Methods and compositions for the identification, characterization, and inhibition of farnesyl protein transferase
US5976851A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Feb 16, 1993 |
| Grant date | Nov 2, 1999 |
| Priority date | — |
| Expiry date | Feb 16, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/1013
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
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 p21.sup.ras. The nucleotide and amino acid sequences of the .alpha. and .beta. subunits of both rat and human farnesyl transferase are disclosed, as are methods and compositions for the preparation of farnesyl transferase by recombinant means, following the molecular 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 p21.sup.ras. Also disclosed is a families of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.