Farnesylthiosalicylic acid: Inhibition of proliferation and enhancement of apoptosis of hormone-dependent breast cancer cells

Anti-Cancer Drugs

Volumn 17, Issue 1, 2006, Pages 33-40

  Santen, Richard J ^a   Lynch, Amanda R ^a   Neal, Lindsey R ^a   McPherson, Robert A ^a,b   Yue, Wei ^a  

^a UNIVERSITY OF VIRGINIA HEALTH SYSTEM   (United States)

^b UNIVERSITY OF QUEENSLAND   (Australia)

Author keywords

Apoptosis; Breast cancer; Cyclodextrin; Farnesylthiosalicylic acid; Ras

Indexed keywords

FARNESYLTHIOSALICYLIC ACID; PROTEIN FARNESYLTRANSFERASE INHIBITOR; RAS PROTEIN;

APOPTOSIS; ARTICLE; BREAST CANCER; CANCER GROWTH; CELL PROLIFERATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG INHIBITION; ENZYME LINKED IMMUNOSORBENT ASSAY; HUMAN; HUMAN CELL; PRIORITY JOURNAL; XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; BREAST NEOPLASMS; CELL LINE, TUMOR; CELL PROLIFERATION; CYCLODEXTRINS; DOSE-RESPONSE RELATIONSHIP, DRUG; ESTRADIOL; FARNESOL; FEMALE; HUMANS; INJECTIONS, INTRAPERITONEAL; MAMMARY NEOPLASMS, EXPERIMENTAL; MICE; MICE, NUDE; NEOPLASMS, HORMONE-DEPENDENT; RAS PROTEINS; SALICYLIC ACIDS; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 33646079383     PISSN: 09594973     EISSN: None     Source Type: Journal    
DOI: 10.1097/01.cad.0000185184.64980.39     Document Type: Article

References (47)

