
• HIV Infections (drug therapy)
• HIV Integrase (metabolism)
• HIV Integrase Inhibitors (therapeutic use)
• HIV-1 (physiology)
• Humans
• Transcription Factors (metabolism)