Abstract:

Gag-Pol protein is one of the important structural proteins of human immunodeficiency virus （HIV）， comprising the basic scaffold proteins and functional enzymes required during the lifecycle of HIV. Currently，the inhibitors targeting different functional domains on Gag-Pol include capsid（CA） inhibitors，protease inhibitors， reverse transcriptase inhibitors， and integrase inhibitors. The CA inhibitors inhibit the maturation of CA or disrupt the assembly of CA，so as to affect the replication of HIV. The primary mechanism of protease inhibitors is to inhibit the protease from cleaving at the cleavage site CA-spacer peptide 1（SP1）. The reverse transcriptase inhibitors block the reverse transcription process of HIV by mimicking the reverse transcription substrates. The integrase inhibitors impact the activity of integrase by targeting the zinc-finger structure at the active center of integrase. This article summarizes the inhibitors targeting HIV Gag-Pol protein and their mechanisms， and reviews the approved dosages and usages of approved patent drugs，so as to provide the references for the future clinical combination therapies and the development of new inhibitors targeting HIV Gag-Pol protein.

Key words: Human immunodeficiency virus, Gag-Pol protein, Protease inhibitor, Reverse transcriptase inhibitor, Integrase inhibitor, Maturation inhibitor