PX-478, an inhibitor of hypoxia-inducible factor-1α, enhances radiosensitivity of prostate carcinoma cells

International Journal of Cancer

Volumn 123, Issue 10, 2008, Pages 2430-2437

  Palayoor, Sanjeewani T ^a   Mitchell, James B ^a   Cerna, David ^a   DeGraff, William ^a   John Aryankalayil, Molykutty ^a   Coleman, C Norman ^a  

^a NATIONAL CANCER INSTITUTE   (United States)

Author keywords

HIF 1 ; Hypoxia; Normoxia; PX 478; Radiosensitivity

Indexed keywords

4 [BIS(2 CHLOROETHYL)OXIDOAMINO]PHENYLALANINE; HISTONE H2AX; HYPOXIA INDUCIBLE FACTOR 1ALPHA; RADIOSENSITIZING AGENT; 2 AMINO 3 (4' N,N BIS(2 CHLOROETHYL)AMINO)PHENYLPROPIONIC ACID N OXIDE; 2-AMINO-3-(4'-N,N-BIS(2-CHLOROETHYL)AMINO)PHENYLPROPIONIC ACID N-OXIDE; HIF1A PROTEIN, HUMAN; HISTONE; MUSTARD GAS DERIVATIVE; PHENYLPROPIONIC ACID DERIVATIVE;

ARTICLE; CANCER CELL CULTURE; CANCER RADIOTHERAPY; CARCINOMA CELL; CELL CYCLE; CELL CYCLE ARREST; CELL CYCLE G2 PHASE; CELL CYCLE S PHASE; CELL HYPOXIA; CELL PH; CELL SURVIVAL; CONTROLLED STUDY; CYTOTOXICITY; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; HUMAN; IN VITRO STUDY; MALE; PHOSPHORYLATION; PRIORITY JOURNAL; PROSTATE CARCINOMA; PROTEIN EXPRESSION; RADIOSENSITIVITY; DRUG ANTAGONISM; FLUORESCENT ANTIBODY TECHNIQUE; METABOLISM; PATHOLOGY; PROSTATE TUMOR; RADIATION DOSE; TUMOR CELL LINE; WESTERN BLOTTING;

BLOTTING, WESTERN; CELL CYCLE; CELL HYPOXIA; CELL LINE, TUMOR; CELL SURVIVAL; FLUORESCENT ANTIBODY TECHNIQUE; HISTONES; HUMANS; HYPOXIA-INDUCIBLE FACTOR 1, ALPHA SUBUNIT; MALE; MUSTARD COMPOUNDS; PHENYLPROPIONATES; PHOSPHORYLATION; PROSTATIC NEOPLASMS; RADIATION TOLERANCE;

EID: 53449096820     PISSN: 00207136     EISSN: 10970215     Source Type: Journal    
DOI: 10.1002/ijc.23807     Document Type: Article

References (44)

