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

Publication date: December 2013 Source:Drug Discovery Today: Technologies, Volume 10, Issue 4 Author(s): Belete A. Desimmie , Jonas Demeulemeester , Frauke Christ , Zeger Debyser 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.
Source: Drug Discovery Today: Technologies - Category: Drugs & Pharmacology Source Type: research