A method of treating cancer

Details A method of treating cancer A method of treating cancer

C - Chemistry, Metallurgy

12

Q

C12Q 1/48 (2006.01) A01N 43/40 (2006.01) A01N 43/50 (2006.01) A01N 43/62 (2006.01) A61K 31/00 (2006.01) A61K 31/415 (2006.01) A61K 31/4174 (2006.01) A61K 31/4178 (2006.01) A61K 31/4439 (2006.01) A61K 31/445 (2006.01) A61K 31/454 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61K 31/55 (2006.01) A61K 31/5513 (2006.01) A61K 38/00 (2006.01) A61K 38/05 (2006.01) C12N 9/10 (2006.01) C12N 9/99 (2006.01) G01N 33/50 (2006.01)

Patent

CA 2301877

The instant invention provides for a method of inhibiting prenyl-protein transferases and treating cancer which comprises administering to a mammal a prenyl-protein transferase inhibitor which is efficacious in vivo as an inhibitor of geranylgeranyl-protein transferase type I (GGTase-I). The invention also provides for a method of inhibiting farnesyl-protein transferase and geranylgeranyl-protein transferase type I by administering a compound that is a dual inhibitor of both of those prenyl-protein transferases. The invention also provides for a method of identifying such a compound, the method comprising a modified inhibitory assay that incorporates a modulator anion that alters the in vitro potency of prenyl-protein transferase inhibitors in a way that predicts their potency in vivo, thus providing convenient identification of compounds that possess such in vivo activity.

L'invention concerne un procédé pour inhiber les prényl-protéine-transférases et traiter le cancer, qui consiste à administrer à un mammifère un inhibiteur de prényl-protéine-transférase constituant un inhibiteur efficace in vivo de la géranylgéranyl-protéine-transférase de type I (GGTase-I). L'invention concerne aussi un procédé permettant d'inhiber la farnésyl-protéine-transférase et la géranylgéranyl-protéine-transférase de type I en administrant un composé qui est un double inhibiteur pour ces deux prényl-protéine-transférases. L'invention concerne en outre un procédé permettant d'identifier le composé susmentionné, qui consiste en un essai inhibiteur modifié comprenant un anion modulateur capable de modifier l'activité in vitro des inhibiteurs de prényl-protéine-transférase de manière à prévoir l'activité in vivo de ces inhibiteurs, moyennant quoi il est possible d'identifier aisément les composés possédant ladite activité in vivo.

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