Endogenous 2-oxoglutarate levels impact potencies of competitive HIF prolyl hydroxylase inhibitors

Pharmacological Research

Volumn 64, Issue 3, 2011, Pages 268-273

  Thirstrup, Kenneth ^a   Christensen, Søren ^a   Møller, Henriette Aaris ^a   Ritzén, Andreas ^a   Bergström, Ann Louise ^a   Sager, Thomas Nikolaj ^a   Jensen, Henrik Sindal ^a  

^a H LUNDBECK A S   (Denmark)

Author keywords

2 Oxoglutarate; Hif prolyl hydroxylase; Scintillation proximity assay; von Hippel Lindau protein

Indexed keywords

2 OXOGLUTARIC ACID; DEFEROXAMINE; FG 0041; HYPOXIA INDUCIBLE FACTOR; JNJ 42041935; OXYGENASE INHIBITOR; PROCOLLAGEN PROLINE 2 OXOGLUTARATE 4 DIOXYGENASE; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG POTENCY; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME ASSAY; HYDROXYLATION; IC 50; MOUSE; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL;

CELL LINE; DIOXYGENASES; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HUMANS; KETOGLUTARIC ACIDS; NUCLEAR PROTEINS; PROCOLLAGEN-PROLINE DIOXYGENASE; RECOMBINANT PROTEINS;

EID: 79959977075     PISSN: 10436618     EISSN: 10961186     Source Type: Journal    
DOI: 10.1016/j.phrs.2011.03.017     Document Type: Article

References (23)