1. Santen RJ, Manni A, Harvey H, Redmond C. Endocrine treatment of breast cancer in women. Endocr Rev 1990; 11:221-265.
2. Early Breast Cancer Collaborative Group. Tamoxifen for early breast cancer: an overview of the randomized trials. Lancet 1998; 351:1451-1467.
3. Santen RJ. Long term tamoxifen therapy: can an antagonist become an agonist? J Clin Endocrinol Metab 1997; 81:2027-2029.
4. Horwitz KB. When tamoxifen turns bad. Endocrinology 1995; 136:821-823.
5. Ali A, Coombes RC. Endocrine-responsive breast cancer and strategies for combating resistance. Nat Rev Cancer 2002; 2:101-112.
6. Katzenellenbogen BS, Montano MM, Ekena K, Herman ME, McInerney EM. Antiestrogens: mechanisms of action and resistance in breast cancer. Breast Cancer Res Treat 1997; 44:22-38.
7. Schiff R, Massarweh S, Shou J, Osborne CK. Breast cancer endocrine resistance: how growth factor signaling and estrogen receptor coregulators modulate response. Clin Cancer Res 2003; 9 (1 pt 2):447S-4454S.
8. King RJ, Darbre PD. Interaction of growth factors during progression towards steroid independence in T-47-D human breast cancer cells. J Cell Biochem 1990; 43:199-211.
9. Nicholson RI, Hutcheson IR, Knowlden JM, Jones HE, Harper ME, Jordan N, et al. Non-endocrine pathways and endocrine resistance: observations with anti-oestrogens and signal transduction inhibitors in combination. Clin Cancer Res 2004; 10:346s-354s.
10. Nicholson RI, Hutcheson IR, Harper ME, Knowlden JM, Barrow D, McClelland RA. et al. Modulation of epidermal growth factor receptor in endocrine-resistant, oestrogen receptor-positive breast cancer. Endocr Relat Cancer 2001; 8:175-182.
11. Knowlden JM, Hutcheson IR, Jones HE, Madde T, Gee JM, Harper ME, et al. Elevated levels of epidermal growth factor receptor/c-erbB2 heterodimers mediate an autocrine growth regulatory pathway in tamoxifen-resistant MCF-7 cells. Endocrinology 2003; 144:1032-1044.
12. Schiff R, Massarweh SA, Shou J, Bharwani L, Mohsin SH, Osborne CK. Cross-talk between estrogen receptor and growth factor pathways as a molecular target for overcoming endocrine resistance. Clin Cancer Res 2004; 10:t6S.
13. Johnston SR, Head J, Pancholi S, Detre S, Martin LA, Smith IE, et al. Integration of signal transduction inhibitors with endocrine therapy: an approach to overcoming hormone resistance in breast cancer. Clin Cancer Res 2003; 9:t32S.
14. Joneson T, Bar-Sagi D. Ras effectors and their role in mitogenesis and oncogenesis. J Mol Med 1997; 75:587-593.
15. Dinsmore CJ, Bell IM. Inhibitors of farnesyltransferase and geranylgeranyltransferase-I for antitumor therapy: substrate based design, conformational constraint and biological activity. Curr Top Med Chem 2003; 3:1075-1093.
16. Prendergast GC. Farnesyltransferase inhibitors: antineoplastic mechanism and clinical prospects. Curr Opin Cell Biol 2000; 12:166-173.
17. Elad-Sfadia G, Haklai R, Ballan E, Gabius HJ, Kloog Y. Galectin-1 augments Ras activation and diverts Ras signals to Raf-1 at the expense of phosphoinositide 3-kinase. J Biol Chem 2002; 277:37169-37175.
18. Marom M, Haklai R, Ben-Baruch G, Marciano D, Egozi Y, Kloog Y. Selective inhibition of Ras-dependent cell growth by farnesylthiosalicylic acid. J Biol Chem 1995; 270:22268-22270.
19. Egozi Y, Weisz B, Gana-Weisz M, Ben-Baruch G, Kloog Y. Growth inhibition of ras-dependent tumors in nude mice by a potent ras-dislodging antagonist. Int J Cancer 1999; 80:911-918.
20. Weisz B, Giehl K, Gana-Weisz M, Egoz Y, Ben Baruch, Marciano G, et al. A new functional Ras antagonist inhibits human pancreatic tumor growth in nude mice. Oncogene 1999; 18:2579-2588.
21. Jansen B, Schlagbauer-Wadl H, Kahr H, Heere-Ress E, Mayer BX, et al. Novel Ras antagonist blocks human melanoma growth. Proc Natl Acad Sci USA 1999; 96:14019-14024.
22. Halaschek-Wiener, Wacheck JV, Schlagbauer-Wadl H, Wolff K, Kloog Y, Jansen B. A novel Ras antagonist regulates both oncogenic Ras and the tumor suppressor p53 in colon cancer cells. Mol Med 2000; 6:693-704.
23. Gana-Weisz M, Haklai R, Marciano D, Egozi Y, Ben Baruch G, Kloog Y. The Ras antagonist S-farnesylthiosalicylic acid induces inhibition of MAPK activation. Biochem Biophys Res Commun 1997; 239:900-904.
