Targeting the PAS-A domain of HIF-1α for development of small molecule inhibitors of HIF-1

Cell Cycle

Volumn 5, Issue 16, 2006, Pages 1847-1853

  Eun, Jung Park ^a   Kong, Dehe ^a   Fisher, Robert ^a   Cardellina, John ^b   Shoemaker, Robert H ^b   Melillo, Giovanni ^a  

^a SAIC FREDERICK INC   (United States)

^b NATIONAL CANCER INSTITUTE   (United States)

Author keywords

Hif 1 ; PAS A domain; Protein protein interaction; Screening; Small molecule inhibitors

Indexed keywords

AMINO ACID; HISTIDINE; HYPOXIA INDUCIBLE FACTOR 1ALPHA; HYPOXIA INDUCIBLE FACTOR 1BETA; LUCIFERASE; NSC 50352; PROTEIN INHIBITOR;

ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG TARGETING; ENZYME ACTIVATION; ENZYME LINKED IMMUNOSORBENT ASSAY; HUMAN; HUMAN CELL; IMMUNOPRECIPITATION; IN VITRO STUDY; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN PROTEIN INTERACTION; PROTEIN TARGETING; TWO HYBRID SYSTEM;

MAMMALIA;

EID: 33748938340     PISSN: 15384101     EISSN: 15514005     Source Type: Journal    
DOI: 10.4161/cc.5.16.3019     Document Type: Article

References (44)

