Highly efficient inhibition of human immunodeficiency virus type 1 reverse transcriptase by aptamers functionalized gold nanoparticles

Abstract

We have developed aptamer (Apt)-conjugated gold nanoparticles (Apt–Au NPs, 13 nm in diameter) as highly effective inhibitors for human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT). Two Apts, RT1t49 (Apt_pol) and ODN 93 (Apt_RH), which recognize the polymerase and RNase H regions of HIV-1 RT, are used to conjugate Au NPs to prepare Apt_pol–Au NPs and Apt_RH–Au NPs, respectively. In addition to DNA sequence, the surface density of the aptamers on Au NPs (nApt–Au NPs; n is the number of aptamer molecules on each Au NP) and the linker length number (T_m; m is the base number of the deoxythymidine linker) between the aptamer and Au NPs play important roles in determining their inhibition activity. A HIV-lentiviral vector-based antiviral assay has been applied to determine the inhibitory effect of aptamers or Apt–Au NPs on the early stages of their replication cycle. The nuclease-stable G-quadruplex structure of 40Apt_RH-T₄₅–Au NPs shows inhibitory efficiency in the retroviral replication cycle with a decreasing infectivity (40.2%).