24. Gana-Weisz M, Halaschek-Wiener J, Jansen B, Elad G, Haklai R, Kloog Y. The Ras inhibitor S-trans,trans-farnesylthiosalicylic acid chemosensitizes human tumor cells without causing resistance. Clin Cancer Res 2002; 8:555-565.
25. Rotblat B, Niv H, Andre S, Kaltner H, Gabius HJ, Kloog Y. Galectin-1(L11A) predicted from a computed galectin-1 farnesyl-binding pocket selectively inhibits Ras-GTP. Cancer Res 2004; 64:3112-3118.
26. Aharonson Z, Gana-Weisz M, Varsano T, Haklai R, Marciano D, Kloog Y. Stringent structural requirements for anti-Ras activity of S-prenyl analogues. Biochim Biophys Acta 1998; 1406:40-50.
27. Elad G, Paz A, Haklai R, Marciano D, Cox A, Kloog Y. Targeting of K-Ras 4B by S-trans,trans-farnesyl thiosalicylic acid. Biochim Biophys Acta 1999; 1452:228-242.
28. Pearson G, Robinson F, Gibson TB, Xu BE, Karandikar M, Berman K, et al. Mitogen activated protein (MAP) kinase pathways: regulation and physiological functions. Endocr Rev 2001; 22:153-183.
29. Yue W, Wang JP, Conaway M, Li Y, Santen RJ. Adaptive hypersensitivity following long-term estrogen deprivation: involvement of multiple signal pathways. J Steroid Biochem Mol Biol 2003; 86:265-274.
30. Jeng MH, Yue W, Eischeid A, Wang JP, Santen RJ. Role of MAPK in the enhanced cell proliferation of long term estrogen deprived human breast cancer cells. Breast Cancer Res Treat 2000; 62:167-175.
31. Santen RJ, Song RX, McPherson R, Kumar R, Adam L, Jeng MH, et al. The role of mitogen-activated protein (MAP) kinase in breast cancer. J Steroid Biochem Mol Biol 2002; 80:239-256.
32. Masamura S, Santner SJ, Heitjan DF, Santen RJ. Estrogen deprivation causes estradiol hypersensitivity in human cancer cells. J Clin Endocrinol Metab 1995; 80:2918-2925.
33. Fiennes AG, Walton J, Winterbourne D, McGlashan D, Hermon-Taylor J. Quantitative correlation of neutral red dye uptake with cell number in human cancer cell cultures. Cell Biol Int Rep 1987; 11:373-378.
34. Shim WS, Conaway M, Masamura S, Yue W, Wang JP, Santen RJ. Estradiol hypersensitivity and MAPK expression in long term deprived human breast cancer cells in vivo. Endocrinology 2000; 141:396-405.
35. Pitha J, Gerloczy A, Olivi A. Parenteral hydroperoxypropyl cyclodextrins: intravenous and intracerebral administration of lipophiles. J Pharm Sci 1994; 83:833-837.
36. Sebolt-Leopold JS. MEK inhibitors: a therapeutic approach to targeting the Ras-MAPK pathway in tumors. Curr Pharm Des 2004; 10:1907-1914.
37. Cox AD, Der CJ. The dark side of Ras: regulation of apoptosis. Oncogene 2003; 22:8999-9006.
38. Daly RJ, Darbre PD. Cellular and molecular events in loss of estrogen sensitivity in ZR-75-1 and T-47-D human breast cancer cells. Cancer Res 1990; 50:5868-5875.
39. Brunner N, Boulay V, Fojo A, Freter CE, Lippman ME, Clarke R. Acquisition of hormone-independent growth in MCF-7 cells is accompanied by increased expression of estrogen-regulated genes but without detectable DNA amplifications. Cancer Res 1993; 53:283-290.
40. Martin LA, Farmer I, Johnston SR, Ali S, Marshall C, Dowsett M. Enhanced estrogen receptor (ER) alpha, ERBB2, and MAPK signal transduction pathways operate during the adaptation of MCF-7 cells to long term estrogen deprivation. J Biol Chem 2003; 278:30458-30468.
41. Yue W, Wang JP, Conaway M, Masamura S, Li Y, Santen RJ. Activation of the MAPK pathway enhances sensitivity of MCF-7 breast cancer cells to the mitogenic effect of estradiol. Endocrinology 2002; 143:3221-3229.
42. Yue W, Wang JP, Li Y, Fan P, Santen RJ. Farnesylthiosalicylic acid blocks mammalian target of rapamycin signaling in breast cancer cells. Int J Cancer 2005; 117:746-754.
43. McMahon LP, Yue W, Santen RJ, Lawrence Jr. JC. Farnesylthiosalicylic acid inhibits mTOR activity both in cells and in vitro by promoting dissociation of the mTOR-raptor complex. Mol Endocrinol 2005; 19:175-183.
44. Pitha J, Irie T, Sklar PB, Nye JS. Drug solubilizers to aid pharmacologists: amorphous cyclodextrin derivatives. Life Sci 1988; 43:493-502.
45. Stella VJ, Rajewsk RA. Cyclodextrins: their future in drug formulation and delivery. Pharm Res 1997; 14:556-557.
46. Cip1. Mol Cell 2003; 11:1491-1501.
47. Matsuura H, Nishitoh H, Takeda K, Matsuzawa A, Amagasa T, Ito M, et al. Phosphorylation-dependent scaffolding role of JSAP1/JIP3 in the ASK1-JNK signaling pathway. A new mode of regulation of the MAPK cascade. J Biol Chem 2002; 77:40703-40709.