Recent advances in small-molecule HIV-1 integrase inhibitors.

HIV-1 integrase catalyzed the insertion of the viral DNA into the genome of human cells in the process of retrotranscription. Integrase is an attractive target for HIV-1 treatment due to the lack of its homologue in human cells and its vital role in HIV-1 replication. Although a major progress about the development of HIV-1 integrase inhibitors has been made, some thorny problems, such as the drug resistance, led to the further study of HIV-1 integrase inhibitors. This review briefly discussed the structure, function and mechanism of catalysis of HIV-1 integrase and made a further conclusion for recent advances in small-molecule inhibitors of HIV-1 integrase.