C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/48 (2006.01) A01N 43/00 (2006.01) A01N 43/40 (2006.01) A01N 43/50 (2006.01) A61K 31/00 (2006.01) A61K 31/415 (2006.01) A61K 31/445 (2006.01) A61K 31/55 (2006.01) C12N 9/10 (2006.01) G01N 33/50 (2006.01)
Patent
CA 2301880
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 an inhibitor of cellular processing of the H-Ras and K4B-Ras proteins. The invention in particular 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 instant invention als provides for a method of identifying such a compound, the method comprising an assay whose readout is a consequence of the biological activity or inhibition of that activity of the Ras protein, thus providing convenient identification of compounds that inhibit cellular processing of the H-Ras and K4B-Ras proteins.
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 du traitement cellulaire des protéines H-Ras et K4B-Ras. En particulier, l'invention concerne 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 aussi un procédé permettant d'identifier le composé susmentionné, par le biais d'un essai dont l'indication correspond à l'activité biologique de la protéine Ras ou à l'inhibition de ladite activité, moyennant quoi on identifie aisément les composés qui inhibent le traitement cellulaire des protéines H-Ras et K4B-Ras.
Defeo-Jones Deborah
Heimbrook David C.
Oliff Allen I.
Stirdivant Steven M.
Gowling Lafleur Henderson Llp
Merck & Co. Inc.
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