Inhibitors of protein− RNA complexation that target the RNA: specific recognition of human immunodeficiency virus type 1 TAR RNA by small organic molecules

HY Mei, M Cui, A Heldsinger, SM Lemrow, JA Loo… - Biochemistry, 1998 - ACS Publications
TAR RNA represents an attractive target for the intervention of human immunodeficiency
virus type 1 (HIV-1) replication by small molecules. We now describe three small molecule …

Structure of TAR RNA complexed with a Tat-TAR interaction nanomolar inhibitor that was identified by computational screening

Z Du, KE Lind, TL James - Chemistry & biology, 2002 - cell.com
Abstract HIV-1 TAR RNA functions critically in viral replication by binding the transactivating
regulatory protein Tat. We recently identified several compounds that experimentally inhibit …

An inhibitor of the Tat/TAR RNA interaction that effectively suppresses HIV-1 replication

F Hamy, ER Felder, G Heizmann… - Proceedings of the …, 1997 - National Acad Sciences
One of the first steps in HIV gene expression is the recruitment of Tat protein to the
transcription machinery after its binding to the RNA response element TAR. Starting from a …

Discovery of selective, small-molecule inhibitors of RNA complexes—1. The tat protein/TAR RNA complexes required for HIV-1 transcription

HY Mei, DP Mack, AA Galan, NS Halim… - Bioorganic & medicinal …, 1997 - Elsevier
We have developed a therapeutic program focusing on the inhibition of a human
immunodeficiency virus-1 specific protein-RNA interaction. This program begins with a …

Selective binding of TAR RNA by a Tat-derived β-peptide

MA Gelman, S Richter, H Cao, N Umezawa… - Organic …, 2003 - ACS Publications
The interaction between the HIV-1 Tat protein and the TAR RNA element in the nascent viral
genomic transcript is required for viral replication. An 11-residue β-peptide (1), an all-β …

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 …

A new class of HIV-1 Tat antagonist acting through Tat− TAR inhibition

F Hamy, V Brondani, A Flörsheimer, W Stark… - Biochemistry, 1998 - ACS Publications
The main transcriptional regulator of the human immunodeficiency virus, the Tat protein,
recognizes and binds to a small structured RNA element at the 5 'end of every viral mRNA …

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 …

Ligand-induced changes in 2-aminopurine fluorescence as a probe for small molecule binding to HIV-1 TAR RNA

TD Bradrick, JP Marino - Rna, 2004 - rnajournal.cshlp.org
Replication of human immunodeficiency virus type 1 (HIV-1) is regulated in part through an
interaction between the virally encoded trans-activator protein Tat and the trans-activator …

Structure of HIV-1 TAR RNA in the absence of ligands reveals a novel conformation of the trinucleotide bulge

F Aboul-ela, J Karn, G Varani - Nucleic acids research, 1996 - academic.oup.com
Efficient transcription from the human immunodeficiency virus (HIV) promoter depends on
binding of the viral regulatory protein Tat to a cis-acting RNA regulatory element, TAR. Tat …