1. A.C. Epstein, J.M. Gleadle, L.A. McNeill, K.S. Hewitson, J. O'Rourke, and D.R. Mole C. elegans EGL-9 and mammalian homologs define a family of dioxygenases that regulate HIF by prolyl hydroxylation Cell 107 2001 43 54 (Pubitemid 32972036)
2. D. Lando, D.J. Peet, D.A. Whelan, J.J. Gorman, and M.L. Whitelaw Asparagine hydroxylation of the HIF transactivation domain a hypoxic switch Science 295 2002 858 861 (Pubitemid 34118367)
3. M. Ivan, T. Haberberger, D.C. Gervasi, K.S. Michelson, V. Gunzler, and K. Kondo Biochemical purification and pharmacological inhibition of a mammalian prolyl hydroxylase acting on hypoxia-inducible factor Proc Natl Acad Sci U S A 99 2002 13459 13464 (Pubitemid 35215403)
4. M. Bergeron, J.M. Gidday, A.Y. Yu, G.L. Semenza, D.M. Ferriero, and F.R. Sharp Role of hypoxia-inducible factor-1 in hypoxia-induced ischemic tolerance in neonatal rat brain Ann Neurol 48 2000 285 296
5. A. Siddiq, I.A. Ayoub, J.C. Chavez, L. Aminova, S. Shah, and J.C. LaManna Hypoxia-inducible factor prolyl 4-hydroxylase inhibition. A target for neuroprotection in the central nervous system J Biol Chem 280 2005 41732 41743 (Pubitemid 41832236)
6. J.L. Johansen, T.N. Sager, J. Lotharius, L. Witten, A. Mork, and J. Egebjerg HIF prolyl hydroxylase inhibition increases cell viability and potentiates dopamine release in dopaminergic cells J Neurochem 115 2010 209 219
7. M.J. Ryle, and R.P. Hausinger Non-heme iron oxygenases Curr Opin Chem Biol 6 2002 193 201 (Pubitemid 34251375)
8. T. Bishop, D. Gallagher, A. Pascual, C.A. Lygate, J.P. de Bono, and L.G. Nicholls Abnormal sympathoadrenal development and systemic hypotension in PHD3-mice Mol Cell Biol 28 2008 3386 3400 (Pubitemid 351657101)
9. R.J. Appelhoff, Y.M. Tian, R.R. Raval, H. Turley, A.L. Harris, and C.W. Pugh Differential function of the prolyl hydroxylases PHD1, PHD2, and PHD3 in the regulation of hypoxia-inducible factor J Biol Chem 279 2004 38458 38465 (Pubitemid 39295997)
10. M.A. McDonough, V. Li, E. Flashman, R. Chowdhury, C. Mohr, and B.M. Lienard Cellular oxygen sensing: Crystal structure of hypoxia-inducible factor prolyl hydroxylase (PHD2) Proc Natl Acad Sci U S A 103 2006 9814 9819 (Pubitemid 43993580)
11. J.R. Tuckerman, Y. Zhao, K.S. Hewitson, Y.M. Tian, C.W. Pugh, and P.J. Ratcliffe Determination and comparison of specific activity of the HIF-prolyl hydroxylases FEBS Lett 576 2004 145 150 (Pubitemid 39330473)
12. C.M. Tegley, V.N. Viswanadhan, K. Biswas, M.J. Frohn, T.A. Peterkin, and C. Chang Discovery of novel hydroxy-thiazoles as HIF-alpha prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation Bioorg Med Chem Lett 18 2008 3925 3928
13. M.H. Rabinowitz Structure based design and biological evaluation of benzimidazole HIF prolyl hydroxylase inhibitors for the treatment of anemia 239th ACS National Meeting & Exposition San Francisco CA, March 21-25, Abstract MEDI 321 2010
14. K.J. Nytko, P. Spielmann, G. Camenisch, R.H. Wenger, and D.P. Stiehl Regulated function of the prolyl-4-hydroxylase domain (PHD) oxygen sensor proteins Antioxid Redox Signal 9 2007 1329 1338 (Pubitemid 47255012)
15. L.A. McNeill, L. Bethge, K.S. Hewitson, and C.J. Schofield A fluorescence-based assay for 2-oxoglutarate-dependent oxygenases Anal Biochem 336 2005 125 131 (Pubitemid 39593508)
16. E. Flashman, E.A. Bagg, R. Chowdhury, J. Mecinovic, C. Loenarz, and M.A. McDonough Kinetic rationale for selectivity toward N- and C-terminal oxygen-dependent degradation domain substrates mediated by a loop region of hypoxia-inducible factor prolyl hydroxylases J Biol Chem 283 2008 3808 3815
17. J.H. Dao, R.J. Kurzeja, J.M. Morachis, H. Veith, J. Lewis, and V. Yu Kinetic characterization and identification of a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 using a time-resolved fluorescence resonance energy transfer-based assay technology Anal Biochem 384 2009 213 223
18. P. Koivunen, M. Hirsila, A.M. Remes, I.E. Hassinen, K.I. Kivirikko, and J. Myllyharju Inhibition of hypoxia-inducible factor (HIF) hydroxylases by citric acid cycle intermediates: possible links between cell metabolism and stabilization of HIF J Biol Chem 282 2007 4524 4532 (Pubitemid 47100953)
19. E.A. Siess, D.G. Brocks, H.K. Lattke, and O.H. Wieland Effect of glucagon on metabolite compartmentation in isolated rat liver cells during gluconeogenesis from lactate Biochem J 166 1977 225 235 (Pubitemid 8157772)
20. D. Haussinger, and H. Sies Effect of phenylephrine on glutamate and glutamine metabolism in isolated perfused rat liver Biochem J 221 1984 651 658 (Pubitemid 14061646)
21. F.R. Sharp, and M. Bernaudin HIF1 and oxygen sensing in the brain Nat Rev Neurosci 5 2004 437 448 (Pubitemid 38715511)
22. E.A. Lipscomb, P.D. Sarmiere, R.J. Crowder, and R.S. Freeman Expression of the SM-20 gene promotes death in nerve growth factor-dependent sympathetic neurons J Neurochem 73 1999 429 432 (Pubitemid 29289152)
23. E.A. Lipscomb, P.D. Sarmiere, and R.S. Freeman SM-20 is a novel mitochondrial protein that causes caspase-dependent cell death in nerve growth factor-dependent neurons J Biol Chem 276 2001 5085 5092