Oliver Werz

Summary

Affiliation: Frankfurt am Main
Country: Germany

Publications

  1. ncbi request reprint 5-Lipoxygenase activation by MAPKAPK-2 and ERKs
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Germany
    Adv Exp Med Biol 525:129-32. 2003
  2. ncbi request reprint 5-lipoxygenase: cellular biology and molecular pharmacology
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, D 60439 Frankfurt, Germany
    Curr Drug Targets Inflamm Allergy 1:23-44. 2002
  3. ncbi request reprint Suppression of receptor-mediated Ca2+ mobilization and functional leukocyte responses by hyperforin
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, D 60439 Frankfurt, Germany
    Biochem Pharmacol 67:1531-9. 2004
  4. ncbi request reprint Extracellular signal-regulated kinases phosphorylate 5-lipoxygenase and stimulate 5-lipoxygenase product formation in leukocytes
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, D 60439 Frankfurt, Germany
    FASEB J 16:1441-3. 2002
  5. ncbi request reprint Activation of 5-lipoxygenase by cell stress is calcium independent in human polymorphonuclear leukocytes
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    Blood 99:1044-52. 2002
  6. ncbi request reprint Hyperforin is a novel type of 5-lipoxygenase inhibitor with high efficacy in vivo
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Max von Laue Str 9, 60438 Frankfurt, Germany
    Cell Mol Life Sci 66:2759-71. 2009
  7. ncbi request reprint Phosphorylation- and stimulus-dependent inhibition of cellular 5-lipoxygenase activity by nonredox-type inhibitors
    Lutz Fischer
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    FASEB J 17:949-51. 2003
  8. doi request reprint SAR studies of acidic dual γ-secretase/PPARγ modulators
    Martina Hieke
    Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max von Laue Str 9, D 60438 Frankfurt am Main, Germany
    Bioorg Med Chem 19:5372-82. 2011
  9. pmc Coupling of boswellic acid-induced Ca2+ mobilisation and MAPK activation to lipid metabolism and peroxide formation in human leucocytes
    Anja Altmann
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, Frankfurt D 60439, Germany
    Br J Pharmacol 141:223-32. 2004
  10. doi request reprint Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid
    Martina Hieke
    Institute of Pharmaceutical Chemistry, ZAFES LiFF Goethe University Frankfurt, Frankfurt am Main, Germany
    J Med Chem 54:4490-507. 2011

Collaborators

Detail Information

Publications56

  1. ncbi request reprint 5-Lipoxygenase activation by MAPKAPK-2 and ERKs
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Germany
    Adv Exp Med Biol 525:129-32. 2003
  2. ncbi request reprint 5-lipoxygenase: cellular biology and molecular pharmacology
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, D 60439 Frankfurt, Germany
    Curr Drug Targets Inflamm Allergy 1:23-44. 2002
    ..This review highlights the determinants of cellular 5-LO activity and summarizes the molecular pharmacology of 5-LO...
  3. ncbi request reprint Suppression of receptor-mediated Ca2+ mobilization and functional leukocyte responses by hyperforin
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, D 60439 Frankfurt, Germany
    Biochem Pharmacol 67:1531-9. 2004
    ..Our data suggest that hyperforin targets component(s) within G protein signaling cascades that regulate Ca(2+) homeostasis, coupled to proinflammatory leukocyte functions...
  4. ncbi request reprint Extracellular signal-regulated kinases phosphorylate 5-lipoxygenase and stimulate 5-lipoxygenase product formation in leukocytes
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, D 60439 Frankfurt, Germany
    FASEB J 16:1441-3. 2002
    ..Finally, the data suggest that ERKs and p38 MAPK-regulated MAPKAPKs can act in conjunction to stimulate 5-LO by phosphorylation...
  5. ncbi request reprint Activation of 5-lipoxygenase by cell stress is calcium independent in human polymorphonuclear leukocytes
    Oliver Werz
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    Blood 99:1044-52. 2002
    ..This mechanism could function independently of Ca(++)-mediated 5-LO activation for stimulation of leukotriene biosynthesis under physiologic conditions as well as in inflammatory diseases...
