title: 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 (Aptpol) and ODN 93 (AptRH), which recognize the polymerase and RNase H regions of HIV-1 RT, are used to conjugate Au NPs to prepare Aptpol-Au NPs and AptRH-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 (Tm; 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 40AptRH-T45-Au NPs shows inhibitory efficiency in the retroviral replication cycle with a decreasing infectivity (40.2%).
authors: Department of Chemistry, National Taiwan University, 1, Section 4, Roosevelt Road, Taipei 10617, Taiwan.
authors: Yen-Chun
authors: YC
authors: Shiang
authors: Chung-Mao
authors: CM
authors: Ou
authors: Shih-Ju
authors: SJ
authors: Chen
authors: Ting-Yu
authors: TY
authors: Ou
authors: Han-Jia
authors: HJ
authors: Lin
authors: Chih-Ching
authors: CC
authors: Huang
authors: Huan-Tsung
authors: HT
authors: Chang
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D052157:Aptamers, Nucleotide / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006046:Gold; D057809:HEK293 Cells; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000235:genetics; D015497:HIV-1 / Q000201:enzymology*; D056945:Hep G2 Cells; D006801:Humans; D053768:Metal Nanoparticles; D058726:Nanoconjugates
chemical_list: D000998:Antiviral Agents; D052157:Aptamers, Nucleotide; D058726:Nanoconjugates; D006046:Gold; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase