Rational design of LEDGINs as first allosteric integrase inhibitors for the treatment of HIV infection.
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.
Belete A
BA
Desimmie
Jonas
J
Demeulemeester
Frauke
F
Christ
Zeger
Z
Debyser
D048868:Adaptor Proteins, Signal Transducing / Q000378:metabolism*; D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy*; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000627:therapeutic use*; D015497:HIV-1 / Q000502:physiology; D006801:Humans; D014157:Transcription Factors / Q000378:metabolism*
D048868:Adaptor Proteins, Signal Transducing; D019428:HIV Integrase Inhibitors; C504649:PSIP1 protein, human; D014157:Transcription Factors; D019427:HIV Integrase