  6. ncbi request reprint Hyperforin is a novel type of 5-lipoxygenase inhibitor with high efficacy in vivo
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Max von Laue Str 9, 60438 Frankfurt, Germany
    Cell Mol Life Sci 66:2759-71. 2009
    ..Together, hyperforin is a novel type of 5-LO inhibitor apparently acting by interference with the C2-like domain, with high effectiveness in vivo...
  7. ncbi request reprint Phosphorylation- and stimulus-dependent inhibition of cellular 5-lipoxygenase activity by nonredox-type inhibitors
    Lutz Fischer
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    FASEB J 17:949-51. 2003
    ....
  8. doi request reprint SAR studies of acidic dual γ-secretase/PPARγ modulators
    Martina Hieke
    Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max von Laue Str 9, D 60438 Frankfurt am Main, Germany
    Bioorg Med Chem 19:5372-82. 2011
    ..Compound 17 showed an IC(50) Aβ42=2.4 μM and an EC(50) PPARγ=7.2 μM and could be a valuable tool to further evaluate the concept of dual γ-secretase/PPARγ modulators in animal models of Alzheimer's disease...
  9. pmc Coupling of boswellic acid-induced Ca2+ mobilisation and MAPK activation to lipid metabolism and peroxide formation in human leucocytes
    Anja Altmann
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, Frankfurt D 60439, Germany
    Br J Pharmacol 141:223-32. 2004
    ....
  10. doi request reprint Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid
    Martina Hieke
    Institute of Pharmaceutical Chemistry, ZAFES LiFF Goethe University Frankfurt, Frankfurt am Main, Germany
    J Med Chem 54:4490-507. 2011
    ..Together, we provide novel promising lead compounds for the treatment of inflammatory diseases valuable for further investigations in vivo...
  11. pmc Induction of central signalling pathways and select functional effects in human platelets by beta-boswellic acid
    Daniel Poeckel
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Str 9, Frankfurt D 60439, Germany
    Br J Pharmacol 146:514-24. 2005
    ..In summary, beta-BA potently induces Ca2+ mobilisation as well as the activation of pivotal protein kinases, and elicits functional platelet responses such as thrombin generation, liberation of AA, and aggregation...
  12. ncbi request reprint Inhibitors of actin polymerisation stimulate arachidonic acid release and 5-lipoxygenase activation by upregulation of Ca2+ mobilisation in polymorphonuclear leukocytes involving Src family kinases
    Lutz Fischer
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    Biochim Biophys Acta 1736:109-19. 2005
    ..We conclude that in PMNL, inhibitors of actin polymerisation cause enhancement of intracellular Ca2+ levels through Src family kinase signaling, thereby facilitating stimulus-induced release of AA and 5-LO product formation...
  13. ncbi request reprint The C2-like beta-barrel domain mediates the Ca2+-dependent resistance of 5-lipoxygenase activity against inhibition by glutathione peroxidase-1
    Eva Bürkert
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    J Biol Chem 278:42846-53. 2003
    ..In summary, our data suggest that interaction of Ca2+ at the C2-like domain of 5-LO protects the enzyme against the effect of GPx-1. Apparently, in the presence of Ca2+, a low lipid hydroperoxide level is sufficient for 5-LO activation...
  14. ncbi request reprint Cell type-dependent activation of 5-lipoxygenase by arachidonic acid
    Eva Bürkert
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    J Leukoc Biol 73:191-200. 2003
    ..Instead, 5-LO activation in MM6 cells required Ca2+ or alternative signaling pathways induced by hyperosmotic stress. In summary, mechanisms for activation of 5-LO differ considerably between cell types...
  15. ncbi request reprint Evaluation of hyperforin analogues for inhibition of 5-lipoxygenase
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Str 9, D 60439 Frankfurt, Germany
    Med Chem 1:287-91. 2005
    ..Our data show that some of the oxidised hyperforin derivatives possess even improved efficacy, whereas alkylation and acylation have detrimental effects...
