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 31/415 (2006.01) A61K 31/445 (2006.01) A61K 31/55 (2006.01) C12N 9/10 (2006.01)
Patent
CA 2301857
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 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. A method of identifying a prenyl- protein transferase inhibitor which is an inhibit or of in vivo growth of cancer cells is also disclosed. The instant method comprises a cell-based in vitro assay which determines the physical state of a protein substrate of geranylgeranyl-protein transferase type I.
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. 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 qui permet d'identifier un inhibiteur de prényl-protéine-transférase constituant un inhibiteur de la croissance in vivo des cellules cancéreuses. Ce procédé consiste en un essai in vitro à base cellulaire, qui permet de déterminer l'état physique d'un substrat de protéine de géranylgéranyl-protéine-transférase de type I.
Burkhardt Anne L.
Buser-Doepner Carolyn A.
Huang Pearl S.
Koblan Kenneth S.
Kohl Nancy E.
Gowling Lafleur Henderson Llp
Merck & Co. Inc.
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