title: Comparative biochemical analysis of HIV-1 subtype B and C integrase enzymes.
abstract: BACKGROUND
  Integrase inhibitors are currently being incorporated into highly active antiretroviral therapy (HAART). Due to high HIV variability, integrase inhibitor efficacy must be evaluated against a range of integrase enzymes from different subtypes.
  
  
  METHODS
  This study compares the enzymatic activities of HIV-1 integrase from subtypes B and C as well as susceptibility to various integrase inhibitors in vitro. The catalytic activities of both enzymes were analyzed in regard to each of 3' processing and strand transfer activities both in the presence and absence of the integrase inhibitors raltegravir (RAL), elvitegravir (EVG), and MK-2048.
  
  
  RESULTS
  Our results show that integrase function is similar with enzymes of either subtype and that the various integrase strand transfer inhibitors (INSTIs) that were employed possessed similar inhibitory activity against both enzymes.
  
  
  CONCLUSIONS
  This suggests that the use of integrase inhibitors against HIV-1 subtype C will result in comparable outcomes to those obtained against subtype B infections.
authors.affiliation: McGill University AIDS Centre, Lady Davis Institute-Jewish General Hospital, Montreal, Quebec, Canada. tamara.bar-magen@mail.mcgill.ca
authors.forename: Tamara
authors.initials: T
authors.lastname: Bar-Magen
authors.forename: Richard D
authors.initials: RD
authors.lastname: Sloan
authors.forename: Verena H
authors.initials: VH
authors.lastname: Faltenbacher
authors.forename: Daniel A
authors.initials: DA
authors.lastname: Donahue
authors.forename: Björn D
authors.initials: BD
authors.lastname: Kuhl
authors.forename: Maureen
authors.initials: M
authors.lastname: Oliveira
authors.forename: Hongtao
authors.initials: H
authors.lastname: Xu
authors.forename: Mark A
authors.initials: MA
authors.lastname: Wainberg
mesh_terms: D004279:DNA, Viral / Q000378:metabolism; D005838:Genotype; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000494:pharmacology*; D015497:HIV-1 / Q000145:classification / Q000201:enzymology* / Q000235:genetics; D020128:Inhibitory Concentration 50; D011760:Pyrrolidinones / Q000494:pharmacology; D015363:Quinolones / Q000494:pharmacology; D000068898:Raltegravir Potassium
chemical_list: D004279:DNA, Viral; D019428:HIV Integrase Inhibitors; D011760:Pyrrolidinones; D015363:Quinolones; D000068898:Raltegravir Potassium; C509700:elvitegravir; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1