Identification of small molecule compounds that inhibit the HIF-1 signaling pathway

Molecular Cancer

Volumn 8, Issue , 2009, Pages

  Xia, Menghang ^a   Bi, Kun ^b   Huang, Ruili ^a   Cho, Ming Hsuang ^a   Sakamuru, Srilatha ^a   Miller, Susanne C ^a   Li, Hua ^c   Sun, Yi ^c   Printen, John ^b   Austin, Christopher P ^a   Inglese, James ^a  

^a NATIONAL INSTITUTES OF HEALTH   (United States)

^b INVITROGEN CORPORATION   (United States)

^c UNIVERSITY OF MICHIGAN   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA LACTAMASE; HYPOXIA INDUCIBLE FACTOR 1; HYPOXIA INDUCIBLE FACTOR 1 INHIBITOR; OXYGEN; PROTEIN INHIBITOR; QUINOCARMYCIN; UNCLASSIFIED DRUG; VASCULOTROPIN;

ARTICLE; CELL ASSAY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG DETERMINATION; DRUG MECHANISM; DRUG STRUCTURE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; HYPOXIA; IC 50; PROTEIN SECRETION; QUANTITATIVE ANALYSIS; REPORTER GENE; SIGNAL TRANSDUCTION; DRUG ANTAGONISM; DRUG EFFECT; GENETICS; METABOLISM; RNA INTERFERENCE; TUMOR CELL LINE; VALIDATION STUDY;

BETA-LACTAMASES; CELL LINE, TUMOR; GENES, REPORTER; HUMANS; HYPOXIA-INDUCIBLE FACTOR 1; OXYGEN; RNA INTERFERENCE; SIGNAL TRANSDUCTION;

EID: 73249124004     PISSN: None     EISSN: 14764598     Source Type: Journal    
DOI: 10.1186/1476-4598-8-117     Document Type: Article

References (34)