  16. ncbi request reprint The aminosteroid phospholipase C antagonist U-73122 (1-[6-[[17-beta-3-methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione) potently inhibits human 5-lipoxygenase in vivo and in vitro
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Germany
    Mol Pharmacol 67:1751-7. 2005
    ..Since 5-LO products induce increases in [Ca2+]i via GPCRs, caution should be used when interpreting data where U-73122 is used as tool to determine a direct role of PLC in receptor-mediated Ca2+ mobilization...
  17. doi request reprint The role of diacylglyceride generation by phospholipase D and phosphatidic acid phosphatase in the activation of 5-lipoxygenase in polymorphonuclear leukocytes
    Dana Albert
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Frankfurt, Germany
    J Leukoc Biol 83:1019-27. 2008
    ..Together, our data suggest that in agonist-stimulated PMNL, the endogenous formation of DAGs via the PLD/PA-P pathway determines 5-LO activation...
  18. ncbi request reprint Analysis of the 5-lipoxygenase promoter and characterization of a vitamin D receptor binding site
    Bernd L Sorg
    Institute of Pharmaceutical Chemistry ZAFES, University of Frankfurt, Marie Curie Str 9, D 60439 Frankfurt, Germany
    Biochim Biophys Acta 1761:686-97. 2006
    ....
  19. ncbi request reprint 1-Oleoyl-2-acetylglycerol stimulates 5-lipoxygenase activity via a putative (phospho)lipid binding site within the N-terminal C2-like domain
    Christina Hörnig
    Institute of Pharmaceutical Chemistry, ZAFES, University of Frankfurt, D 60439 Frankfurt, Germany
    J Biol Chem 280:26913-21. 2005
    ..We conclude that OAG directly stimulates 5-LO by acting at a phospholipid binding site located within the C2-like domain...
  20. ncbi request reprint Induction of 5-lipoxygenase activation in polymorphonuclear leukocytes by 1-oleoyl-2-acetylglycerol
    Dana Albert
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Str 9, D 60439, Frankfurt, Germany
    Biochim Biophys Acta 1631:85-93. 2003
    ..Together, OAG acts as a direct agonist for 5-LO product synthesis in PMNL stimulating 5-LO by novel undefined mechanisms...
  21. ncbi request reprint DNA methylation regulates 5-lipoxygenase promoter activity
    Johannes Uhl
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Germany
    Adv Exp Med Biol 525:169-72. 2003
  22. ncbi request reprint Hyperforin is a dual inhibitor of cyclooxygenase-1 and 5-lipoxygenase
    Dana Albert
    Institute of Pharmaceutical Chemistry, University of Frankfurt, D 60439 Frankfurt, Germany
    Biochem Pharmacol 64:1767-75. 2002
    ....
  23. ncbi request reprint Monocyte-derived soluble protein confers 5-lipoxygenase activity Ca2+-dependent
    Eva Bürkert
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Frankfurt, Germany
    Biochem Biophys Res Commun 295:985-91. 2002
    ..Further characterization showed that this factor is a 80-100 kDa heat-sensitive protein...
  24. pmc Caspase-mediated degradation of human 5-lipoxygenase in B lymphocytic cells
    Oliver Werz
    Institutes of Pharmaceutical Chemistry and Organic Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    Proc Natl Acad Sci U S A 102:13164-9. 2005
    ..We suggest that splitting of BL41-E95-A cells induces de novo synthesis of a protein involved in the activation of casp-6, which cleaves 5-LO...
  25. pmc Molecular pharmacological profile of the nonredox-type 5-lipoxygenase inhibitor CJ-13,610
    Lutz Fischer
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Str 9, Frankfurt D 60439, Germany
    Br J Pharmacol 142:861-8. 2004
    ..In summary, CJ-13,610 may possess considerable potential as a potent orally active nonredox-type 5-LO inhibitor that lacks certain disadvantages of former representatives of this class of 5-LO inhibitors...
