Characterization of a human carcinoma cell line selected for resistance to the farnesyl transferase inhibitor 4-(2-(4-(8-chloro-3,10-dibromo-6,11-dihydro- 5H-benzo-(5,6)-cyclohepta(1,2-b)-pyridin-11(R)-yl)-1-piperidinyl)-2-oxo-ethyl) -1-piperidinecarboxamide (SCH66336)

Molecular Pharmacology

Volumn 68, Issue 2, 2005, Pages 477-486

  Bruzek, Laura M ^a   Poynter, Jenny N ^a   Kaufmann, Scott H ^a   Adjei, Alex A ^a  

^a MAYO CLINIC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2 AMINO 3 METHOXYPHENYL)CHROMONE; CISPLATIN; GEMCITABINE; LONAFARNIB; MAMMALIAN TARGET OF RAPAMYCIN; MITOGEN ACTIVATED PROTEIN KINASE KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE KINASE 2; N [[5 [(2 AMINO 3 MERCAPTOPROPYL)AMINO][1,1' BIPHENYL] 2 YL]CARBONYL]METHIONINE METHYL ESTER; PACLITAXEL; PHOSPHOTRANSFERASE INHIBITOR; PROTEIN FARNESYLTRANSFERASE INHIBITOR; PROTEIN INHIBITOR; PROTEIN KINASE B; PROTEIN KINASE B BETA; RAPAMYCIN; S6 KINASE;

ARTICLE; CANCER CELL CULTURE; CARCINOMA CELL; CELL STRAIN HCT116; COLORECTAL CARCINOMA; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EXPOSURE; DRUG INHIBITION; DRUG SELECTIVITY; DRUG SENSITIZATION; DRUG UPTAKE; ENZYME ACTIVATION; ENZYME INHIBITION; EXPERIMENT; HUMAN; HUMAN CELL; IMMUNOBLOTTING; INHIBITION KINETICS; PHOSPHORYLATION; PRIORITY JOURNAL; SIGNAL TRANSDUCTION; STANDARD;

ALKYL AND ARYL TRANSFERASES; CARCINOMA; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG RESISTANCE, NEOPLASM; ENZYME INHIBITORS; FARNESYLTRANSTRANSFERASE; HCT116 CELLS; HUMANS; PIPERIDINES; PYRIDINES;

EID: 23044465584     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.104.010074     Document Type: Article

References (38)

