Recent Advances in Small-Molecule HIV-1 Integrase Inhibitors

Curr Med Chem. 2021;28(24):4910-4934. doi: 10.2174/0929867328666210114124744.

Abstract

HIV-1 integrase catalyzed the insertion of 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 major progress in the development of HIV-1 integrase inhibitors has been made, some thorny problems, such as 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 different conclusion for recent advances in small-molecule inhibitors of HIV-1 integrase.

Keywords: AIDS; HIV-1 integrase inhibitors; allosteric integrase inhibitors.; anti-AIDS drugs; dual inhibitors; integrase.

Publication types

  • Review

MeSH terms

  • DNA, Viral
  • HIV Integrase Inhibitors* / pharmacology
  • HIV Integrase*
  • HIV-1*
  • Humans

Substances

  • DNA, Viral
  • HIV Integrase Inhibitors
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1