The HSP90 inhibitor, AT13387, is effective against imatinib-sensitive and -resistant gastrointestinal stromal tumor models

Molecular Cancer Therapeutics

Volumn 11, Issue 8, 2012, Pages 1799-1808

  Smyth, Tomoko ^a   Van Looy, Thomas ^b   Curry, Jayne E ^a   Rodriguez Lopez, Ana M ^a   Wozniak, Agnieszka ^b   Zhu, Meijun ^c   Donsky, Rachel ^c   Morgan, Jennifer G ^c   Mayeda, Mark ^c   Fletcher, Jonathan A ^c   Schöffski, Patrick ^b   Lyons, John ^a   Thompson, Neil T ^a   Wallis, Nicola G ^a  

^a ASTEX PHARMACEUTICALS   (United Kingdom)

^b UNIVERSITY HOSPITALS LEUVEN   (Belgium)

^c BRIGHAM AND WOMEN S HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AT 13387; HEAT SHOCK PROTEIN 70; HEAT SHOCK PROTEIN 90; HEAT SHOCK PROTEIN 90 INHIBITOR; IMATINIB; PROTEIN KINASE B; PROTEIN TYROSINE KINASE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CELL CULTURE; CONTROLLED STUDY; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG SENSITIVITY; DRUG TOLERABILITY; GASTROINTESTINAL STROMAL TUMOR; HUMAN; HUMAN CELL; MOUSE; NONHUMAN; PRIORITY JOURNAL; TUMOR XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; BENZAMIDES; CELL LINE, TUMOR; CELL PROLIFERATION; DRUG RESISTANCE, NEOPLASM; GASTROINTESTINAL STROMAL TUMORS; HSP90 HEAT-SHOCK PROTEINS; HUMANS; ISOINDOLES; MICE; MICE, SCID; PIPERAZINES; PROTO-ONCOGENE PROTEINS C-KIT; PYRIMIDINES; SIGNAL TRANSDUCTION; TUMOR BURDEN; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84864886616     PISSN: 15357163     EISSN: 15388514     Source Type: Journal    
DOI: 10.1158/1535-7163.MCT-11-1046     Document Type: Article

References (40)

