Antitumor activity of ER-51785, a new peptidomimetic inhibitor of farnesyl transferase: Synergistic effect in combination with paclitaxel

Oncology Research

Volumn 12, Issue 11-12, 2000, Pages 477-484

  Nakamura, Katsuji ^a   Yamaguchi, Atsumi ^a   Namiki, Masayuki ^a   Ishihara, Hiroshi ^a   Nagasu, Takeshi ^a   Kowalczyk, James J ^b   Garcia, Ana Maria ^b   Lewis, Michael D ^b   Yoshimatsu, Kentaro ^a  

^a EISAI CO LTD   (Japan)

^b EISAI RESEARCH INSTITUTE   (United States)

Author keywords

ER 51785; Farnesyl transferase; ras; Tumor regression; Xenograft

Indexed keywords

ANTINEOPLASTIC AGENT; BENZAMIDE DERIVATIVE; DRUG DERIVATIVE; ENZYME INHIBITOR; ER 51785; FARNESYL TRANS TRANSFERASE; METHIONINE; PACLITAXEL; TRANSFERASE;

ANIMAL; ARTICLE; BLADDER TUMOR; CELL CULTURE; CELL DIVISION; CELL LINE; CELL STRAIN 3T3; CELL TRANSFORMATION; DRUG ANTAGONISM; DRUG EFFECT; DRUG POTENTIATION; HUMAN; MOUSE; NUDE MOUSE; ONCOGENE RAS; PANCREAS TUMOR; PATHOLOGY; PROTEIN PROCESSING; XENOGRAFT;

3T3 CELLS; ALKYL AND ARYL TRANSFERASES; ANIMALS; ANTINEOPLASTIC AGENTS; ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS; BENZAMIDES; CELL DIVISION; CELL LINE, TRANSFORMED; CELL TRANSFORMATION, NEOPLASTIC; DRUG SYNERGISM; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; GENES, RAS; HUMANS; METHIONINE; MICE; MICE, NUDE; PACLITAXEL; PANCREATIC NEOPLASMS; PROTEIN PROCESSING, POST-TRANSLATIONAL; TRANSPLANTATION, HETEROLOGOUS; TUMOR CELLS, CULTURED; URINARY BLADDER NEOPLASMS;

EID: 0034585273     PISSN: 09650407     EISSN: None     Source Type: Journal    
DOI: 10.3727/096504001108747486     Document Type: Article

References (29)

