Inhibitors of farnesyl-protein transferase

Details Inhibitors of farnesyl-protein transferase Inhibitors of farnesyl-protein transferase

1993-09-30

1995-11-21

Warden, Jill

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

548550, 546216, A61K 3800, C07D20712, C07D20724, C07D21140

Patent

active

054687330

ABSTRACT:
The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

REFERENCES:
patent: 5238922 (1993-08-01), Graham et al.
Kohl et al Proc. Natl. Acad. Sci., USA vol. 91 p. 9141 (1994).
Kohl, et al., Science, vol. 30, pp. 1934-1937 (1993).
James, et al., Science, vol. 30, pp. 1937-1942 (1993).
Omura, et al, Journal of Antibiotics, vol. 46, pp. 222-229 (1993).
Shiomi, et al., Jour. of Antibiotics, vol. 46, pp. 229-234 (1993).

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