  26. ncbi request reprint Identification of molecular targets of the oligomeric nonprenylated acylphloroglucinols from Myrtus communis and their implication as anti-inflammatory compounds
    Christian Feisst
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Frankfurt, Germany
    J Pharmacol Exp Ther 315:389-96. 2005
    ....
  27. doi request reprint Inhibition of 5-lipoxygenase by U73122 is due to covalent binding to cysteine 416
    Michael Hörnig
    Institute of Pharmaceutical Chemistry ZAFES, University of Frankfurt, Max von Laue Str 9, D 60438 Frankfurt, Germany
    Biochim Biophys Acta 1821:279-86. 2012
    ..Together, our data suggest that the area around Cys416 which is close to the proposed AA entry channel to the active site is an interesting target for the development of new 5-LO inhibitors...
  28. ncbi request reprint Boswellic acids activate p42(MAPK) and p38 MAPK and stimulate Ca(2+) mobilization
    Anja Altmann
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    Biochem Biophys Res Commun 290:185-90. 2002
    ..Our results suggest that 11-keto-BAs might function as potent activators of PMNL by stimulation of MAPK and mobilization of intracellular Ca(2+)...
  29. ncbi request reprint Hypertonicity suppresses ionophore-induced product formation and translocation of 5-lipoxygenase in human leukocytes
    Eva Bürkert
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    J Leukoc Biol 71:477-86. 2002
    ..In summary, we show that hypertonicity blocks agonist-induced release of AA, 5-LO product formation, and translocation and in parallel, prevents activation of p38 MAPK and downstream 5-LO kinases in leukocytes...
  30. doi request reprint Identification of human cathepsin G as a functional target of boswellic acids from the anti-inflammatory remedy frankincense
    Lars Tausch
    Institute of Pharmaceutical Chemistry, Johann Wolfgang Goethe University Frankfurt, Frankfurt, Germany
    J Immunol 183:3433-42. 2009
    ..In conclusion, we show that catG is a functional and pharmacologically relevant target of BAs, and interference with catG could explain some of the anti-inflammatory properties of frankincense...
  31. doi request reprint Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo
    Thomas Hanke
    Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max von Laue Strasse 9, D 60438 Frankfurt am Main, Germany
    J Med Chem 56:9031-44. 2013
    ..Together, 2-aminothiazole-featured pirinixic acids represent potent dual 5-LO/mPGES-1 inhibitors with an attractive pharmacological profile as anti-inflammatory drugs. ..
  32. ncbi request reprint Extraction and visualization of potential pharmacophore points using support vector machines: application to ligand-based virtual screening for COX-2 inhibitors
    Lutz Franke
    Institut für Organische Chemie und Chemische Biologie and Institut für Pharmazeutische Chemie, Johann Wolfgang Goethe Universitat, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    J Med Chem 48:6997-7004. 2005
    ..It was demonstrated that the SVM machine-learning method can be used in virtual screening and be analyzed in a human-interpretable way that results in a set of rules for designing novel molecules...
  33. ncbi request reprint Myrtucommulone from Myrtus communis induces apoptosis in cancer cells via the mitochondrial pathway involving caspase-9
    Irina Tretiakova
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Max von Laue Strasse 9, Frankfurt am Main, Germany
    Apoptosis 13:119-31. 2008
    ..Conclusively, MC induces apoptosis in cancer cell lines, with marginal cytotoxicity for non-transformed cells, via the mitochondrial cytochrome c/Apaf-1/caspase-9 pathway...
  34. ncbi request reprint The 5-lipoxygenase promoter is regulated by DNA methylation
    Johannes Uhl
    Institutes of Pharmaceutical Chemistry and Microbiology, University of Frankfurt, Marie Curie Strasse 9, D 60439 Frankfurt, Germany
    J Biol Chem 277:4374-9. 2002
    ....
