Targeting RNA with small-molecule drugs: therapeutic promise and chemical challenges
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 …
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 …
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 …
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 …
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 …
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 …
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
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 …
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 …
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 …
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 …
lead to the successful design of specific RNA-binding molecules. Recent combinatorial and …