1. Antonescu CR. The GIST paradigm: lessons for other kinase-driven cancers. J Pathol 2011;223:251-61.
2. Hornick JL, Fletcher CD. The role of KIT in the management of patients with gastrointestinal stromal tumors. Hum Pathol 2007;38:679-87. (Pubitemid 46560810)
3. Hirota S, Isozaki K, Moriyama Y, Hashimoto K, Nishida T, Ishiguro S, et al. Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors. Science 1998;279:577-80. (Pubitemid 28067289)
4. Debiec-Rychter M, Dumez H, Judson I, Wasag B, Verweij J, Brown M, et al. Use of c-KIT/PDGFRA mutational analysis to predict the clinical response to imatinib in patientswith advanced gastrointestinal stromal tumours entered on phase I and II studies of the EORTC Soft Tissue and Bone Sarcoma Group. Eur J Cancer 2004;40:689-95. (Pubitemid 38326618)
5. Heinrich MC, Corless CL, Demetri GD, Blanke CD, von MM, Joensuu H, et al. Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol 2003;21:4342-9. (Pubitemid 46621810)
6. Gramza AW, Corless CL, Heinrich MC. Resistance to tyrosine kinase inhibitors in gastrointestinal stromal tumors. Clin Cancer Res 2009;15:7510-8.
7. Liegl B, Kepten I, Le C, Zhu M, Demetri GD, Heinrich MC, et al. Heterogeneity of kinase inhibitor resistance mechanisms in GIST. J Pathol 2008;216:64-74.
8. Csermely P, Schnaider T, Soti C, Prohaszka Z, Nardai G. The 90-kDa molecular chaperone family: structure, function, and clinical applications. A comprehensive review. Pharmacol Ther 1998;79:129-68. (Pubitemid 28380440)
9. Solit DB, Rosen N. Hsp90: a novel target for cancer therapy. Curr Top Med Chem 2006;6:1205-14. (Pubitemid 44120915)
10. Fumo G, Akin C, Metcalfe DD, Neckers L. 17-Allylamino-17- demethoxygeldanamycin (17-AAG) is effective in down-regulating mutated, constitutively activated KIT protein in human mast cells. Blood 2004;103:1078-84. (Pubitemid 38129574)
11. Bauer S, Yu LK, Demetri GD, Fletcher JA. Heat shock protein 90 inhibition in imatinib-resistant gastrointestinal stromal tumor. Cancer Res 2006;66:9153-61. (Pubitemid 44521135)
12. Dewaele B, Wasag B, Cools J, Sciot R, Prenen H, Vandenberghe P, et al. Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation. Clin Cancer Res 2008;14:5749-58.
13. Floris G, Sciot R, Wozniak A, Van LT, Wellens J, Faa G, et al. The novel heat shock protein 90 inhibitor, IPI-493, is highly effective in human gastrostrointestinal stromal tumor (GIST) xenografts carrying heterogeneous KIT mutations. Clin Cancer Res 2011;17:5604-14.
14. Floris G, Debiec-Rychter M, Wozniak A, Stefan C, Normant E, Faa G, et al. The heat shock protein 90 inhibitor IPI-504 induces KIT degradation, tumor shrinkage and cell proliferation arrest in xenografts models of gastrointestinal stromal tumors. Mol Cancer Ther 2011;10:1897-908.
15. Biamonte MA, Van de Water R, Arndt JW, Scannevin RH, Perret D, Lee WC. Heat shock protein 90: inhibitors in clinical trials. J Med Chem 2010;53:3-17.
16. Demetri GD, Le Cesne A, Von Mehren M, Chmielowski B, Bauer S, Chow WA, et al.Final results from a phase III study of IPI-504 (retaspimycin hydrochloride) versus placebo in patients (pts) with gastrointestinal stromal tumors (GIST) following failure of kinase inhibitor therapies [abstract]. 2010 In: Proceedings of the Gastrointestinal Cancers Symposium; 2010 Jan 22. Alexandria, VA: American Society of Clinical Oncology.
17. Graham B, Curry J, Smyth T, Fazal L, Feltell R, Harada I, et al. The HSP90 inhibitor, AT13387, displays a long duration of action in vitro and in vivo in non-small cell lung cancer. Cancer Sci 2011;103:522-7.
18. Woodhead AJ, Angove H, Carr MG, Chessari G, Congreve M, Coyle JE, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl) -1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem 2010;53:5956-69.
19. Taguchi T, Sonobe H, Toyonaga S, Yamasaki I, Shuin T, Takano A, et al. Conventional and molecular cytogenetic characterization of a new human cell line, GIST-T1, established from gastrointestinal stromal tumor. Lab Invest 2002;82:663-5. (Pubitemid 34522379)
20. Gunaratnam M, Swank S, Haider SM, Galesa K, Reszka AP, Beltran M, et al. Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. J Med Chem 2009;52:3774-83.