1. Arkin MR, Wells JA. Small-molecule inhibitors of protein-protein interactions: Progression towards the dream. Nat Rev Drug Discov 2004; 3:301-7.
2. Karamouzis MV, Gorgoulis VG, Papavassiliou AG. Transcription factors and neoplasia: Vistas in novel drug design. Clin Cancer Res 2002; 8:949-61.
3. Kim R, Tanabe K, Emi M, Uchida Y, Inoue H, Toge T. Inducing cancer cell death by targeting transcription factors. Anticancer Drugs 2003; 14:3-11.
4. Semenza GL. Targeting HIF-1 for cancer therapy. Nat Rev Cancer 2003; 3:72132.
5. Potter C, Harris AL. Hypoxia inducible carbonic anhydrase IX, marker of tumor: Hypoxia, survival pathway and therapy target. Cell Cycle 2004; 3:164-7.
6. Koshiji M, Huang LE. Dynamic balancing of the dual nature of HIF-1alpha for cell survival. Cell Cycle 2004; 3:853-4.
7. Wang GL, Jiang BH, Rue EA, Semenza GL. Hypoxia-inducible factor 1 is a basic-helix-loop-helix-PAS heterodimer regulated by cellular O2 tension. Proc Natl Acad Sci USA 1995; 92:5510-4.
8. Brahimi-Horn C, Pouyssegur J. When hypoxia signaling meets the ubiquitin-proteasomal pathway, new targets for cancer therapy. Crit Rev Oncol Hematol 2005; 53:115-23.
9. Garber K. New drugs target hypoxia response in tumors. J Natl Cancer Inst 2005; 97:1112-4.
10. Toogood PL. Inhibition of protein-protein association by small molecules: Approaches and progress. J Med Chem 2002; 45:1543-58.
11. Fotcouhi N, Graves, B. Small molecule inhibitors of p53/MDM2 interaction. Curr Top Med Chem 2005; 5:159-65.
12. Oltersdorf T, Elmore SW, Shoemaker AR, Armstrong RC, Augeri DJ, Belli BA, Bruncko M, Deckwerth TL, Dinges J, Hajduk PJ, Joseph MK, Kitada S, Korsmeyer SJ, Kunzer AR, Letai A, Li C, Mitten MJ, Nettesheim DG, Ng S, Nimmer PM, O'Connor JM, Oleksijew A, Petros AM, Reed JC, Shen W, Tahir SK, Thompson CB, Tomaselli KJ, Wang B, Wendt MD, Zhang H, Fesik SW, Rosenberg SH. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 2005; 435:677-81.
13. Pagliaro L, Felding J, Audouze K, Nielsen SJ, Terry RB, Krog-Jensen C, Butcher S. Emerging classes of protein-protein interaction inhibitors and new tools for their development. Curr Opin Chem Biol 2004; 8:442-9.
14. Mueller TD, Zhang JL, Sebald W, Duschl A. Structure, binding, and antagonists in the IL-4/IL-13 receptor system. Biochim Biophys Acta 2002; 1592:237-50.
15. Stephanou A, Latchman DS. STAT-1: A novel regulator of apoptosis. Int J Exp Pathol 2003; 84:239-44.
16. 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.
17. Monks A, Scudiero D, Skehan P, Shoemaker R, Paull K, Vistica D, Hose C, Langley J, Cronise P, Vaigro-Wolff A, Gray-Goodrich M, Campbell, H, Mayo J, Boyd M. Feasibility of a high-flux anticancer drug screen using a diverse panel of cultures human tumor cell lines. J Natl Cancer Inst 1991; 83:757-66.
18. Melillo G. HIF-1: A target for cancer, ischemia and inflammation-too good to be true? Cell Cycle 2004; 3:154-55.
19. Rapisarda A, Shoemaker RH, Melillo G. Targeting topoisomerase I to inhibit hypoxia inducible factor 1. Cell Cycle 2004; 3:172-5.
20. 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.
21. 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.
22. Yeo EJ, Chun YS, Cho YS, Kim J, Lee JC, Kim MS, Park JW. YC-1: A potential anticancer drug targeting hypoxia-inducible factor 1. J Natl Cancer Inst 2003; 95:516-25.
23. Tan C, de Noronha RG, Roecker AJ, Pyrzynska B, Khwaja F, Zhang Z, Zhang H, Teng Q, Nicholson AC, Giannakakou P, Zhou W, Olson JJ, Pereira MM, Nicolaou KC, Van Meir EG. Identification of a novel small-molecule inhibitor of the hypoxia-inducible factor 1 pathway. Cancer Res 2005; 65:605-12.
24. 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-1 alpha. Mol Cancer Ther 2004; 3:233-44.
25. Rapisarda A, Uranchimeg B, Sordet O, Pommier Y, Shoemaker RH, Melillo G. Topoisomerase I-mediated inhibition of hypoxia-inducible factor 1: Mechanism and therapeutic implications. Cancer Res 2004; 64:1475-82.
26. Rapisarda A, Zalek, J, Hollingshead M, Braunschweig T, Uranchimeg B, Bonomi CA, Borgel SD, Carter JP, Hewitt SM, Shoemaker RH, Melillo G. Scheduled-dependent inhibition of hypoxia-inducible factor-1alpha protein accumulation, angiogenesis, and tumor growth by topotecan in U251-HRE glioblastoma xenografts. Cancer Res 2004; 64:6845-8.
27. Vassilev LT, Vu BT, Graves B, Carvajal D, Podlaski F, Filipovic Z, Kong N, Kammlott U, Lukacs C, Klein C, Fotouhi N, Liu EA. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science 2004; 303:844-8.
28. Vassilev LT. Small-molecule antagonists of p53-MDM2 binding: Research tools and potential therapeutics. Cell Cycle 2004; 3:419-21.
29. Waal ND, Yang W, Oslob JD, Arkin MR, Hyde J, Lu W, McDowell RS, Yu CH, Raimundo BC. Identification of nonpeptidic small-molecule inhibitors of interleukin-2. Bioorg Med Chem Lett 2005; 15:983-7.
30. Emerson SD, Palermo R, Liu CM, Tilley JW, Chen L, Danho W, Madison VS, Greeley DN, Ju G, Fry DC. NMR characterization of interleukin-2 in complexes with the IL-2Ralpha receptor component, and with low molecular weight compounds that inhibit the IL-2/IL-Ralpha interaction. Protein Sci 2003; 12:811-22.
31. Lepourcelet M, Chen YN, France DS, Wang H, Crews P, Petersen F, Bruseo C, Wood AW, Shivdasani RA. Small-molecule antagonists of the oncogenic Tcf/beta-catenin protein complex. Cancer Cell 2004; 5:91-102.
32. Roehrl MH, Kang S, Aramburu J, Wagner G, Rao A, Hogan PG. Selective inhibition of calcineurin-NFAT signaling by blocking protein-protein interaction with small organic molecules. Proc Natl Acad Sci USA 2004; 101:7554-9.
33. Berg T, Cohen SB, Desharnais J, Sonderegger C, Maslyar DJ, Goldberg J, Boger DL, Vogt PK. Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts. Proc Natl Acad Sci USA 2002; 99:3830-5.
34. 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, Petersen F, Eck MJ, Bair KW, Wood AW, Livingston DM. Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway. Cancer Cell 2004; 6:33-43.
35. Kewley RJ, Whitelaw ML, Chapman-Smith A. The mammalian basic helix-loop-helix/PAS family of transcriptional regulators. Int J Biochem Cell Biol 2004; 36:189-204.
36. Pongratz I, Antonsson C, Whitelaw ML, Poellinger L. Role of the PAS domain in regulation of dimerization and DNA binding specificity of the dioxin receptor. Mol Cell Biol 1998; 18:4079-88.
37. Gu YZ, Hogenesch JB, Bradfield CA. The PAS superfamily: Sensors of environmental and developmental signals. Annu Rev Pharmacol Toxicol 2000; 40:519-561.
38. Erbel PJ, Card PB, Karakuzu O, Bruick RK, Gardner KH. Structural basis for PAS domain heterodimerization in the basic helix-loop-helix-PAS transcription factor hypoxia-inducible factor. Proc Natl Acad Sci USA 2003; 100:15504-19.
39. Card PB, Erbel PJ, Gardner KH. Structural basis of ARNT PAS-B dimerization: Use of a common Beta-sheet interface for hetero- and homodimerization. J Mol Biol 2005; 353:664-77.
40. Yang J, Zhang L, Erbel PJ, Gardner KH, Ding K, Garcia JA. Bruick RK. Functions of the Per/ARNT/Sim domains of the hypoxia-inducible factor. J Biol Chem 2005; 280:36047-54.
41. Enyedy IJ, Ling Y, Nacro K, Tomita Y, Wu X, Cao Y, Guo R, Li B, Zhu X, Huang Y, Long YQ, Roller PP, Yang D, Wang S. Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening. J Med Chem 2001; 44:4313-24.
42. Stephen AG, Worthy KM, Towler E, Mikovits JA, Sei S, Roberts P, Yang QE, Akee RK, Klausmeyer P, McCloud TG, Henderson L, Rein A, Covell DG, Currens M, Shoemaker RH, Fisher RJ. Identification of HIV-1 nucleocapsid protein: Nucleic acid antagonists with cellular anti-HIV activity. Biochem Biophys Res Commun 2002; 296:1228-37.
43. Neamati N, Hong H, Sunder S, Milne GW, Pommier Y. Potent inhibitors of human immunodeficiency virus type 1 integrase: Identification of a novel four-point pharmacophore and tetracyclines as novel inhibitors. Mol Pharmacol 1997; 52:1041-55.
44. Howlett DR, George AR, Owen DE, Ward RV, Markwell RE. Common structural features determine the effectiveness of carvedilol, daunomycin and rolitetracycline as inhibitors of Alzheimer beta-amyloid fibril formation. Biochem J 1999; 343: 419-23.