Targeting RNA with small-molecule drugs: therapeutic promise and chemical challenges

J Gallego, G Varani - Accounts of chemical research, 2001 - ACS Publications
Researchers' increasing awareness of the essential role played by RNA in many biological
processes and in the progression of disease makes the discovery of new RNA targets an …

Combinatorial chemistry

NK Terrett - 1998 - books.google.com
Combinatorial chemistry, by accelerating the process of chemical synthesis, is having a
profound effect on all branches of chemistry, but especially on drug discovery. This …

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 …

NMR-based characterization of phenothiazines as a RNA binding scaffold

M Mayer, TL James - Journal of the American Chemical Society, 2004 - ACS Publications
Phenothiazines were identified by virtual screening as promising ligands for HIV-1 TAR RNA
and A-site ribosomal RNA, and binding in each case was verified experimentally …

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 …

Inhibition of translation by RNA–small molecule interactions

I Harvey, P Garneau, J Pelletier - Rna, 2002 - cambridge.org
Small molecule ligand–RNA interactions have the potential to influence gene expression at
a variety of steps and in a number of ways. Here, we demonstrate that such interactions are …

Click dimers to target HIV TAR RNA conformation

S Kumar, P Kellish, WE Robinson Jr, D Wang… - Biochemistry, 2012 - ACS Publications
A series of neomycin dimers have been synthesized using “click chemistry” with varying
functionality and length in the linker region to target the human immunodeficiency virus type …

Discovery of a small molecule Tat-trans-activation-responsive RNA antagonist that potently inhibits human immunodeficiency virus-1 replication

S Hwang, N Tamilarasu, K Kibler, H Cao, A Ali… - Journal of Biological …, 2003 - ASBMB
Antiretroviral therapy to treat AIDS uses molecules that target the reverse transcriptase and
protease enzymes of human immunodeficiency virus, type 1 (HIV-1). A major problem …

Targeting RNA: new opportunities to address drugless targets

GJR Zaman, PJA Michiels, CAA van Boeckel - Drug discovery today, 2003 - Elsevier
Historically, pharmaceutical industries have focussed on the discovery of compounds that
target the protein products of genes. The intermediary product between gene and protein …

Design of RNA-binding proteins and ligands

AC Cheng, V Calabro, AD Frankel - Current Opinion in Structural Biology, 2001 - Elsevier
The rapidly expanding database of RNA structures and protein complexes is beginning to
lead to the successful design of specific RNA-binding molecules. Recent combinatorial and …