Targeting RNA with Small-molecule drugs: Therapeutic promise and chemical challenges

Accounts of Chemical Research

Volumn 34, Issue 10, 2001, Pages 836-843

  Gallego, J ^b   Varani, G ^a,b  

^a UNIVERSITY OF WASHINGTON   (United States)

^b MRC LABORATORY OF MOLECULAR BIOLOGY   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIINFECTIVE AGENT; BACTERIAL RNA; VIRUS RNA;

ARTICLE; BIOLOGY; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DRUG DESIGN; DRUG EFFECT; HUMAN IMMUNODEFICIENCY VIRUS 1; PROTEIN SECONDARY STRUCTURE; RIBOSOME; RNA ANALYSIS; RNA BINDING; RNA PROCESSING; RNA SEQUENCE; RNA STRUCTURE; STRUCTURE ACTIVITY RELATION;

ANTI-BACTERIAL AGENTS; COMPUTATIONAL BIOLOGY; DRUG DESIGN; NUCLEIC ACID CONFORMATION; RIBOSOMES; RNA, BACTERIAL; RNA, VIRAL; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0034783659     PISSN: 00014842     EISSN: None     Source Type: Journal    
DOI: 10.1021/ar000118k     Document Type: Article

References (55)

1. Progress in anti-HIV structure-based drug design
2. RNA as a small-molecule drug target: Doubling the value of genomics
3. Gene inhibition using antisense oligonucleotides
4. A good antisense molecule is hard to find
5. Imprinted expression of small nucleolar RNAs in brain: Time for RNomics
6. Alternative Pre-mRNA splicing: The logic of combinatorial control
7. Post-Transcriptional gene silencing by Double-Stranded RNA
8. Duplexes of 21-Nucleotide RNAs mediate interference in cultured mammalian cells
9. RNA recognition by the human immunodeficiency virus tat and rev proteins
10. An inhibitor of the Tat/TAR RNA interaction that effectively suppresses HIV-1 replication
11. Inhibitors of Protein-RNA complexation that target the RNA: Specific recognition of human immunodeficiency virus type I TAR RNA by small organic molecules
12. New class of HIV-1 tat antagonist acting through Tat-TAR inhibition
13. Inhibition of gene expression in human cells through small Molecule-RNA interactions
14. P-TEFb kinase is required for HIV tat transcriptional activation in vivo in vitro
15. Internal initiation of translation in eukaryotes: The picornavirus paradigm beyond
16. Potential RNA drug target in the hepatitis C virus internal ribosomal entry site
17. Structures of two domains essential for hepatitis C virus internal ribosome entry site function
18. The crisis in antibiotic resistance
19. HIV treatment failure: Testing for HIV resistance in clinical practice
20. Design of small molecules that recognize RNA: Development of aminoglycosides as potential antitumor agents that target oncogenic RNA sequences
21. Aminoglycoside antibiotics are able to specifically bind the 5′-untranslated region of thymidilate synthase messenger RNA
22. Inhibition of human telomerase in immortal human cells leads to progressive telomere shortening and cell death
23. Interaction of antibiotics with functional sites in 16S ribosomal RNA
24. Structure of the A site of Escherichia coli 16S ribosomal RNA complexed with an aminoglycoside antibiotic
25. Paromomycin binding induces a local conformational change in the A site of 16S rRNA
26. The complete atomic structure of the large ribosomal subunit at 2.4 A resolution
27. Structure of the 30S ribosomal subunit
28. Functional insights from the structure of the 30S ribosomal subunit and its interaction with antibiotics
29. The structural basis for the action of the antibiotics tetracyclin pactamycin hygromycin B on the 30S ribosomal subunit
30. Recognition of the Codon-Anticodon helix by ribosomal RNA
31. Structural basis of RNA folding recognition in an AMP-RNA aptamer complex
32. High-resolution molecular discrimination by RNA
33. Interlocking structural motifs mediate molecular discrimination by a Theophylline-Binding RNA
34. Conformation of the TAR-Arginine complex by NMR
35. The structure of the human immunodeficiency virus Type-1 TAR RNA reveals principles of RNA recognition by tat protein
36. Binding of neomycin to TAR element of HIV-1 RNA induces dissociation of tat protein by an allosteric mechanism
37. Detailed View of a Ribosomal Active Site: The structure of the L11-RNA complex
38. Electrostatic Interactions in RNA aminoglycosides binding
39. Direct observation of Aminoglycoside-RNA interactions by surface plasmon resonance
40. Inhibition of the Self-Cleavage reaction of the human hepatitis delta virus ribozyme by antibiotics
41. Simple aminols as aminoglycoside surrogates
42. Probing the specificity of Aminoglycoside-Ribosomal RNA interactions with designed synthetic analogs
43. A library approach to the discovery of small molecules that recognize RNA: Use of a 1,3-Hydroxyamine motif as a core
44. Determinants of aminoglycoside-binding specificity for rRNA by using mass spectrometry
45. NMR-Based screening in drug discovery
46. Recent advances in structure-based rational drug design
47. Structure-Based discovery of ligands targeted to the RNA double helix
48. Identification of ligands for RNA targets via structure-based virtual screening: HIV-1 TAR
49. Oxazolidinones; a review
50. Rapid combinatorial synthesis of aminoglycoside antibiotic mimetics: Use of a polyethylene glycol-linked amine and a neamine-derived aldehyde in multiple component condensation as a strategy for the discovery of new inhibitors of the HIV RNA Rev responsive element
51. Modulation of the Rev-RRE interaction by aromatic heterocyclic compounds
52. Heterocyclic inhibitor of the Rev-RRE complex binds to RRE as a dimer
53. Synthesis of novel polyazadipyridinocyclophane scaffolds their application for the generation of libraries
54. HIV-1 TAR RNA recognition by an unnutural biopolymer
55. Neomycin-Acridine Conjugate: A potent inhibitor of Rev-RRE binding