Characterization of the in vitro activity of AZD3409, a novel prenyl transferase inhibitor

Cancer Chemotherapy and Pharmacology

Volumn 67, Issue 1, 2011, Pages 137-145

  Appels, Natalie M G M ^a   Bolijn, Maria J ^b   Van Eijndhoven, Maria A J ^b   Stephens, Trevor C ^c   Beijnen, Jos H ^a,b,d   Schellens, Jan H M ^b,d  

^a SLOTERVAART HOSPITAL   (Netherlands)

^b ANTONI VAN LEEUWENHOEK HOSPITAL   (Netherlands)

^c ASTRAZENECA   (United Kingdom)

^d UTRECHT UNIVERSITY   (Netherlands)

Author keywords

AZD3409; Farnesyl transferase; Geranylgeranyl transferase; In vitro characterization

Indexed keywords

AZD 3409; CHAPERONE; GERANYLGERANYL TRANSFERASE 1; GGTI 2147; HDJ 2 PROTEIN; KI4B RAS PROTEIN; LONAFARNIB; PROTEIN FARNESYLTRANSFERASE; RAP1 PROTEIN; RAP1A PROTEIN; RAS PROTEIN; TRANSFERASE; TRANSFERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CELL PROLIFERATION; CELL STRAIN MCF 7; CONTROLLED STUDY; DRUG CYTOTOXICITY; EMBRYO; ENZYME INHIBITION; GROWTH INHIBITION; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; MOUSE; NONHUMAN; ONCOGENE H RAS; ONCOGENE RAS; PRIORITY JOURNAL; PROTEIN FARNESYLATION; PROTEIN GERANYLGERANYLATION; PROTEIN MODIFICATION;

ALKYL AND ARYL TRANSFERASES; ANIMALS; CELL LINE, TUMOR; CELL PROLIFERATION; DIMETHYLALLYLTRANSTRANSFERASE; FARNESYLTRANSTRANSFERASE; FIBROBLASTS; HUMANS; IMIDAZOLES; INHIBITORY CONCENTRATION 50; LEUCINE; MICE; MUTATION; PIPERIDINES; PYRIDINES; RAS PROTEINS; TRANSFECTION;

EID: 78651084823     PISSN: 03445704     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00280-010-1300-6     Document Type: Article

References (24)