21. Heinrich MC, Corless CL, Blanke CD, Demetri GD, Joensuu H, Roberts PJ, et al. Molecular correlates of imatinib resistance in gastrointestinal stromal tumors. J Clin Oncol 2006;24:4764-74. (Pubitemid 46630941)
22. Lassus H, Sihto H, Leminen A, Nordling S, Joensuu H, Nupponen NN, et al. Genetic alterations and protein expression of KIT and PDGFRA in serous ovarian carcinoma. Br J Cancer 2004;91:2048-55. (Pubitemid 40136610)
23. McLean SR, Gana-Weisz M, Hartzoulakis B, Frow R, Whelan J, Selwood D, et al. Imatinib binding and cKIT inhibition is abrogated by the cKIT kinase domain I missense mutation Val654Ala. Mol Cancer Ther 2005;4:2005-15.
24. Squires MS, Feltell RE, Wallis NG, Lewis EJ, Smith DM, Cross DM, et al. Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines. Mol Cancer Ther 2009;8:324-32.
25. Curry J, Angove H, Fazal L, Lyons J, Reule M, Thompson N, et al. Aurora B kinase inhibition in mitosis: strategies for optimising the use of aurora kinase inhibitors such as AT9283. Cell Cycle 2009;8:1921-9.
26. Workman P, Aboagye EO, Balkwill F, Balmain A, Bruder G, Chaplin DJ, et al. Guidelines for the welfare and use of animals in cancer research. Br J Cancer 2010;102:1555-77.
27. Hollands C. The Animals (scientific procedures) Act 1986. Lancet 1986;2:32-3. (Pubitemid 16095623)
28. Floris G, Debiec-Rychter M, Sciot R, Stefan C, Fieuws S, Machiels K, et al. High efficacy of panobinostat towards human gastrointestinal stromal tumors in a xenograft mouse model. Clin Cancer Res 2009;15:4066-76.
29. Banerji U, Walton M, Raynaud F, Grimshaw R, Kelland L, Valenti M, et al. Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models. Clin Cancer Res 2005;11:7023-32. (Pubitemid 41428762)
30. Penner CR, Folpe AL, Budnick SD. C-kit expression distinguishes salivary gland adenoid cystic carcinoma from polymorphous low-grade adenocarcinoma. Mod Pathol 2002;15:687-91. (Pubitemid 34787302)
31. Modi S, Stopeck AT, Gordon MS, Mendelson D, Solit DB, Bagatell R, et al. Combination of trastuzumab and tanespimycin (17-AAG, KOS-953) is safe and active in trastuzumab-refractory HER-2 overexpressing breast cancer: a phase I dose-escalation study. J Clin Oncol 2007;25:5410-7. (Pubitemid 350232217)
32. Solit DB, Osman I, Polsky D, Panageas KS, Daud A, Goydos JS, et al. Phase II trial of 17-allylamino-17-demethoxygeldanamycin in patients with metastatic melanoma. Clin Cancer Res 2008;14:8302-7.
33. Solit DB, Ivy SP, Kopil C, Sikorski R, Morris MJ, Slovin SF, et al. Phase I trial of 17-allylamino-17-demethoxygeldanamycin in patients with advanced cancer. Clin Cancer Res 2007;13:1775-82. (Pubitemid 46952945)
34. Heinrich MC, Blanke CD, Druker BJ, Corless CL. Inhibition of KIT tyrosine kinase activity: a novel molecular approach to the treatment of KIT-positive malignancies. J Clin Oncol 2002;20:1692-703. (Pubitemid 34260552)
35. Lim KH, Tefferi A, Lasho TL, Finke C, Patnaik M, Butterfield JH, et al. Systemic mastocytosis in 342 consecutive adults: survival studies and prognostic factors. Blood 2009;113:5727-36.
36. Paschka P, Marcucci G, Ruppert AS, Mrozek K, Chen H, Kittles RA, et al. Adverse prognostic significance of KIT mutations in adult acute myeloid leukemia with inv(16) and t(8;21): a Cancer and Leukemia Group B study. J Clin Oncol 2006;24:3904-11. (Pubitemid 46630738)
37. Schnittger S, Kohl TM, Haferlach T, Kern W, Hiddemann W, Spiekermann K, et al. KIT-D816 mutations in AML1-ETO-positive AML are associated with impaired event-free and overall survival. Blood 2006;107:1791-9. (Pubitemid 43289355)
38. Ma Y, Zeng S, Metcalfe DD, Akin C, Dimitrijevic S, Butterfield JH, et al. The c-KIT mutation causing human mastocytosis is resistant to STI571 and other KIT kinase inhibitors; kinases with enzymatic site mutations show different inhibitor sensitivity profiles than wild-type kinases and those with regulatory-type mutations. Blood 2002;99:1741-4. (Pubitemid 34533049)
39. Went PT, Dirnhofer S, Bundi M, Mirlacher M, Schraml P, Mangialaio S, et al. Prevalence of KIT expression in human tumors. J Clin Oncol 2004;22:4514-22. (Pubitemid 41185118)
40. Woodman SE, Davies MA. Targeting KIT in melanoma: a paradigm of molecular medicine and targeted therapeutics. Biochem Pharmacol 2010;80:568-74.