1. Mole DR, Ratcliffe PJ. Cellular oxygen sensing in health and disease. Pediatr Nephrol 2008, 23:681-94. 10.1007/s00467-007-0632-x, 17955264.
2. Wang GL, Semenza GL. Purification and characterization of hypoxia-inducible factor 1. J Biol Chem 1995, 270:1230-7. 10.1074/jbc.270.3.1230, 7836384.
3. Huang LE, Gu J, Schau M, Bunn HF. Regulation of hypoxia-inducible factor 1alpha is mediated by an O2-dependent degradation domain via the ubiquitin-proteasome pathway. Proc Natl Acad Sci USA 1998, 95:7987-92. 10.1073/pnas.95.14.7987, 20916, 9653127.
4. Salceda S, Caro J. Hypoxia-inducible factor 1alpha (HIF-1alpha) protein is rapidly degraded by the ubiquitin-proteasome system under normoxic conditions. Its stabilization by hypoxia depends on redox-induced changes. J Biol Chem 1997, 272:22642-7. 10.1074/jbc.272.36.22642, 9278421.
5. Ivan M, Kondo K, Yang H, Kim W, Valiando J, Ohh M, Salic A, Asara JM, Lane WS, Kaelin WG. HIFalpha targeted for VHL-mediated destruction by proline hydroxylation: implications for O2 sensing. Science 2001, 292:464-8. 10.1126/science.1059817, 11292862.
6. Jaakkola P, Mole DR, Tian YM, Wilson MI, Gielbert J, Gaskell SJ, Kriegsheim A, Hebestreit HF, Mukherji M, Schofield CJ. Targeting of HIF-alpha to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation. Science 2001, 292:468-72. 10.1126/science.1059796, 11292861.
7. Lando D, Peet DJ, Gorman JJ, Whelan DA, Whitelaw ML, Bruick RK. Asparagine hydroxylation of HIF transactivation domain: a hypoxic switch. Science 2002, 295:858-861. 10.1126/science.1068592, 11823643.
8. Forsythe JA, Jiang BH, Iyer NV, Agani F, Leung SW, Koos RD, Semenza GL. Activation of vascular endothelial growth factor gene transcription by hypoxia-inducible factor 1. Mol Cell Biol 1996, 16:4604-13. 231459, 8756616.
9. Guillemin K, Krasnow MA. The hypoxic response: huffing and HIFing. Cell 1997, 89:9-12. 10.1016/S0092-8674(00)80176-2, 9094708.
10. Chen C, Pore N, Behrooz A, Ismail-Beigi F, Maity A. Regulation of glut1 mRNA by hypoxia-inducible factor-1. Interaction between H-ras and hypoxia. J Biol Chem 2001, 276:9519-25. 10.1074/jbc.M010144200, 11120745.
11. Iyer NV, Kotch LE, Agani F, Leung SW, Laughner E, Wenger RH, Gassmann M, Gearhart JD, Lawler AM, Yu AY, Semenza GL. Cellular and developmental control of O2 homeostasis by hypoxia-inducible factor 1 alpha. Genes Dev 1998, 12:149-62. 10.1101/gad.12.2.149, 316445, 9436976.
12. Redell MS, Tweardy DJ. Targeting transcription factors for cancer therapy. Curr Pharm Des 2005, 11:2873-87. 10.2174/1381612054546699, 16101443.
13. Ryan HE, Lo J, Johnson RS. HIF-1 alpha is required for solid tumor formation and embryonic vascularization. Embo J 1998, 17:3005-15. 10.1093/emboj/17.11.3005, 1170640, 9606183.
14. Tang N, Wang L, Esko J, Giordano FJ, Huang Y, Gerber HP, Ferrara N, Johnson RS. Loss of HIF-1alpha in endothelial cells disrupts a hypoxia-driven VEGF autocrine loop necessary for tumorigenesis. Cancer Cell 2004, 6:485-95. 10.1016/j.ccr.2004.09.026, 15542432.
15. Garber K. New drugs target hypoxia response in tumors. J Natl Cancer Inst 2005, 97:1112-4.
16. Nagle DG, Zhou YD. Natural product-derived small molecule activators of hypoxia-inducible factor-1 (HIF-1). Curr Pharm Des 2006, 12:2673-88. 10.2174/138161206777698783, 16842166.
17. Semenza GL. Targeting HIF-1 for cancer therapy. Nat Rev Cancer 2003, 3:721-32. 10.1038/nrc1187, 13130303.
18. Inglese J, Auld DS, Jadhav A, Johnson RL, Simeonov A, Yasgar A, Zheng W, Austin CP. Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries. Proc Natl Acad Sci USA 2006, 103:11473-8. 10.1073/pnas.0604348103, 1518803,1518803, 16864780.
19. Xia M, Huang R, Guo V, Southall N, Cho MH, Inglese J, Austin CP, Nirenberg M. Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memory. Proc Natl Acad Sci USA 2009, 106:2412-7. 10.1073/pnas.0813020106, 2638736,2638736, 19196967.
20. Triantafyllou A, Liakos P, Tsakalof A, Georgatsou E, Simos G, Bonanou S. Cobalt induces hypoxia-inducible factor-1alpha (HIF-1alpha) in HeLa cells by an iron-independent, but ROS-, PI-3K- and MAPK-dependent mechanism. Free Radic Res 2006, 40:847-56. 10.1080/10715760600730810, 17015263.
21. Maxwell P, Salnikow K. HIF-1: an oxygen and metal responsive transcription factor. Cancer Biol Ther 2004, 3:29-35.
22. Vukovic V, Haugland HK, Nicklee T, Morrison AJ, Hedley DW. Hypoxia-inducible factor-1alpha is an intrinsic marker for hypoxia in cervical cancer xenografts. Cancer Res 2001, 61:7394-8.
23. Chau NM, Rogers P, Aherne W, Carroll V, Collins I, McDonald E, Workman P, Ashcroft M. Identification of novel small molecule inhibitors of hypoxia-inducible factor-1 that differentially block hypoxia-inducible factor-1 activity and hypoxia-inducible factor-1alpha induction in response to hypoxic stress and growth factors. Cancer Res 2005, 65:4918-28. 10.1158/0008-5472.CAN-04-4453, 15930314.
24. Chiarugi V, Magnelli L, Chiarugi A, Gallo O. Hypoxia induces pivotal tumor angiogenesis control factors including p53, vascular endothelial growth factor and the NFkappaB-dependent inducible nitric oxide synthase and cyclooxygenase-2. J Cancer Res Clin Oncol 1999, 125:525-8. 10.1007/s004320050312, 10480347.
25. Xia M, Huang R, Sun Y, Semenza GL, Aldred SF, Witt K, Inglese J, Tice RR, Austin CP. Identification of chemical compounds that induce HIF-1α activity. Toxicological Sciences 2009, 112:153-163. 10.1093/toxsci/kfp123, 19502547.
26. Babaoglu K, Simeonov A, Irwin JJ, Nelson ME, Feng B, Thomas CJ, Cancian L, Costi PM, Maltby DA, Jadhav A, Inglese J, Austin CP, Shoichet BK. Comprehensive mechanistic analysis of hits from high-throughput and docking screens against β-lactamase. J Med Chem 2008, 51:2502-2511. 10.1021/jm701500e, 2655312, 18333608.
27. Kong D, Park EJ, Stephen AG, Calvani M, Cardellina JH, Monks A, Fisher RJ, Shoemaker RH, Melillo G. Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity. Cancer Res 2005, 65:9047-55. 10.1158/0008-5472.CAN-05-1235, 16204079.
28. Kung AL, Zabludoff SD, France DS, Freedman SJ, Tanner EA, Vieira A, Cornell-Kennon S, Lee J, Wang B, Wang J. Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway. Cancer Cell 2004, 6:33-43. 10.1016/j.ccr.2004.06.009, 15261140.
29. Bi K, Xia M, Allred J, Inglese J, Printen J. A high throughput cell-based assay for interrogating hypoxia-induced signaling pathway. Drug Discovery Technology and Development: 8-11. August 2005; Boston
30. 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.
31. Niles WD, Coassin PJ. Piezo- and solenoid valve-based liquid dispensing for miniaturized assays. Assay Drug Dev Techno 2005, 3:189-202.
32. Cleveland PH, Koutz PJ. Nanoliter dispensing for uHTS using pin tools. Assay Drug Dev Technol 2005, 3:213-25. 10.1089/adt.2005.3.213, 15871695.
33. Michael S, Auld D, Klumpp C, Jadhav A, Zheng W, Thorne N, Austin CP, Inglese J, Simeonov A. A robotic platform for quantitative high-throughput screening. Assay Drug Dev Technol 2008, 6:637-57. 10.1089/adt.2008.150, 2651822, 19035846.
34. Yasgar A, Shinn P, Jadhav A, Auld D, Michael S, Zheng W, Austin CP, Inglese J, Simeonov A. Compound Management for Quantitative High-Throughput Screening. JALA Charlottesv Va 2008, 13:79-89. 2390859, 18496600.