Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving transferase
Patent
1998-08-26
2000-08-15
Krass, Frederick
Chemistry: molecular biology and microbiology
Measuring or testing process involving enzymes or...
Involving transferase
435 772, 435193, 436 64, 436 71, 436 86, 436100, 436101, 436102, 436103, 436182, 436815, C12Q 148
Patent
active
061034878
ABSTRACT:
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.
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Barnett Stanley F.
Heimbrook David C.
Huber Hans E.
Patrick Denis R.
Daniel Mark R.
Krass Frederick
Merck & Co. , Inc.
Muthard David A.
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