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References

  • 1
    Semenza GL ( 2001) HIF-1 and mechanisms of hypoxia sensing. Curr Opin Cell Biol 13: 167171.
  • 2
    Stolze IP, Mole DR, Ratcliffe PJ ( 2006) Regulation of HIF: prolyl hydroxylases. Novartis Found Symp 272: 1525, 25–36.
  • 3
    Haase VH ( 2009) The VHL tumor suppressor: master regulator of HIF. Curr Pharm Des 15: 38953903.
  • 4
    Semenza GL ( 2003) Targeting HIF-1 for cancer therapy. Nat Rev Cancer 3: 721732.
  • 5
    Palayoor ST, Mitchell JB, Cerna D, Degraff W, John-Aryankalayil M, Coleman CN ( 2008) PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells. Int J Cancer 123: 24302437.
  • 6
    Harada H, Inoue M, Itasaka S, Hirota K, Morinibu A, Shinomiya K, Zeng L, Ou G, Zhu Y, Yoshimura M, McKenna WG, Muschel RJ, Hiraoka M ( 2012) Cancer cells that survive radiation therapy acquire HIF-1 activity and translocate towards tumour blood vessels. Nat Commun 3: 783.
  • 7
    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 ( 2005) Identification of a novel small-molecule inhibitor of the hypoxia-inducible factor 1 pathway. Cancer Res 65: 605612.
  • 8
    Choi HJ, Song BJ, Gong YD, Gwak WJ, Soh Y ( 2008) Rapid degradation of hypoxia-inducible factor-1alpha by KRH102053, a new activator of prolyl hydroxylase 2. Br J Pharmacol 154: 114125.
  • 9
    Mooring SR, Jin H, Devi NS, Jabbar AA, Kaluz S, Liu Y, Van Meir EG, Wang B (2011) Design and synthesis of novel small-molecule inhibitors of the hypoxia inducible factor pathway. J Med Chem 54:84718489.
  • 10
    Greenberger LM, Horak ID, Filpula D, Sapra P, Westergaard M, Frydenlund HF, Albaek C, Schroder H, Orum H ( 2008) A RNA antagonist of hypoxia-inducible factor-1alpha, EZN-2968, inhibits tumor cell growth. Mol Cancer Ther 7: 35983608.
  • 11
    Tian H, McKnight SL, Russell DW ( 1997) Endothelial PAS domain protein 1 (EPAS1), a transcription factor selectively expressed in endothelial cells. Genes Dev 11: 7282.
  • 12
    Tian H, Hammer RE, Matsumoto AM, Russell DW, McKnight SL ( 1998) The hypoxia-responsive transcription factor EPAS1 is essential for catecholamine homeostasis and protection against heart failure during embryonic development. Genes Dev 12: 33203324.
  • 13
    Holmquist-Mengelbier L, Fredlund E, Lofstedt T, Noguera R, Navarro S, Nilsson H, Pietras A, Vallon-Christersson J, Borg A, Gradin K, Poellinger L, Pahlman S ( 2006) Recruitment of HIF-1alpha and HIF-2alpha to common target genes is differentially regulated in neuroblastoma: HIF-2alpha promotes an aggressive phenotype. Cancer Cell 10: 413423.
  • 14
    Yang J, Zhang L, Erbel PJ, Gardner KH, Ding K, Garcia JA, Bruick RK ( 2005) Functions of the Per/ARNT/Sim domains of the hypoxia-inducible factor. J Biol Chem 280: 3604736054.
  • 15
    Erbel PJ, Card PB, Karakuzu O, Bruick RK, Gardner KH ( 2003) Structural basis for PAS domain heterodimerization in the basic helix-loop-helix-PAS transcription factor hypoxia-inducible factor. Proc Natl Acad Sci USA 100: 1550415509.
  • 16
    Cunningham BC, Wells JA ( 1989) High-resolution epitope mapping of hGH-receptor interactions by alanine-scanning mutagenesis. Science 244: 10811085.
  • 17
    Scheuermann TH, Tomchick DR, Machius M, Guo Y, Bruick RK, Gardner KH ( 2009) Artificial ligand binding within the HIF2alpha PAS-B domain of the HIF2 transcription factor. Proc Natl Acad Sci USA 106: 450455.
  • 18
    Key J, Scheuermann TH, Anderson PC, Daggett V, Gardner KH ( 2009) Principles of ligand binding within a completely buried cavity in HIF2alpha PAS-B. J Am Chem Soc 131: 1764717654.
  • 19
    Jhoti H ( 2007) Fragment-based drug discovery using rational design. Ernst Schering Found Symp Proc 3: 169185.
  • 20
    Fattori D, Squarcia A, Bartoli S ( 2008) Fragment-based approach to drug lead discovery: overview and advances in various techniques. Drugs R D 9: 217227.
  • 21
    Foloppe N ( 2011) The benefits of constructing leads from fragment hits. Future Med Chem 3: 11111115.
  • 22
    Erlanson DA, Wells JA, Braisted AC ( 2004) Tethering: fragment-based drug discovery. Annu Rev Biophys Biomol Struct 33: 199223.
