High-content assay to study protein prenylation

Journal of Biomolecular Screening

Volumn 13, Issue 6, 2008, Pages 456-467

  Simonen, Marjo ^a,b   Ibig Rehm, Yvonne ^a   Hofmann, Gabriele ^a   Zimmermann, Johann ^a   Albrecht, Genevieve ^a   Magnier, Maxime ^a   Heidinger, Valerie ^a   Gabriel, Daniela ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b WSJ 350312 ^*  (Switzerland)

Author keywords

Green fluorescent protein (GFP); High content analysis; Mevalonate pathway; Plasma membrane localization; Protein prenylation

Indexed keywords

COMPACTIN; DIMETHYLALLYLTRANSFERASE; GERANYLTRANSFERASE; GREEN FLUORESCENT PROTEIN; ISOPRENOID; MEVALONIC ACID; SMALL INTERFERING RNA; ZOLEDRONIC ACID;

ANALYTIC METHOD; ARTICLE; ASSAY; CELL COUNT; CELL MEMBRANE; CONTROLLED STUDY; HUMAN; HUMAN CELL; IMAGE ANALYSIS; MICROSCOPY; NUCLEOTIDE SEQUENCE; ONCOGENE H RAS; PRENYLATION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN LOCALIZATION; VALIDATION PROCESS;

CELL LINE, TUMOR; CELL MEMBRANE; DIMETHYLALLYLTRANSTRANSFERASE; DIPHOSPHONATES; ENZYME INHIBITORS; GENES, REPORTER; GERANYLTRANSTRANSFERASE; GREEN FLUORESCENT PROTEINS; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; IMIDAZOLES; LUCIFERASES; METHIONINE; MEVALONIC ACID; PROTEIN PRENYLATION; RAS PROTEINS; REPRODUCIBILITY OF RESULTS; RNA, SMALL INTERFERING; TRANSFECTION;

EID: 46149124549     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057108318757     Document Type: Article

References (41)

