Targeting RNA with peptidomimetic oligomers in human cells

Replication of human immunodeficiency virus type 1 (HIV-1) requires specifi c interactions of Tat protein with the transactivation responsive region (T AR) RNA, a 59-base stem-loop structure located at the 5'-end of all HIV mRN As. Here we report that two TAR RNA-binding peptidomimetics, oligourea and oligocarbamate, inhibit transcriptional activation by Tat protein in human cells with an IC50 of similar to0.5 and 1 muM, respectively. Peptidomimetic s that can target specific RNA structures provide novel molecules that can be used to control cellular processes involving protein-RNA interactions in vivo. (C) 2001 Elsevier Science Ltd. All rights reserved.