  35. ncbi request reprint Development of 5-lipoxygenase inhibitors--lessons from cellular enzyme regulation
    Oliver Werz
    Institute of Pharmaceutical Chemistry ZAFES, University of Frankfurt, Marie Curie Str 9, D 60439 Frankfurt, Germany
    Biochem Pharmacol 70:327-33. 2005
    ..This comment focuses on the impact of these stimulatory and inhibitory pathways on the efficacy of 5-LO inhibitors and suggests additional criteria for the development of this class of compounds...
  36. doi request reprint Celecoxib inhibits 5-lipoxygenase
    Thorsten J Maier
    Pharmazentrum frankfurt ZAFES, Institute of Clinical Pharmacology, Johann Wolfgang Goethe University, Theodor Stern Kai 7, 60590 Frankfurt Main, Germany
    Biochem Pharmacol 76:862-72. 2008
    ..2 mg/kg. Together, celecoxib is a direct inhibitor of 5-LO in vitro and in vivo. These findings provide a potential molecular basis for some of the described COX-2-independent pharmacological effects of celecoxib...
  37. ncbi request reprint Identification of pirinixic acid derivatives bearing a 2-aminothiazole moiety combines dual PPARα/γ activation and dual 5-LO/mPGES-1 inhibition
    Thomas Hanke
    Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max von Laue Str 9, D 60438 Frankfurt am Main, Germany
    Bioorg Med Chem Lett 24:3757-63. 2014
    ..Therefore, docking of 13 on PPARγ was performed to determine the potential binding mode. ..
  38. ncbi request reprint Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity
    Martina Hieke
    Institute of Pharmaceutical Chemistry, ZAFES LiFF Goethe University Frankfurt, Max von Laue Strasse 9, D 60438 Frankfurt am Main, Germany
    J Med Chem 53:4691-700. 2010
    ..0 microM, EC(50)(PPARgamma) = 11.0 microM) and the replacement of the two phenyl residues of 8 by cyclohexyl yielding compound 22 (IC(50)(Abeta42) = 5.1 microM, EC(50)(PPARgamma) = 6.6 microM)...
  39. doi request reprint Development of a method for expression and purification of the regulatory C2-like domain of human 5-lipoxygenase
    Angela A Y Michel
    Institute of Pharmaceutical Chemistry, University of Frankfurt, Max von Laue Str 9, D 60438 Frankfurt, Germany
    Protein Expr Purif 59:110-6. 2008
    ....
  40. ncbi request reprint Inhibition of 5-lipoxygenase product synthesis by natural compounds of plant origin
    Oliver Werz
    Department of Pharmaceutical Analytics, Pharmaceutical Institute, Eberhard Karls University Tuebingen, Tuebingen, Germany
    Planta Med 73:1331-57. 2007
    ..In the second part, natural compounds that interfere with 5-LO product formation are compiled and grouped into structural classes, and the underlying molecular mechanisms and structure-activity relationships are discussed...
  41. ncbi request reprint Cholesterol and its anionic derivatives inhibit 5-lipoxygenase activation in polymorphonuclear leukocytes and MonoMac6 cells
    Dmitry A Aleksandrov
    A N Belozersky Institute of Physicochemical Biology, Moscow State University, Russia
    FEBS J 273:548-57. 2006
    ..The fact that cellular LT production is regulated by sulfated cholesterol highlights a possible regulatory role of sulfotransferases/sulfatases in 5-LO product synthesis...
  42. ncbi request reprint 3-O-acetyl-11-keto-boswellic acid decreases basal intracellular Ca2+ levels and inhibits agonist-induced Ca2+ mobilization and mitogen-activated protein kinase activation in human monocytic cells
    Daniel Poeckel
    Department of Pharmaceutical Analysis, Institute of Pharmacy, Eberhard Karls University Tubingen, Auf der Morgenstelle 8, 72076 Tubingen, Germany
    J Pharmacol Exp Ther 316:224-32. 2006
    ..Interruption of these events may represent a possible mechanism underlying the reported anti-inflammatory properties of AKBA...
