C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/10 (2006.01) A61K 38/03 (2006.01) A61K 38/06 (2006.01) A61K 38/07 (2006.01) C07K 1/107 (2006.01) C07K 4/00 (2006.01) C07K 5/08 (2006.01) C07K 5/103 (2006.01) C07K 5/107 (2006.01) C07K 5/11 (2006.01) C07K 5/117 (2006.01) C07K 7/02 (2006.01) C12N 9/10 (2006.01) C12N 9/99 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2142990
Disclosed are methods and compositions for the identification, characterization and inhibition of mammalian farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21ras. The nucleotide and amino acid sequences of the .alpha. and .beta. subunits of both rat and human farnesyl transferase are dis- closed, as are methods and compositions for the preparation of farnesyl transferase by recombinant means, following the molecu- lar cloning and co-expression of its two subunits, for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21ras. Also disclosed is a family of compounds which act either as false substrates for the enzyme or as pure inhibibors and can therefore be employed for the inhibition of the enzyme. The most potent inhibitors are one in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine. Improved inhibitors with defined structures and characteristica are slso disclosed.
Brown Michael S.
Goldstein Joseph L.
Marsters James C. Jr.
Reiss Yuval
Bereskin & Parr
Genentech Inc.
The Board Of Regents Of The University Of Texas System
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