Mutations in the thumb-connection and RNase H domain of HIV type-1 reverse transcriptase of antiretroviral treatment-experienced patients

Antivir Ther. 2009;14(2):231-9.

Abstract

Background: Antiretroviral therapy that targets HIV type-1 (HIV-1) reverse transcriptase (RT) can be linked to mutations in the thumb-connection (amino acids [AA] 241-426) and RNase H (AA 427-560) domains, which could affect drug resistance.

Methods: Genotypical and statistical analyses were performed on HIV-1 RT from 100 antiretroviral treatment-naive and 248 antiretroviral treatment-experienced patients, the majority of whom were infected with HIV-1 subtype B. The RT region was analysed in three parts: the polymerase (AA 1-240), thumb-connection (AA 241-426) and RNase H (AA 427-560) domains.

Results: The polymerase domain had statistically significant changes between the two groups at 24 AA positions that are known resistance sites. Within the thumb-connection domain, R284 and N348 had statistically significant changes between the groups (P=0.007 and P< or =0.001, respectively). In treatment-experienced patients, 17.3% had R284K, whereas 24.5% had N348I substitutions. Both R284 and N348 were 100% conserved in treatment-naive patients. Within the RNase H domain, only K451 showed a statistically significant change (P</=0.001), with K451R present in 11% of treatment-experienced patients but remaining 100% conserved among treatment-naive patients.

Conclusions: RT mutations at three positions outside of the polymerase region were associated with antiretroviral therapy: R284K, N348I and K451R. Both R284K and K451R interact with the phosphate backbone of the template or primer in HIV-1 RT crystal structures and could potentially influence the positioning of the primer strand, thus affecting polymerization, the efficiency of nucleoside reverse transcriptase inhibitor excision and/or RNase H activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / analogs & derivatives
  • Adenine / therapeutic use
  • Alkynes
  • Amino Acid Substitution / drug effects
  • Benzoxazines / therapeutic use
  • Cyclopropanes
  • Drug Resistance, Multiple, Viral
  • Genetic Variation / drug effects
  • HIV Infections / drug therapy
  • HIV Infections / virology
  • HIV Reverse Transcriptase / chemistry
  • HIV Reverse Transcriptase / genetics*
  • HIV-1* / drug effects
  • HIV-1* / genetics
  • Humans
  • Lamivudine / therapeutic use
  • Mutation / drug effects*
  • Organophosphonates / therapeutic use
  • Protein Structure, Tertiary / genetics
  • Reverse Transcriptase Inhibitors / therapeutic use*
  • Ribonuclease H, Human Immunodeficiency Virus / genetics
  • Stavudine / therapeutic use
  • Tenofovir

Substances

  • Alkynes
  • Benzoxazines
  • Cyclopropanes
  • Organophosphonates
  • Reverse Transcriptase Inhibitors
  • Lamivudine
  • Tenofovir
  • Stavudine
  • HIV Reverse Transcriptase
  • Ribonuclease H, Human Immunodeficiency Virus
  • Adenine
  • efavirenz