1. Bachtiary B, Schindl M, Potter R, Dreier B, Knocke TH, Hainfellner JA, Horvat R, Birner P. Overexpression of hypoxia-inducible factor 1α indicates diminished response to radiotherapy and unfavorable prognosis in patients receiving radical radiotherapy for cervical cancer. Clin Cancer Res 2003;9:2234-40.
2. Aebersold DM, Burri P, Beer KT, Laissue J, Djonov V, Greiner RH, Semenza GL. Expression of hypoxia-inducible factor-1α: a novel predictive and prognostic parameter in the radiotherapy of oropharyngeal cancer. Cancer Res 2001;61:2911-16.
3. Fyles AW, Milosevic M, Wong R, Kavanagh MC, Pintilie M, Sun A, Chapman W, Levin W, Manchul L, Keane TJ, Hill RP. Oxygenation predicts radiation response and survival in patients with cervix cancer. Radiother Oncol 1998;48:149-56.
4. Brizel DM, Sibley GS, Prosnitz LR, Scher RL, Dewhirst MW. Tumor hypoxia adversely affects the prognosis of carcinoma of the head and neck. Int J Radiat Oncol Biol Phys 1997;38:285-9.
5. Nordsmark M, Overgaard M, Overgaard J. Pretreatment oxygenation predicts radiation response in advanced squamous cell carcinoma of the head and neck. Radiother Oncol 1996;41:31-9.
6. Hall EJ. The oxygen effects and reoxygenation. Radiobiology for the radiologist, 5th edn. Philadelphia, PA: Lippincott Williams and Wilkins, 2000.91-111.
7. Gray LH, Conger AD, Ebert M, Hornsey S, Scott OC. The concentration of oxygen dissolved in tissues at the time of irradiation as a factor in radiotherapy. Br J Radiol 1953;26:638-48.
8. Overgaard J. Hypoxic radiosensitization: adored and ignored. J Clin Oncol 2007;25:4066-74.
9. Semenza GL. Regulation of mammalian O2 homeostasis by hypoxiainducible factor 1. Annu Rev Cell Dev Biol 1999;15:551-78.
10. Semenza GL. Targeting HIF-1 for cancer therapy. Nat Rev Cancer 2003;3:721-32.
11. Harris AL. Hypoxia - a key regulatory factor in tumour growth. Nat Rev Cancer 2002;2:38-47.
12. Zhong H, Chiles K, Feldser D, Laughner E, Hanrahan C, Georgescu MM, Simons JW, Semenza GL. Modulation of hypoxia-inducible factor 1α expression by the epidermal growth factor/phosphatidylinositol 3-kinase/PTEN/AKT/FRAP pathway in human prostate cancer cells: implications for tumor angiogenesis and therapeutics. Cancer Res 2000;60:1541-5.
13. Welsh S, Williams R, Kirkpatrick L, Paine-Murrieta G, Powis G. Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1α. Mol Cancer Ther 2004;3:233-44.
14. Ricker JL, Chen Z, Yang XP, Pribluda VS, Swartz GM, Van Waes C. 2-Methoxyestradiol inhibits hypoxia-inducible factor 1α, tumor growth, and angiogenesis and augments paclitaxel efficacy in head and neck squamous cell carcinoma. Clin Cancer Res 2004;10:8665-73.
15. Palayoor ST, Tofilon PJ, Coleman CN. Ibuprofen-mediated reduction of hypoxia-inducible factors HIF-1α and HIF-2α in prostate cancer cells. Clin Cancer Res 2003;9:3150-7.
16. Welsh SJ, Williams RR, Birmingham A, Newman DJ, Kirkpatrick DL, Powis G. The thioredoxin redox inhibitors 1-methylpropyl 2-imidazolyl disulfide and pleurotin inhibit hypoxia-induced factor 1α and vascular endothelial growth factor formation. Mol Cancer Ther 2003;2:235-43.
17. Rapisarda A, Uranchimeg B, Scudiero DA, Selby M, Sausville EA, Shoemaker RH, Melillo G. Identification of small molecule inhibitors of hypoxia-inducible factor 1 transcriptional activation pathway. Cancer Res 2002;62:4316-24.
18. Isaacs JS, Jung YJ, Mimnaugh EG, Martinez A, Cuttitta F, Neckers LM. Hsp90 regulates a von Hippel Lindau-independent hypoxia-inducible factor-1α-degradative pathway. J Biol Chem 2002;277:29936-44.
19. Mizuno T, Nagao M, Yamada Y, Narikiyo M, Ueno M, Miyagishi M, Taira K, Nakajima Y. Small interfering RNA expression vector targeting hypoxia-inducible factor 1α inhibits tumor growth in hepatobiliary and pancreatic cancers. Cancer Gene Ther 2006;13:131-40.
20. Li L, Lin X, Staver M, Shoemaker A, Semizarov D, Fesik SW, Shen Y. Evaluating hypoxia-inducible factor-1α as a cancer therapeutic target via inducible RNA interference in vivo. Cancer Res 2005;65:7249-58.
21. Moeller BJ, Dreher MR, Rabbani ZN, Schroeder T, Cao Y, Li CY, Dewhirst MW. Pleiotropic effects of HIF-1 blockade on tumor radiosensitivity. Cancer Cell 2005;8:99-110.
22. Zhang Q, Zhang ZF, Rao JY, Sato JD, Brown J, Messadi DV, Le AD. Treatment with siRNA and antisense oligonucleotides targeted to HIF-1α induced apoptosis in human tongue squamous cell carcinomas. Int J Cancer 2004;111:849-57.
23. Zhang X, Kon T, Wang H, Li F, Huang Q, Rabbani ZN, Kirkpatrick JP, Vujaskovic Z, Dewhirst MW, Li CY. Enhancement of hypoxia-induced tumor cell death in vitro and radiation therapy in vivo by use of small interfering RNA targeted to hypoxia-inducible factor-1α. Cancer Res 2004;64:8139-42.
