INHIBITION OF GENE TRANSCRIPTION BY POLYAMIDE DNA-BINDING LIGANDS

• Main Authors: MOSIER, DONALD, E, DERVAN, PETER, B, GOTTESFELD, JOEL, M, BAIRD, ELDON, E
• Format: Patent
• Language: English; French
• Published: 20.08.1998
• Edition: 6
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; VINEGAR; WINE

The invention provides polyamides suitable for modulating cellular or viral gene expression by binding to an identified target DNA sequence adjacent to the binding site of a minor groove transcription factor protein. The polyamides of the present invention are useful for the treatment of a human infected with a virus such as HIV-1. The polyamides of the present invention are also useful for the treatment of conditions, such as cancers, that result from the expression or over-expression of cellular genes, particularly oncogenes. L'invention porte sur des polyamides pouvant moduler l'expression de gènes cellulaires ou viraux en se fixant à une séquence cible d'ADN identifiée contiguë au site de fixation d'une protéine facteur de transcription dans le petit sillon. Lesdites polyamides sont utilisées pour traiter les humains infectés par le VIH-1 et également pour traiter des maladies telles que le cancer, résultant de l'expression ou de la surexpression de gènes cellulaires, et en particulier d'oncogènes.