Advances in the development of HIV integrase strand transfer inhibitors

Eur J Med Chem. 2021 Dec 5:225:113787. doi: 10.1016/j.ejmech.2021.113787. Epub 2021 Aug 18.

Abstract

HIV-1 integrase (IN) is a key enzyme in viral replication that catalyzes the covalent integration of viral cDNA into the host genome. Currently, five HIV-1 IN strand transfer inhibitors (INSTIs) are approved for clinical use. These drugs represent an important addition to the armamentarium for antiretroviral therapy. This review briefly illustrates the development history of INSTIs. The characteristics of the currently approved INSTIs, as well as their future perspectives, are critically discussed.

Keywords: HIV-1 integrase; Metal chelating; Resistance; Strand transfer inhibitors.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Drug Development*
  • HIV Integrase / metabolism*
  • HIV Integrase Inhibitors / chemical synthesis
  • HIV Integrase Inhibitors / chemistry
  • HIV Integrase Inhibitors / pharmacology*
  • HIV-1 / drug effects*
  • HIV-1 / enzymology
  • Humans
  • Microbial Sensitivity Tests
  • Molecular Structure

Substances

  • Anti-HIV Agents
  • HIV Integrase Inhibitors
  • HIV Integrase