Inhibitors and target molecule co-localization

Details Inhibitors and target molecule co-localization Inhibitors and target molecule co-localization

A - Human Necessities

61

K

A61K 31/70 (2006.01) C12N 9/22 (2006.01) C12N 15/11 (2006.01) C12Q 1/70 (2006.01) A61K 38/00 (2006.01) A61K 39/00 (2006.01)

Patent

CA 2157015

The invention provides mechanisms for the co-localization in a living cell of a target molecule and of an inhibitor for the target molecule. The invention also provides novel chimeric tRNALYS-ribozyme molecules that compete effectiely with tRNALYS for HIV-1 reverse transcriptase binding sites. The chimeric human tRNALYS-ribozymes inhibit reverse HIV transcription by delivering inhibitors such as ribozymes of HIV-1 reverse transcriptase directly to the virion particle and render it non-functional. The chimeric molecules of the invention thus serve as highly specific non-toxic therapeutic agents and vaccines for viral, including lentiviral, infections. These chimeric molecules also reveal a novel, site specific RNA cleaving activity of HIV-1.

Cette invention concerne des mécanismes permettant de co-localiser dans une cellule vivante une molécule cible et un inhibiteur de cette même molécule cible, ainsi que de nouvelles molécules de ribozyme ARNt?LYS¿ chimères qui sont en forte concurrence avec l'ARNt?LYS¿ pour les sites de liaison de la transcriptase inverse du VIH-1. Ces ribosymes d'ARNt?LYS¿ humaines chimères inhibent la tanscription inverse du VIH-1 en apportant directement à la particule du virion des inhibiteurs tels que des ribozymes de la transcriptase inverse du VIH-1 et la rendent non fonctionnelle. Les molécules chimères de cette invention servent par conséquent d'agents et de vaccins thérapeutiques non toxiques hautement spécifiques utilisables contre les infections virales, y compris lentivirales. Ces molécules chimères ont également permis de découvrir une nouvelle activité de clivage de l'ARN à spécificité de site du VIH-1.

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