Development of small molecules with a noncanonical binding mode to HIV-1 trans activation response (TAR) RNA

FA Abulwerdi, MD Shortridge… - Journal of medicinal …, 2016 - ACS Publications
Small molecules that bind to RNA potently and specifically are relatively rare. The study of
molecules that bind to the HIV-1 transactivation response (TAR) hairpin, a cis-acting HIV …

Essential structural requirements for specific recognition of HIV TAR RNA by peptide mimetics of Tat protein

A Davidson, K Patora-Komisarska… - Nucleic acids …, 2011 - academic.oup.com
The pharmacological disruption of the interaction between the HIV Tat protein and its
cognate transactivation response RNA (TAR) would generate novel anti-viral drugs with a …

An evolved RNA recognition motif that suppresses HIV-1 Tat/TAR-dependent transcription

DW Crawford, BD Blakeley, PH Chen… - ACS chemical …, 2016 - ACS Publications
Potent and selective recognition and modulation of disease-relevant RNAs remain a
daunting challenge. We previously examined the utility of the U1A N-terminal RNA …

A small-molecule probe induces a conformation in HIV TAR RNA capable of binding drug-like fragments

A Davidson, DW Begley, C Lau, G Varani - Journal of molecular biology, 2011 - Elsevier
The HIV-1 transactivation response (TAR) element–Tat interaction is a potentially valuable
target for treating HIV infection, but efforts to develop TAR-binding antiviral drugs have not …

Simultaneous recognition of HIV-1 TAR RNA bulge and loop sequences by cyclic peptide mimics of Tat protein

A Davidson, TC Leeper… - Proceedings of the …, 2009 - National Acad Sciences
The interaction of the HIV-1 transactivator protein Tat with its transactivation response (TAR)
RNA is an essential step in viral replication and therefore an attractive target for developing …

Targeting the HIV Trans‐Activation Responsive Region—Approaches Towards RNA‐Binding Drugs

A Krebs, V Ludwig, O Boden, MW Göbel - ChemBioChem, 2003 - Wiley Online Library
RNA±protein interactions are essential for many biological processes such as translation,
RNA splicing, and transcription. For a long time, RNA was regarded mainly as a passive …

[HTML][HTML] Structure-based computational database screening, in vitro assay, and NMR assessment of compounds that target TAR RNA

KE Lind, Z Du, K Fujinaga, BM Peterlin, TL James - Chemistry & biology, 2002 - cell.com
There has been little prior effort to discover new drugs on the basis of a unique RNA
structure. Binding of the viral transactivator Tat to the 5′ bulge of the transactivation …

Structure-based drug design targeting an inactive RNA conformation: exploiting the flexibility of HIV-1 TAR RNA

AIH Murchie, B Davis, C Isel, M Afshar… - Journal of molecular …, 2004 - Elsevier
The targeting of RNA for the design of novel anti-viral compounds represents an area of vast
potential. We have used NMR and computational methods to model the interaction of a …

Structural mimicry of retroviral tat proteins by constrained β-hairpin peptidomimetics: ligands with high affinity and selectivity for viral TAR RNA regulatory elements

Z Athanassiou, RLA Dias, K Moehle… - Journal of the …, 2004 - ACS Publications
An approach is described to the design of β-hairpin peptidomimetic ligands for bovine
immunodeficiency virus (BIV) Tat protein, which inhibit binding to its transactivator response …

Targeting RNA with peptidomimetic oligomers in human cells

N Tamilarasu, I Huq, TM Rana - Bioorganic & medicinal chemistry letters, 2001 - Elsevier
Replication of human immunodeficiency virus type 1 (HIV-1) requires specific interactions of
Tat protein with the trans-activation responsive region (TAR) RNA, a 59-base stem-loop …