A selective HIV-1 RNA G-quadruplex-targeting L-aptamer-D-antisense conjugate inhibits HIV-1 minus strand transfer

Chem Commun (Camb). 2024 Nov 14;60(92):13558-13561. doi: 10.1039/d4cc03448a.

Abstract

Herein, we develop an L-RNA aptamer, L-Apt.T8, for recognizing HIV-1 U3-III RNA G-quadruplex, and conjugate the L-Apt.T8 with DNA antisense (L-Apt.T8-10D) to enhance the binding affinity and selectivity. We demonstrate that L-Apt.T8-10D can inhibit HIV-1 U3-tRNA segment complementary binding and nucleocapsid interaction, and interrupt in vitro HIV-1 minus strand transfer.

MeSH terms

  • Aptamers, Nucleotide* / chemistry
  • Aptamers, Nucleotide* / pharmacology
  • G-Quadruplexes* / drug effects
  • HIV-1* / drug effects
  • Humans
  • Oligonucleotides, Antisense / chemistry
  • Oligonucleotides, Antisense / pharmacology
  • RNA, Viral* / metabolism

Substances

  • Aptamers, Nucleotide
  • RNA, Viral
  • Oligonucleotides, Antisense