1. Barbacid, M. Ras genes. Annu. Rev. Biochem. 56:779-827; 1987.
2. Joneson, T.; White, M. A.; Wigler, M. H.; Bar-Sagi, D. Stimulation of membrane ruffling and MAP kinase activation by distinct effectors of RAS. Science 271:810-812; 1996.
3. Lowy, D. R.; Willumsen, B. M. Function and regulation of Ras. Annu. Rev. Biochem. 62:851-891; 1993.
4. Bos, J. L. Ras oncogenes in human cancer: A review. Cancer Res. 49:4682-4689; 1989.
5. Cox, A. D.; Der, C. J. The ras/cholesterol connection: Implications for ras oncogenicity. Crit. Rev. Oncog. 3:365-400; 1992.
6. Hancock, J. F.; Magee, A. I.; Childs, J. E.; Marshall, C. J. All ras proteins are polyisoprenylated but only some are palmitoylated. Cell 57:1167-1177; 1989.
7. Casey, P. J.; Solski, P. A.; Der, C. J.; Buss, J. E. p21ras is modified by a farnesyl isoprenoid. Proc. Natl. Acad. Sci. USA 86: 8323-8327; 1989.
8. Kato, K.; Cox, A. D.; Hisaka, M. M.; Graham, S. M.; Buss, J. E.; Der, C. J. Isoprenoid addition to Ras protein is the critical modification for its membrane association and transforming activity. Proc. Natl. Acad. Sci. USA 89:6403-6407; 1992.
9. Porfiri, E.; Evans, T.; Chardin, P.; Hancock, J. F. Prenylation of Ras proteins is required for efficient hSOSI-promoted guanine nucleotide exchange. J. Biol. Chem. 269:22672-22677; 1994.
10. Cox, A. D.; Garcia, A. M.; Westwick, J. K.; Kowalczyk, J. J.; Lewis, M. D.; Brenner, D. A.; Der, C. J. The CAAX peptidomimetic compound B581 specifically blocks farnesylated, but not geranylgeranylated or myristylated, oncogenic ras signaling and transformation. J. Biol. Chem. 269:19203-19206; 1994.
11. Cadwallader, K. A.; Paterson, H.; Macdonald, S. G.; Hancock, J. F. N-terminally myristoylated Ras proteins require palmitoylation or a polybasic domain for plasma membrane localization. Mol. Cell. Biol. 14:4722-4730; 1994.
12. Gibbs, J. B. Ras C-terminal processing enzymes: New drug targets? Cell 65:1-4; 1991.
13. Garcia, A. M.; Rowell, C.; Ackermann, K.; Kowalczyk, J. J.; Lewis, M. D. Peptidomimetic inhibitors of Ras farnesylation and function in whole cells. J. Biol. Chem. 268:18415-18418; 1993.
14. Nagasu, T.; Yoshimatsu, K.; Rowell, C.; Lewis, M. D.; Garcia, A. M. Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase Inhibitor B956. Cancer Res. 55: 5310-5314; 1995.
15. Toyo'oka, T.; Imai, K. New fluorogenic reagent having halogenobenzofurazan structure for thiols: 4-(aminosulfonyl)-7-fluoro-2,1, 3-benzoxadiazole. Anal. Chem. 56:2461-2464; 1984.
16. James, G.; Goldstein, J. L.; Brown, M. S. Resistance of K-RasBV12 proteins to farnesyltransferase inhibitors in Rat1 cells. Proc. Natl. Acad. Sci. USA 93:4454-4458; 1996.
17. Liu, M.; Bryant, M. S.; Chen, J.; Lee, S.; Yaremko, B.; Lipari, P.; Malkowski, M.; Ferrari, E.; Nielsen, L.; Prioli, N.; Dell, J.; Sinha, D.; Syed, J.; Korfmacher, W. A.; Nomeir, A. A.; Lin, C-C.; Wang, L.; Taveras, A. G.; Doll, R. J.; Njoroge, G.; Mallams, A. K.; Remiszewski, S.; Catino, J. J.; Girijavallabhan, V. M.; Kirschemeier, P.; Bishop, W. R. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res. 58:4947-4956; 1998.
18. Thissen, J. A.; Gross, J. M.; Subramanian, K.; Meyer, T.; Casey, P. J. Prenylation-dependent association of Ki-Ras with microtubules. Evidence for a role in subcellular trafficking. J. Biol. Chem. 272:30362-30370; 1997.
19. Omer, C. A.; Chen, Z.; Diehl, R. E.; Conner, M. W.; Chen, H. Y.; Trumbauer, M. E.; Gopal-Truter, S.; Seeburger, G.; Bhimnathwala, H.; Abrams, M. T.; Davide, J. P.; Ellis, M. S.; Gibbs, J. B.; Greenberg, I.; Koblan, K. S.; Kral, A. M.; Liu, D.; Lobell, R. B.; Miller, P. J.; Mosser, S. D.; O'Neill, T. J.; Rands, E.; Schaber, M. D.; Senderak, E. T.; Oliff, A.; Kohl, N. E. Mouse mammary tumor virus-Ki-rasB transgenic mice develop mammary carcinomas that can be growth-inhibited by a farnesyl:protein transferase inhibitor. Cancer Res. 60:2680-2688; 2000.
20. James, G. L.; Goldstein, J. L.; Brown, M. S.; Rawson, T. E.; Somers, T. C.; McDowell, R. S.; Crowley, C. W.; Lucas, B.K.; Levinson, A. D.; Marsters, J. C., Jr. Benzodiazepine peptidomimetics: Potent inhibitors of Ras farnesylation in animal cells. Science 260: 1937-1942; 1993.
21. Prendergast, G. C.; Davide, J. P.; deSolms, S. J.; Giuliani, E. A.; Graham, S. L.; Gibbs, J. B.; Oliff, A.; Kohl, N. E. Farnesyltransferase inhibition causes morphological reversion of ras-transformed cells by a complex mechanism that involves regulation of the actin cytoskeleton. Mol. Cell. Biol. 14:4193-4202; 1994.
22. Kohl, N. E.; Omer, C. A.; Conner, M. W.; Anthony, N. J.; Davide, J. P.; DeSolms, S. J.; Giuliani, E. A.; Gomez, R. P.; Graham, S. L.; Hamilton, K.; Handt, L. K.; Hartman, G. D.; Koblan, K. S.; Kral, A. M.; Miller, P. J.; Mosser, S. D.; O'Neill, T. J.; Rands, E.; Schaber, M. D.; Gibbs, J. B.; Oliff, A. Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice. Nat. Med. 1:792-797; 1995.
23. Lebowitz, P. F.; Sakamuro, D.; Prendergast, G. C. Farnesyl transferase inhibitors induce apoptosis of Ras-transformed cells denied substratum attachment. Cancer Res. 57:708-713; 1997.
24. Yeung, S. C.; Xu, G.; Pan, J.; Christgen, M.; Bamiagis, A. Manumycin enhances the cytotoxic effect of paclitaxel on anaplastic thyroid carcinoma cells. Cancer Res. 60:650-656; 2000.
25. Sun, J.; Blaskovich, M. A.; Knowles, D.; Qian, Y.; Ohkanda, J.; Bailey, R. D.; Hamilton, A. D.; Sebti, S. M. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: Combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 59:4919-4926; 1999.
26. Blagosklonny, M. V.; Schulte, T. W.; Nguyen, P.; Mimnaugh, E. G.; Trepel, J.; Neckers, L. Paclitaxel induction of p21WAF1 and p53 requires c-raf-1. Cancer Res. 55:4623-4626; 1995.
27. Blagosklonny, M. V.; Schulte, T.; Nguyen, P.; Trepel, J.; Neckers, L. Paclitaxel-induced apoptosis and phosphorylation of Bcl-2 protein involves c-Raf-1 and represents a novel c-Raf-1 signal transduction pathway. Cancer Res. 56:1851-1854; 1996.
28. Blagosklonny, M. V.; Giannakakou, P.; el-Deiry, W. S.; Kingston, D. G.; Higgs, P. I.; Neckers, L.; Fojo, T. Raf-1/bcl-2 phosphorylation: A step from microtubule damage to cell death. Cancer Res. 57:130-135; 1997.
29. Moasser, M. M.; Sepp-Lorenzino, L.; Kohl, N. E.; Oliff, A.; Balog, A.; Su, D. S.; Danishefsky, S. J.; Rosen, N. Farnesyl transferase inhibitors cause enhanced mitotic sensitivity to paclitaxel and epothilones. Proc. Natl. Acad. Sci. USA 95:1369-1374; 1998.