24. Sun X, Kanwar JR, Leung E, Vale M, Krissansen GW. Regression of solid tumors by engineered overexpression of von Hippel-Lindau tumor suppressor protein and antisense hypoxia-inducible factor-1α. Gene Ther 2003;10:2081-9.
25. Kung AL, Zabludoff SD, France DS, Freedman SJ, Tanner EA, Vieira A, Cornell-Kennon S, Lee J, Wang B, Wang J, Memmert K, Naegeli HU, et al. Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway. Cancer Cell 2004;6:33-43.
26. Staab A, Loeffler J, Said HM, Diehlmann D, Katzer A, Beyer M, Fleischer M, Schwab F, Baier K, Einsele H, Flentje M, Vordermark D. Effects of HIF-1 inhibition by chetomin on hypoxia-related transcription and radiosensitivity in HT 1080 human fibrosarcoma cells. BMC Cancer 2007;7:213.
27. Powis G, Kirkpatrick L. Hypoxia inducible factor-1α as a cancer drug target. Mol Cancer Ther 2004;3:647-54.
28. Koh MY, Spivak-Kroizman T, Venturini S, Welsh S, Williams RR, Kirkpatrick DL, Powis G. Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1α. Mol Cancer Ther 2008;7:90-100.
29. Russo A, Mitchell JB, Finkelstein E, DeGraff WG, Spiro IJ, Gamson J. The effects of cellular glutathione elevation on the oxygen enhancement ratio. Radiat Res 1985;103:232-9.
30. Palayoor ST, Burgos MA, Shoaibi A, Tofilon PJ, Coleman CN. Effect of radiation and ibuprofen on normoxic renal carcinoma cells overexpressing hypoxia-inducible factors by loss of von Hippel-Lindau tumor suppressor gene function. Clin Cancer Res 2004;10:4158-64.
31. Cook JA, Glass J, Lebovics R, Bobo H, Pass H, DeLaney TF, Oldfield EH, Mitchell JB, Glatstein E, Goffman TE. Measurement of thymidine replacement in patients with high grade gliomas, head and neck tumors, and high grade sarcomas after continuous intravenous infusions of 5-iododeoxyuridine. Cancer Res 1992;52:719-25.
32. Dote H, Cerna D, Burgan WE, Carter DJ, Cerra MA, Hollingshead MG, Camphausen K, Tofilon PJ. Enhancement of in vitro and in vivo tumor cell radiosensitivity by the DNA methylation inhibitor zebularine. Clin Cancer Res 2005;11:4571-9.
33. Koukourakis MI, Bentzen SM, Giatromanolaki A, Wilson GD, Daley FM, Saunders MI, Dische S, Sivridis E, Harris AL. Endogenous markers of two separate hypoxia response pathways (hypoxia inducible factor 2α and carbonic anhydrase 9) are associated with radiotherapy failure in head and neck cancer patients recruited in the CHART randomized trial. J Clin Oncol 2006;24:727-35.
34. Zhong H, Willard M, Simons J. NS398 reduces hypoxia-inducible factor (HIF)-1α and HIF-1 activity: multiple-level effects involving cyclooxygenase-2 dependent and independent mechanisms. Int J Cancer 2004;112:585-95.
35. Hur E, Kim HH, Choi SM, Kim JH, Yim S, Kwon HJ, Choi Y, Kim DK, Lee MO, Park H. Reduction of hypoxia-induced transcription through the repression of hypoxia-inducible factor-1α/aryl hydrocarbon receptor nuclear translocator DNA binding by the 90-kDa heatshock protein inhibitor radicicol. Mol Pharmacol 2002;62:975-82.
36. Chang H, Shyu KG, Lee CC, Tsai SC, Wang BW, Hsien Lee Y, Lin S. GL331 inhibits HIF-1α expression in a lung cancer model. Biochem Biophys Res Commun 2003;302:95-100.
37. Mabjeesh NJ, Escuin D, LaVallee TM, Pribluda VS, Swartz GM, Johnson MS, Willard MT, Zhong H, Simons JW, Giannakakou P. 2ME2 inhibits tumor growth and angiogenesis by disrupting microtubules and dysregulating HIF. Cancer Cell 2003;3:363-75.
38. Jones MK, Szabo IL, Kawanaka H, Husain SS, Tarnawski AS. von Hippel Lindau tumor suppressor and HIF-1α: new targets of NSAIDs inhibition of hypoxia-induced angiogenesis. FASEB J 2002;16:264-6.
39. Zhang Q, Tang X, Lu QY, Zhang ZF, Brown J, Le AD. Resveratrol inhibits hypoxia-induced accumulation of hypoxia-inducible factor-1α and VEGF expression in human tongue squamous cell carcinoma and hepatoma cells. Mol Cancer Ther 2005;4:1465-74.
40. Lanzi C, Cassinelli G, Cuccuru G, Supino R, Zuco V, Ferlini C, Scambia G, Zunino F. Cell cycle checkpoint efficiency and cellular response to paclitaxel in prostate cancer cells. Prostate 2001;48:254-64.
41. Banath JP, Olive PL. Expression of phosphorylated histone H2AX as a surrogate of cell killing by drugs that create DNA double-strand breaks. Cancer Res 2003;63:4347-50.
42. MacPhail SH, Banath JP, Yu TY, Chu EH, Lambur H, Olive PL. Expression of phosphorylated histone H2AX in cultured cell lines following exposure to X-rays. Int J Radiat Biol 2003;79:351-8.
43. Nazarov IB, Smirnova AN, Krutilina RI, Svetlova MP, Solovjeva LV, Nikiforov AA, Oei SL, Zalenskaya IA, Yau PM, Bradbury EM, Tomilin NV. Dephosphorylation of histone γ-H2AX during repair of DNA double-strand breaks in mammalian cells and its inhibition by calyculin A. Radiat Res 2003;160:309-17.
44. Macpherson GR, Figg WD. Small molecule-mediated anti-cancer therapy via hypoxia-inducible factor-1 blockade. Cancer Biol Ther 2004;3:503-4.