Peptide inhibitors of farnesyl-protein transferase

Details Peptide inhibitors of farnesyl-protein transferase Peptide inhibitors of farnesyl-protein transferase

1995-06-02

1997-08-26

Tsang, Cecilia J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530330, A61K 3800

Patent

active

056611285

ABSTRACT:
The present invention is directed to tetrapeptides which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to a method of treating cancer with tetrapeptide inhibitors of farnesyl protein transferase, as well as pharmaceutical formulations useful for this method of treatment.

REFERENCES:
patent: 5043268 (1991-08-01), Stock
patent: 5141851 (1992-08-01), Brown et al.
patent: 5238922 (1993-08-01), Graham et al.
patent: 5326773 (1994-07-01), De Solms et al.
patent: 5340828 (1994-08-01), Graham et al.
patent: 5352705 (1994-10-01), Deana et al.
Gibbs, J.B. et al., "Selective Inhibition of Farnesyl-Protein Transferase Blocks Ras Processing in Vivo", The Journal of Biological Chemistry, vol. 268, No. 11, pp. 7617-7620 (1993).
Goldstein, J.L. et al., "Nonfarnesylated Tetrapeptide Inhibitors of Protein Farnesyltransferase", The Journal of Biological Chemistry, vol. 266, No. 24 pp. 15575-15578 (1991).
James, G.L. et al., "Benzodiazepine Peptidomimetic BZA-5B Interrupts the MAP Kinase Activation Pathway in H-Ras-transformed Rat-1 Cells, but Not in Untransformed Cells", The Journal of Biological Chemistry, vol. 269, No. 44, pp. 27705-27714 (1994).
James, G.L. et al., "Benzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation in Animal Cells", Science, vol. 260, pp. 1937-1942 (1993).
Kohl, N.E. et al., "Selective Inhibition of Ras-Dependent Transformation by a Farnesyltransferase Inhibitor", Science, vol. 260 pp. 1934-1937 (1993).
Kohl, N.E. et al., "Protein Farnesyltransferase Inhibitors Block the Growth of Ras-Dependent Tumors in Nude Mice", Proc. Natl. Acad. Sci. USA Med. Sci., vol. 91 pp. 9141-9145 (1994).
Pompliano, D.L. et al., "Steady-State Kinetic Mechanism of Ras Farnesyl:Protein Transferase, Biochemistry", vol. 31, pp. 3800-3807 (1992).
James, G.L. et al., "Polylsine and CVIM Sequences of K-Ras B Dictate Specificity of Prenylation an Confer Resistance to Benzodiazepine Peptidomimetic In Vito", The Journal of Biological Chemistry, vol. 270, No. 11 pp. 6221-6226 (1995).

Affiliated with

Also associated with

Rating

Peptide inhibitors of farnesyl-protein transferase does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Peptide inhibitors of farnesyl-protein transferase, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Peptide inhibitors of farnesyl-protein transferase will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1988583