  • 23
    Singh J, Petter RC, Baillie TA, Whitty A ( 2011) The resurgence of covalent drugs. Nat Rev Drug Discov 10: 307317.
  • 24
    Zhu J, Martinez-Yamout M, Cardoso R, Yan J, Love RA, Grodsky N, Brooun A, Dyson HJ (2012). Homodimerization of the PAS-B domains of hypoxia-inducible factors. J Phys Chem B 116: 69606965.
  • 25
    Ward JHJ ( 1963) Hierarchical grouping to optimize an objective function. J Am Stat Assoc 48: 236244.
  • 26
    Jones DT, Harris AL ( 2012) Small-molecule inhibitors of the HIF pathway and synthetic lethal interactions. Expert Opin Ther Targets 16: 463480.
  • 27
    Semenza GL ( 2012) Hypoxia-inducible factors: mediators of cancer progression and targets for cancer therapy. Trends Pharmacol Sci 33: 207214.
  • 28
    Johnson DS, Weerapana E, Cravatt BF (2010), Strategies for discovering and derisking covalent, irreversible enzyme inhibitors. Future Med Chem 2: 949964.
  • 29
    Honigberg LA, Smith AM, Sirisawad M, Verner E, Loury D, Chang B, Li S, Pan Z, Thamm DH, Miller RA, Buggy JJ ( 2010) The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci USA 107: 1307513080.
  • 30
    Zhou W, Hur W, McDermott U, Dutt A, Xian W, Ficarro SB, Zhang J, Sharma SV, Brugge J, Meyerson M, Settleman J, Gray NS ( 2010) A structure-guided approach to creating covalent FGFR inhibitors. Chem Biol 17: 285295.
  • 31
    Fry DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, McNamara DJ, Nelson JM, Sherwood V, Smaill JB, Trumpp-Kallmeyer S, Dobrusin EM ( 1998) Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor. Proc Natl Acad Sci USA 95: 1202212027.
  • 32
    Cohen MS, Zhang C, Shokat KM, Taunton J ( 2005) Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Science 308: 13181321.
  • 33
    Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Janne PA ( 2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 462: 10701074.
  • 34
    Ramstrom O, Lehn JM ( 2002) Drug discovery by dynamic combinatorial libraries. Nat Rev Drug Discov 1: 2636.
  • 35
    Muchmore SW, Debe DA, Metz JT, Brown SP, Martin YC, Hajduk PJ ( 2008) Application of belief theory to similarity data fusion for use in analog searching and lead hopping. J Chem Inf Model 48: 941948.
  • 36
    Weerapana E, Wang C, Simon GM, Richter F, Khare S, Dillon MB, Bachovchin DA, Mowen K, Baker D, Cravatt BF ( 2010) Quantitative reactivity profiling predicts functional cysteines in proteomes. Nature 468: 790795.
  • 37
    Ahmad R, Raina D, Meyer C, Kharbanda S, Kufe D ( 2006) Triterpenoid CDDO-Me blocks the NF-kappaB pathway by direct inhibition of IKKbeta on Cys-179. J Biol Chem 281: 3576435769.
  • 38
    Shishodia S, Sethi G, Konopleva M, Andreeff M, Aggarwal BB ( 2006) A synthetic triterpenoid, CDDO-Me, inhibits IkappaBalpha kinase and enhances apoptosis induced by TNF and chemotherapeutic agents through down-regulation of expression of nuclear factor kappaB-regulated gene products in human leukemic cells. Clin Cancer Res 12: 18281838.
  • 39
    Buettner R, Corzano R, Rashid R, Lin J, Senthil M, Hedvat M, Schroeder A, Mao A, Herrmann A, Yim J, Li H, Yuan YC, Yakushijin K, Yakushijin F, Vaidehi N, Moore R, Gugiu G, Lee TD, Yip R, Chen Y, Jove R, Horne D, Williams JC ( 2011) Alkylation of cysteine 468 in Stat3 defines a novel site for therapeutic development. ACS Chem Biol 6: 432443.
  • 40
    Vonrhein C, Flensburg C, Keller P, Sharff A, Smart O, Paciorek W, Womack T, Bricogne G (2011) Data processing and analysis with the autoPROC toolbox. Acta Cryst D 67: 293302.
  • 41
    Card PB, Erbel PJ, Gardner KH ( 2005) Structural basis of ARNT PAS-B dimerization: use of a common beta-sheet interface for hetero- and homodimerization. J Mol Biol 353: 664677.
  • 42
    Brunger AT, Adams PD, Clore GM, DeLano WL, Gros P, Grosse-Kunstleve RW, Jiang JS, Kuszewski J, Nilges M, Pannu NS, Read RJ, Rice LM, Simonson T, Warren GL ( 1998) Crystallography & NMR system: A new software suite for macromolecular structure determination. Acta Cryst D 54: 905921.
  • 43
    Wiseman T, Williston S, Brandts JF, Lin LN ( 1989) Rapid measurement of binding constants and heats of binding using a new titration calorimeter. Anal Biochem 179: 131137.