1. JL Bos 1989 Ras oncogenes in human cancer: a review Cancer Res 49 17 4682 4689 1:CAS:528:DyaL1MXltlWksL4%3D 2547513
2. K Kato AD Cox MM Hisaka SM Graham JE Buss CJ Der 1992 Isoprenoid addition to Ras protein is the critical modification for its membrane association and transforming activity Proc Natl Acad Sci USA 89 14 6403 6407 1:CAS:528:DyaK38Xlt12jtL0%3D 10.1073/pnas.89.14.6403 1631135
3. DB Whyte P Kirschmeier TN Hockenberry I Nunez-Oliva L James JJ Catino WR Bishop JK Pai 1997 K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors J Biol Chem 272 22 14459 14464 1:CAS:528:DyaK2sXjsFygs74%3D 10.1074/jbc.272.22.14459 9162087 (Pubitemid 27232866)
4. NE Kohl MW Conner JB Gibbs SL Graham GD Hartman A Oliff 1995 Development of inhibitors of protein farnesylation as potential chemotherapeutic agents J Cell Biochem Suppl 22 145 150 1:STN:280:DyaK28%2FhtVehtA%3D%3D 10.1002/jcb.240590819 8538192
5. TB Brunner SM Hahn AK Gupta RJ Muschel WG McKenna EJ Bernhard 2003 Farnesyltransferase inhibitors: an overview of the results of preclinical and clinical investigations Cancer Res 63 18 5656 5668 1:CAS:528: DC%2BD3sXnvVSjtrc%3D 14522880
6. M Crul GJ de Klerk JH Beijnen JHM Schellens 2001 Ras biochemistry and farnesyl transferase inhibitors: a literature survey Anticancer Drugs 12 3 163 184 1:CAS:528:DC%2BD3MXislegsrc%3D 10.1097/00001813-200103000-00001 11290863 (Pubitemid 32269912)
7. N Mijimolle J Velasco P Dubus C Guerra CA Weinbaum PJ Casey V Campuzano M Barbacid 2005 Protein farnesyltransferase in embryogenesis, adult homeostasis, and tumor development Cancer Cell 7 4 313 324 1:CAS:528:DC%2BD2MXjvFSkurY%3D 10.1016/j.ccr.2005.03.004 15837621 (Pubitemid 40544649)
8. RB Lobell CA Omer MT Abrams HG Bhimnathwala MJ Brucker CA Buser JP Davide SJ de Solms CJ Dinsmore MS Ellis-Hutchings AM Kral D Liu WC Lumma SV Machotka E Rands TM Williams SL Graham GD Hartman AI Oliff DC Heimbrook NE Kohl 2001 Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models Cancer Res 61 24 8758 8768 1:CAS:528:DC%2BD38Xht1OntQ%3D%3D 11751396
9. JM Bergman MT Abrams JP Davide IB Greenberg RG Robinson CA Buser HE Huber KS Koblan NE Kohl RB Lobell SL Graham GD Hartman TM Williams CJ Dinsmore 2001 Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I Bioorg Med Chem Lett 11 11 1411 1415 1:CAS:528:DC%2BD3MXktVagsL0%3D 10.1016/S0960-894X(01)00240-2 11378366 (Pubitemid 32510832)
10. RB Lobell D Liu CA Buser JP Davide E DePuy K Hamilton KS Koblan Y Lee S Mosser SL Motzel JL Abbruzzese CS Fuchs EK Rowinsky EH Rubin S Sharma PJ Deutsch KE Mazina BW Morrison L Wildonger SL Yao NE Kohl 2002 Preclinical and clinical pharmacodynamic assessment of L-778, 123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I Mol Cancer Ther 1 747 758 1:CAS:528:DC%2BD38XlsFSmtb8%3D 12479371
11. TC Stephens MJ Wardleworth ZS Matusiak SE Ashton UJ Hancox M Bate R Ferguson T Boyle 2003 AZD3409, a novel, oral, protein prenylation inhibitor with promising preclinical antitumor activity Proc Am Assoc Canc Res 44 R4870
12. J Kelly J Dominguez-Ecrig HY Leung TC Stephens DE Neal BR Davies 2005 The prenyltransferase inhibitor AZD3409 has anti-tumor activity in preclinical models of urothelial carcinoma Proc Am Assoc Canc Res 46 5962
13. R Streeper D Campos G Carrizales TC Stephens E Izbicka 2006 Regulation of tumor signaling pathways by AZD3409 in vitro Anticancer Res 26 6B 4185 4189 1:CAS:528:DC%2BD2sXpslCgtw%3D%3D 17201131
14. MR Maiello A D'Alessio A De Luca A Carotenuto AM Rachiglio M Napolitano L Cito A Guzzo N Normanno 2007 AZD3409 inhibits the growth of breast cancer cells with intrinsic resistance to the EGFR tyrosine kinase inhibitor gefitinib Breast Cancer Res Treat 102 3 275 282 1:CAS:528:DC%2BD2sXjsVSiu78%3D 10.1007/s10549-006-9340-7 17004112 (Pubitemid 46474845)
15. W Voigt 2005 Sulforhodamine B assay and chemosensitivity Methods Mol Med 110 39 48 1:CAS:528:DC%2BD2MXktF2jtbY%3D 15901925
16. NMGM Appels H Rosing TC Stephens JHM Schellens JH Beijnen 2006 Quantification of farnesyl-methylcysteine in lysates of peripheral blood mononuclear cells using liquid chromatography coupled with electrospray tandem mass spectrometry: a novel pharmacodynamic assay for farnesyl transferase inhibitors Anal Chem 78 2617 2622 1:CAS:528:DC%2BD28XitFGktr8%3D 10.1021/ac051786s 16615771
17. JC Otto E Kim SG Young PJ Casey 1999 Cloning and characterization of a mammalian prenyl protein-specific protease J Biol Chem 274 13 8379 8382 1:CAS:528:DyaK1MXitFyrsrs%3D 10.1074/jbc.274.13.8379 10085068 (Pubitemid 29164625)
18. AA Adjei JN Davis C Erlichman PA Svingen SH Kaufmann 2000 Comparison of potential markers of farnesyltransferase inhibition Clin Cancer Res 6 6 2318 2325 1:CAS:528:DC%2BD3cXksVGhs7g%3D 10873082
19. LS Ulsh TY Shih 1984 Metabolic turnover of human c-rasH p21 protein of EJ bladder carcinoma and its normal cellular and viral homologs Mol Cell Biol 4 8 1647 1652 1:CAS:528:DyaL2cXlvV2jtbw%3D 6092927
20. HR Ashar L James K Gray D Carr M McGuirk E Maxwell S Black L Armstrong RJ Doll AG Taveras WR Bishop P Kirschmeier 2001 The farnesyl transferase inhibitor SCH 66336 induces a G(2) → M or G(1) pause in sensitive human tumor cell lines Exp Cell Res 262 1 17 27 1:CAS:528:DC%2BD3cXovVOgtL4%3D 10.1006/excr.2000.5076 11120601 (Pubitemid 32989004)
21. T Nagasu K Yoshimatsu C Rowell MD Lewis AM Garcia 1995 Inhibition of human tumor xenograft growth by treatment with the farnesyl transferase inhibitor B956 Cancer Res 55 22 5310 5314 1:CAS:528:DyaK2MXpsVaqsro%3D 7585593
22. L Sepp-Lorenzino Z Ma E Rands NE Kohl JB Gibbs A Oliff N Rosen 1995 A peptidomimetic inhibitor of farnesyl:protein transferase blocks the anchorage-dependent and -independent growth of human tumor cell lines Cancer Res 55 22 5302 5309 1:CAS:528:DyaK2MXpsVaqsr0%3D 7585592
23. WC Rose FY Lee CR Fairchild M Lynch T Monticello RA Kramer V Manne 2001 Preclinical antitumor activity of BMS-214662, a highly apoptotic and novel farnesyltransferase inhibitor Cancer Res 61 20 7507 7517 1:CAS:528: DC%2BD3MXnvFShsb4%3D 11606387
24. NMGM Appels JH Beijnen JHM Schellens 2005 Development of farnesyl transferase inhibitors: a review Oncologist 10 8 565 578 10.1634/theoncologist. 10-8-565 16177281 (Pubitemid 41429120)