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

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. [ABSTRACT FROM AUTHOR]