The HIV-1 integrase-LEDGF allosteric inhibitor MUT-A: resistance profile impairment of virus maturation and infectivity but without influence on RNA packaging or virus immunoreactivity

摘要

Background HIV-1 Integrase (IN) interacts with the cellular co-factor LEDGF/p75 and tethers the HIV preintegration complex to the host genome enabling integration. Recently a new class of IN inhibitors was described, the IN-LEDGF allosteric inhibitors (INLAIs). Designed to interfere with the IN-LEDGF interaction during integration, the major impact of these inhibitors was surprisingly found on virus maturation, causing a reverse transcription defect in target cells.