1. Roskoski R. Jr: Protein prenylation: a pivotal posttranslational process. Biochem Biophys Res Commun 2003 ; 303: 1-7.
2. Der CJ, Krontiris TG, Cooper GM: Transforming genes of human bladder and lung carcinoma cell lines are homologous to the ras genes of Harvey and Kirsten sarcoma viruses. Proc Natl Acad Sci USA 1982 ; 79: 3637-3640.
3. Scharovsky OG, Rozados VR, Gervasoni SI, Matar P.: Inhibition of ras oncogene: a novel approach to antineoplastic therapy. J Biomed Sci 2000 ; 7: 292-298.
4. Tamanoi F., Gau CL, Jiang C., Edamatsu H., Kato-Stankiewicz J.: Protein farnesylation in mammalian cells: effects of farnesyltransferase inhibitors on cancer cells. Cell Mol Life Sci 2001 ; 58: 1636-1649.
5. Perrin D., Hill BT: Tomorrow's anticancer agents: inhibitors of Ras farnesylation. EXS 2000 ; 89: 153-179.
6. Cohen LH, Pieterman E., van Leeuwen RE, Overhand M., Burm BE, van der Marel GA,, et al. Inhibitors of prenylation of Ras and other G-proteins and their application as therapeutics. Biochem Pharmacol 2000 ; 60: 1061-1068.
7. Swanson KM, Hohl RJ: Anti-cancer therapy: targeting the mevalonate pathway. Curr Cancer Drug Targets 2006 ; 6: 15-37.
8. Bergstrom JD, Bostedor RG, Masarachia PJ, Reszka AA, Rodan G.: Alendronate is a specific, nanomolar inhibitor of farnesyl diphosphate synthase. Arch Biochem Biophys 2000 ; 373: 231-241.
9. Dunford JE, Thompson K., Coxon FP, Luckman SP, Hahn FM, Poulter CD,, et al. Structure-activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates. J Pharmacol Exp Ther 2001 ; 296: 235-242.
10. Keller RK, Fliesler SJ: Mechanism of aminobisphosphonate action: characterization of alendronate inhibition of the isoprenoid pathway. Biochem Biophys Res Commun 1999 ; 266: 560-563.
11. van Beek E., Pieterman E., Cohen L., Lowik C., Papapoulos S.: Farnesyl pyrophosphate synthase is the molecular target of nitrogen-containing bisphosphonates. Biochem Biophys Res Commun 1999 ; 264: 108-111.
12. Conte P., Guarneri V.: Safety of intravenous and oral bisphosphonates and compliance with dosing regimens. Oncologist 2004 ; 9 (suppl 4). 28-37.
13. van Beek ER, Lowik CW, Ebetino FH, Papapoulos SE: Binding and antiresorptive properties of heterocycle-containing bisphosphonate analogs: structure-activity relationships. Bone 1998 ; 23: 437-442.
14. Konstantinopoulos PA, Karamouzis MV, Papavassiliou AG: Post-translational modifications and regulation of the RAS superfamily of GTPases as anticancer targets. Nat Rev Drug Discov 2007 ; 6: 541-555.
15. Thompson K., Rogers MJ, Coxon FP, Crockett JC: Cytosolic entry of bisphosphonate drugs requires acidification of vesicles after fluid-phase endocytosis. Mol Pharmacol 2006 ; 69: 1624-1632.
16. Luckman SP, Coxon FP, Ebetino FH, Russell RG, Rogers MJ: Heterocycle-containing bisphosphonates cause apoptosis and inhibit bone resorption by preventing protein prenylation: evidence from structure-activity relationships in J774 macrophages. J Bone Miner Res 1998 ; 13: 1668-1678.
17. Boijoux O., Boutonnet C., Giamarchi C., Favre G., Vagner S., Faye JC: Chemical-based translational induction of luciferase expression: an efficient tool for in vivo screening of protein farnesylation inhibitors. Mol Pharmacol 2005 ; 67: 1829-1833.
18. Choy E., Chiu VK, Silletti J., Feoktistov M., Morimoto T., Michaelson D.,, et al. Endomembrane trafficking of ras: the CAAX motif targets proteins to the ER and Golgi. Cell 1999 ; 98: 69-80.
19. Hancock JF, Magee AI, Childs JE, Marshall CJ: All ras proteins are polyisoprenylated but only some are palmitoylated. Cell 1989 ; 57: 1167-1177.
20. Willumsen BM, Cox AD, Solski PA, Der CJ, Buss JE: Novel determinants of H-Ras plasma membrane localization and transformation. Oncogene 1996 ; 13: 1901-1909.
21. Mikic I., Planey S., Zhang J., Ceballos C., Seron T., von Massenbach B.,, et al. A live cell, image-based approach to understanding the enzymology and pharmacology of 2-bromopalmitate and palmitoylation. Methods Enzymol 2006 ; 414: 150-187.
22. Bivona TG, Quatela S., Philips MR: Analysis of ras activation in living cells with GFP-RBD. Methods Enzymol 2005 ; 407: 128-143.
23. Lommerse PH, Snaar-Jagalska BE, Spaink HP, Schmidt T.: Single-molecule diffusion measurements of H-Ras at the plasma membrane of live cells reveal microdomain localization upon activation. J Cell Sci 2005 ; 118: 1799-1809.
24. Rocks O., Peyker A., Kahms M., Verveer PJ, Koerner C., Lumbierres M.,, et al. An acylation cycle regulates localization and activity of palmitoylated Ras isoforms. Science 2005 ; 307: 1746-1752.
25. Vita F., Soranzo MR, Borelli V., Bertoncin P., Zabucchi G.: Subcellular localization of the small GTPase Rab5a in resting and stimulated human neutrophils. Exp Cell Res 1996 ; 227: 367-373.
26. Ward SM, Gadbut AP, Tang D., Papageorge AG, Wu L., Li G.,, et al. TGFbeta regulates the expression of G alpha(i2) via an effect on the localization of ras. J Mol Cell Cardiol 2002 ; 34: 1217-1226.
27. Corish P., Tyler-Smith C.: Attenuation of green fluorescent protein half-life in mammalian cells. Protein Eng 1999 ; 12: 1035-1040.
28. Knight LA, Conroy M., Fernando A., Polak M., Kurbacher CM, Cree IA: Pilot studies of the effect of zoledronic acid (Zometa) on tumor-derived cells ex vivo in the ATP-based tumor chemosensitivity assay. Anticancer Drugs 2005 ; 16: 969-976.
29. Senaratne SG, Pirianov G., Mansi JL, Arnett TR, Colston KW: Bisphosphonates induce apoptosis in human breast cancer cell lines. Br J Cancer 2000 ; 82: 1459-1468.
30. Glickman JF, Schmid A.: Farnesyl pyrophosphate synthase: real-time kinetics and inhibition by nitrogen-containing bisphosphonates in a scintillation assay. Assay Drug Dev Technol 2007 ; 5: 205-214.
31. Fleisch H.: Bisphosphonates: mechanisms of action. Expert Opin Ther Patents 2001 ; 11: 1371-1381.
32. Green JR, Clay V., Richardson J., Hassan IF: The effect of zoledronate and pamidronate on the intestinal permeability barrier in vitro and in vivo. Int J Pharm 1997 ; 153: 59-66.
33. Park EJ, Lee D., Shin YG, Lantvit DD, van Breemen RB, Kinghorn AD,, et al. Analysis of 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors using liquid chromatography-electrospray mass spectrometry. J Chromatogr B Biomed Sci Appl 2001 ; 754: 327-332.
34. Shi Y., Gera J., Hsu JH, Van Ness B., Lichtenstein A.: Cytoreductive effects of farnesyl transferase inhibitors on multiple myeloma tumor cells. Mol Cancer Ther 2003 ; 2: 563-572.
35. Qian Y., Marugan JJ, Fossum RD, Vogt A., Sebti SM, Hamilton AD: Probing the hydrophobic pocket of farnesyltransferase: aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors. Bioorg Med Chem 1999 ; 7: 3011-3024.
36. El Oualid F., Cohen LH, van der Marel GA, Overhand M.: Inhibitors of protein: geranylgeranyl transferases. Curr Med Chem 2006 ; 13: 2385-2427.
37. Vasudevan A., Qian Y., Vogt A., Blaskovich MA, Ohkanda J., Sebti SM, et al: Potent, highly selective, and non-thiol inhibitors of protein geranylgeranyltransferase-I J Med Chem 1999 ; 42: 1333-1340.
38. Whyte DB, Kirschmeier P., Hockenberry TN, Nunez-Oliva I., James L., Catino JJ,, et al. K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors. J Biol Chem 1997 ; 272: 14459-14464.
39. Coxon FP, Helfrich MH, Van't Hof R., Sebti S., Ralston SH, Hamilton A.,, et al. Protein geranylgeranylation is required for osteoclast formation, function, and survival: inhibition by bisphosphonates and GGTI-298 J Bone Miner Res 2000 ; 15: 1467-1476.
40. Gelb MH, Brunsveld L., Hrycyna CA, Michaelis S., Tamanoi F., Van Voorhis WC,, et al. Therapeutic intervention based on protein prenylation and associated modifications. Nat Chem Biol 2006 ; 2: 518-528.
41. Vogt A., Sun J., Qian Y., Hamilton AD, Sebti SM: The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner J Biol Chem 1997 ; 272: 27224-27229.