1. Adjei AA (2003) Farnesyltransferase inhibitors, in Cancer Chemotherapy and Biologic Response Modifiers Annual 21 (Giaccone G and Sondel P eds) pp 127-144, Elsevier Science, B.V., Amsterdam.
2. Adjei AA, Davis JN, Erlichman C, Svingen PA, and Kaufmann SH (2000a) Comparison of potential markers of farnesyltransferase inhibition. Clin Cancer Res 6:2318-2325.
3. Adjei AA, Erlichman C, Davis JN, Cutler DL, Sloan JA, Marks RS, Hanson LJ, Svingen PA, Atherton P, Bishop WR, et al. (2000b) A Phase I trial of the farnesyltransferase inhibitor SCH66336: evidence for biological and clinical activity. Cancer Res 60:1871-1877.
4. Ashar HR, James L, Gray K, Carr D, Black S, Armstrong L, Bishop WR, and Kirschmeier P (2000) Farnesyl transferase inhibitors block the farnesylation of CENP-E and CENP-F and alter the association of CENP-E with the microtubules. J Biol Chem 275:30451-30457.
5. Bjornsti MA and Houghton PJ (2004) The TOR pathway: a target for cancer therapy. Nat Rev Cancer 4:335-348.
6. Bradford MM (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
7. Britten CD, Rowinsky E, Yao S, Soignet S, Rosen N, Eckhardt SG, Drengler R, Hammond L, Siu LL, Smith L, et al. (1999) The farnesyl protein transferase (FPTase) inhibitor L-778,123 in patients with solid cancers (Abstract 597). Proc Am Soc Clin Oncol 18:155A
8. Brognard J, Clark AS, Ni Y, and Dennis PA (2001) Akt/protein kinase B is constitutively active in non-small cell lung cancer cells and promotes cellular survival and resistance to chemotherapy and radiation. Cancer Res 61:3986-3997.
9. Chun KH, Lee HY, Hassan K, Khuri F, Hong WK, and Lotan R (2003) Implication of protein kinase B/Akt and Bcl-2/Bcl-XL suppression by the farnesyl transferase inhibitor SCH66336 in apoptosis induction in squamous carcinoma cells. Cancer Res 63:4796-4800.
10. Clarke S (1992) Protein isoprenylation and methylation at carboxyl-terminal cysteine residues. Annu Rev Biochem 61:355-386.
11. Datta SR, Brunet A, and Greenberg ME (1999) Cellular survival: a play in three Akts. Genes Dev 13:2905-2927.
12. Del Villar K, Urano J, Guo L, and Tamanoi F (1999) A mutant form of human protein farnesyltransferase exhibits increased resistance to farnesyltransferase inhibitors. J Biol Chem 274:27010-27017.
13. Downward J (1998) Ras signalling and apoptosis. Curr Opin Genet Dev 8:49-54.
14. Du W and Prendergast GC (1999) Geranylgeranylated RhoB mediates suppression of human tumor cell growth by farnesyltransferase inhibitors. Cancer Res 59:5492-5496.
15. Dudley DT, Pang L, Decker SJ, Bridges AJ, and Saltiel AR (1995) A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci USA 91:7686-7689.
16. Eskens FA, Awada A, Cutler DL, de Jonge MJ, Luyten GP, Faber MN, Statkevich P, Sparreboom A, Verweij J, Hanauske AR, et al. (2001) Phase I and pharmacokinetic study of the oral farnesyl transferase inhibitor SCH 66336 given twice daily to patients with advanced solid tumors. J Clin Oncol 19:1167-1175.
17. Gibbs JB, Pompliano DL, Mosser SD, Rands E, Lingham RB, Singh SB, Scolnick EM, Kohl NE, and Oliff A (1993) Selective inhibition of farnesyl-protein transferase blocks ras processing in vivo. J Biol Chem 268:7617-7620.
18. Haluska P, Dy GK, and Adjei AA (2002) Farnesyl transferase inhibitors as anticancer agents. Eur J Cancer 38:1685-1700.
19. Harlow E and Lane D (1988) Antibodies: A Laboratory Manual. Cold Spring Harbor Laboratory Press, Cold Spring Harbor, NY.
20. Jiang K, Coppola D, Crespo NC, Nicosia SV, Hamilton AD, Sebti SM, and Cheng JQ (2000) The phosphoinositide 3-OH kinase/AKT2 pathway as a critical target for farnesyltransferase inhibitor-induced apoptosis. Mol Cell Biol 20:139-148.
21. Karp JE, Lancet JE, Kaufmann SH, End DW, Wright JJ, Bol K, Horak I, Tidwell ML, Liesveld J, Kottke TJ, et al. (2001) Clinical and biologic activity of the farnesyltransferase inhibitor R115777 in adults with refractory and relapsed acute leukemias: a phase 1 clinical-laboratory correlative trial. Blood 97:3361-3369.
22. Kato K, Cox AD, Hisaka MM, Graham SM, Buss JE, and Der CJ (1992) Isoprenoid addition to Ras protein is the critical modification for its membrane association and transforming activity. Proc Natl Acad Sci USA 89:6403-6407.
23. Kaufmann SH (1989) Additional members of the rat liver lamin polypeptide family: structural and immunological characterization. J Biol Chem 264:13946-13955.
24. Kaufmann SH (2001) Reutilization of immunoblots after chemiluminescent detection. Anal Biochem 296:283-286.
25. Kaufmann SH, Svingen PA, Gore SD, Armstrong DK, Cheng YC, and Rowinsky EK (1997) Altered formation of topotecan-stabilized topoisomerase I-DNA adducts in human leukemia cells. Blood 89:2098-2104.
26. Kohl NE, Mosser SD, deSolms SJ, Giuliani EA, Pompliano DL, Graham SL, Smith RL, Scolnick EM, Oliff A, and Gibbs JB (1993) Selective inhibition of ras-dependent transformation by a farnesyltransferase inhibitor. Science (Wash DC) 260:1934-1937.
27. Lange-Carter CA, Pleiman CM, Gardner AM, Blumer KJ, and Johnson GL (1993) A divergence in the MAP kinase regulatory network defined by MEK kinase and Raf. Science (Wash DC) 260:315-319.
28. Lebowitz PF, Sakamuro D, and Prendergast GC (1997) Farnesyl transferase inhibitors induce apoptosis of Ras-transformed cells denied substratum attachment. Cancer Res 57:708-713.
29. Lerner EC, Qian Y, Blaskovich MA, Fossum RD, Vogt A, Sun J, Cox AD, Der CJ, Hamilton AD, and Sebti SM (1995) Ras CAAX peptidomimetic FTI-277 selectively blocks oncogenic Ras signaling by inducing cytoplasmic accumulation of inactive Ras-Raf complexes. J Biol Chem 270:26802-26806.
30. Nave BT, Ouwens M, Withers DJ, Alessi DR, and Shepherd PR (1999) Mammalian target of rapamycin is a direct target for protein kinase B: identification of a convergence point for opposing effects of insulin and amino-acid deficiency on protein translation. Biochem J 344:427-431.
31. Neshat MS, Mellinghoff IK, Tran C, Stiles B, Thomas G, Petersen R, Frost P, Gibbons JJ, Wu H, and Sawyers CL (2001) Enhanced sensitivity of PTEN deficient tumors to inhibition of FRAP/mTOR. Proc Natl Acad Sci USA 98:10314-10319.
32. Reynolds THT, Bodine SC, and Lawrence CJ Jr (2002) Control of Ser2448 phosphorylation in the mammalian target of rapamycin by insulin and skeletal muscle load. J Biol Chem 277:17657-17662.
33. Samowitz WS, Curtin K, Schaffer D, Robertson M, Leppert M, and Slattery ML (2000) Relationship of Ki-ras mutations in colon cancers to tumor location, stage and survival: a population-based study. Cancer Epidemiol Biomarkers Prev 9:1193-1197.
34. Sinensky M, Fantle K, and Dalton M (1994) An antibody which specifically recognizes prelamin A but not mature lamin A: application to detection of blocks in farnesylation-dependent protein processing. Cancer Res 54:3229-3232.
35. Smith PK, Krohn RI, Hermanson GT, Mallia AK, Gartner FH, Provenzano MD, Fujimoto EK, Goeke NM, Olson BJ, and Klenk DC (1985) Measurement of protein using bicinchoninic acid. Anal Biochem 150:76-85.
36. Smith V, Rowlands MG, Barrie E, Workman P, and Kelland LR (2002) Establishment and characterization of acquired resistance to the farnesyl protein transferase inhibitor R115777 in a human colon cancer cell line. Clin Cancer Res 8:2002-2009.
37. Suzuki N, Urano J, and Tamanoi F (1998) Farnesyltransferase inhibitors induce cytochrome c release and caspase 3 activation preferentially in transformed cells. Proc Natl Acad Sci USA 95:15356-15361.
38. Zhang FL and Casey PJ (1996) Protein prenylation: molecular mechanisms and functional consequences. Annu Rev Biochem 65:241-269.