Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice

Nature Medicine

Volumn 1, Issue 8, 1995, Pages 792-797

  Kohl, Nancy E ^a   Omer, Charles A ^a   Davide, Joseph P ^a   Hamilton, Kelly ^a   Koblan, Kenneth S ^a   Kral, Astrid M ^a   Miller, Patricia J ^a   Mosser, Scott D ^a   O'neill, Timothy J ^a   Rands, Elaine ^a   Schaber, Michael D ^a   Gibbs, Jackson B ^a   Oliff, Allen ^a   Conner, Michael W ^a   Anthony, Neville J ^b   Jane Desolms, S ^b   Giuliani, Elizabeth A ^b   Gomez, Robert P ^b   Graham, Samuel L ^b   Hartman, George D ^b  

^a Department of Cancer Research ^*  (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 [[2 [[2 [(2 AMINO 3 MERCAPTOPROPYL)AMINO] 3 METHYLPENTYL]OXY] 1 OXO 3 PHENYLPROPYL]AMINO] 4 (METHYLSULFONYL)BUTANOIC ACID ISOPROPYL ESTER; DOXORUBICIN; ENZYME INHIBITOR; FARNESYL TRANS TRANSFERASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BREAST CARCINOMA; CANCER THERAPY; ENZYME INHIBITION; INTRAPERITONEAL DRUG ADMINISTRATION; MOUSE; NONHUMAN; ONCOGENE RAS; PRIORITY JOURNAL; SALIVARY GLAND CARCINOMA; SUBCUTANEOUS DRUG ADMINISTRATION; TRANSGENIC MOUSE;

ANIMAL; ANTINEOPLASTIC AGENTS; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; FEMALE; GENES, RAS; MAMMARY NEOPLASMS, EXPERIMENTAL; METHIONINE; MICE; MICE, TRANSGENIC; SALIVARY GLAND NEOPLASMS; TRANSFERASES;

ANIMALIA; MAMMALIA; MOUSE MAMMARY TUMOR VIRUS; MUS MUSCULUS;

EID: 0029150669     PISSN: 10788956     EISSN: 1546170X     Source Type: Journal    
DOI: 10.1038/nm0895-792     Document Type: Article

References (17)

1. Barbacid, M. Ras genes. Annu. -Rev. Biochem. 56, 779-827 (1987).
2. Lowy, D.R. & Willumsen, B.M. Function and regulation of ras. Annu. Rev. Biochem. 62, 851-891 (1993).
3. Adams, J.M. & Cory, S. Transgenic models of tumor development. Science 254, 1161-1167(1991).
4. Clark, G.J. & Der, CJ. Ras proto-oncogene activation in human malignancy, in Cellular Cancer Markers (eds Garrett, C.T. & Sell, S.) 17-52 (Humana Press, Totowa, New Jersey, 1995).
5. Bos, J.L. Ras oncogenes in human cancer: A review. Cancer Res. 49, 4682-4689 (1989).
6. Gibbs, J.B. Ras C-terminal processing enzymes—new drug targets? Cell 65, 1-4 (1991).
7. Clarke, S. Protein isoprenylation and méthylation at carboxyl-terminal cysteine residues. Annu. Rev. Biochem. 61, 355-386 (1992).
8. Gibbs, J.B., Oliff, A. & Kohl, N.E. Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic. Cell 77, 175-178 (1994).
9. Patel, D.V. et al. Phosphinyl acid-based bisubstrate analog inhibitors of Ras far- nesyl protein transferase. J. med. Chem. 38, 435-442 (1995).
10. Kohl, N.E. et al. Farnesyltransferase inhibitors block the growth of ras-depen¬dent tumors in nude mice. Proc. natn. Acad. Sci. U.S.A. 91, 9141-9145 (1994).
11. Sinn, E. et al. Coexpression of MMTVJv-Ha-ras and MMTVJc-myc genes in transgenic mice: Synergistic action of oncogenes in vivo. Cell 49, 465-475 (1987).
12. Dexter, D.L., Diamond, M., Creveling, J. & Chen, S.-F. Chemotherapy of mam¬mary carcinomas arising in ras transgenic mice. Invest, new Drugs 11, 161-168 (1993).
13. James, G.L. etal. Benzodiazepine peptidomimetics: Potent inhibitors of Ras far¬nésylation in animal cells. Science 260, 1937-1942 (1993).
14. Prendergast, G.C. et al. Farnesyltransferase inhibition causes morphological re¬version of Ras-transformed cells by a complex mechanism that involves regula¬tion of the actin cytoskeleton. Molec. cell. Biol. 14, 4193-4202 (1994).
15. James, G.L., Goldstein, J.L., Pathak, R.K., Anderson, R.G.W. & Brown, M.S. A prenytated protein of peroxisomes. J. hiol. Chem. 269, 14182-14190 (1994).
16. Vogelstein, B. & Kinzler, K.W. The multistep nature of cancer. Trends Genet. 9, 138-141 (1993).
17. Yamada, H., Yoshida, T., Sakamoto, H., Terada, M, & Sugimura, T. Establishment of a human pancreatic adenocarcinoma cell line (PSN-1) with amplification of both c-myc and activated c-Ki-ras by a point mutation. Biochem. biophys. Res. Commun. 140, 167-173 (1986)