A selective HIV-1 RNA G-quadruplex-targeting l-aptamer–d-antisense conjugate inhibits HIV-1 minus strand transfer

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.