  43. pmc Coactosin-like protein supports 5-lipoxygenase enzyme activity and up-regulates leukotriene A4 production
    Marija Rakonjac
    Department of Medical Biochemistry and Biophysics, Division of Physiological Chemistry II, Karolinska Institutet, S 171 77 Stockholm, Sweden
    Proc Natl Acad Sci U S A 103:13150-5. 2006
    ..Furthermore, in stimulated cells, CLP appears to function in a complex together with 5LO and membranes, increasing the capacity of 5LO for leukotriene biosynthesis...
  44. ncbi request reprint Carnosic acid and carnosol potently inhibit human 5-lipoxygenase and suppress pro-inflammatory responses of stimulated human polymorphonuclear leukocytes
    Daniel Poeckel
    Department of Pharmaceutical Analytics, Pharmaceutical Institute, Eberhard Karls University Tubingen, Auf der Morgenstelle 8, D 72076 Tubingen, Germany
    Biochem Pharmacol 76:91-7. 2008
    ..4.21.37). Together, our findings provide a pharmacological basis for the anti-inflammatory properties reported for CS- and CA-containing extracts...
  45. ncbi request reprint Extracellular signal-regulated kinase-2 phosphorylates RORalpha4 in vitro
    Adriane Lechtken
    Institute of Pharmaceutical Chemistry ZAFES, Johann Wolfgang Goethe University Frankfurt, Max von Laue Strasse 9, 60438 Frankfurt am Main, Germany
    Biochem Biophys Res Commun 358:890-6. 2007
    ..The RORalpha4-T128A mutant exhibits an increased DNA-binding affinity, an increased transcriptional activity and, in the interplay with the opponent RevErbalpha, acts as a stronger competitor at ROR response elements than RORalpha4-WT...
  46. ncbi request reprint 5-Lipoxygenase: regulation of expression and enzyme activity
    Olof Radmark
    Department of Medical Biochemistry and Biophysics, Division of Physiological Chemistry II, Karolinska Institutet, S 17177 Stockholm, Sweden
    Trends Biochem Sci 32:332-41. 2007
    ..With regard to the control of enzyme activity, many of these findings focus on the N-terminal domain of 5-LO...
  47. ncbi request reprint Therapeutic options for 5-lipoxygenase inhibitors
    Oliver Werz
    Pharmaceutical Institute, University of Tubingen, Auf der Morgenstelle 8, D 72076 Tubingen, Germany
    Pharmacol Ther 112:701-18. 2006
    ..In this review, we summarize the knowledge on possible functions of the 5-LO pathway in various diseases like asthma, cancer and cardiovascular events and review the corresponding potential therapeutic roles of 5-LO inhibitors...
  48. ncbi request reprint Boswellic acids stimulate arachidonic acid release and 12-lipoxygenase activity in human platelets independent of Ca2+ and differentially interact with platelet-type 12-lipoxygenase
    Daniel Poeckel
    Department of Pharmaceutical Analytics, Institute of Pharmacy, Eberhard Karls University Tubingen, Auf der Morgenstelle 8, D 72076 Tubingen, Germany
    Mol Pharmacol 70:1071-8. 2006
    ....
  49. ncbi request reprint Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2)
    Oliver Werz
    Department of Medical Biochemistry and Biophysics, Division of Physiological Chemistry II, Karolinska Institutet, S 171 77 Stockholm, Sweden
    J Biol Chem 277:14793-800. 2002
    ....
  50. ncbi request reprint Inhibition of human 5-lipoxygenase and anti-neoplastic effects by 2-amino-1,4-benzoquinones
    Daniel Poeckel
    Department of Pharmaceutical Analytics, Institute of Pharmacy, Eberhard Karls University Tubingen, Auf der Morgenstelle 8, 72076 Tubingen, Germany
    Med Chem 2:591-5. 2006
    ..Based on these features, bioactive 2-amino-1,4-benzoquinones may possess potential for the pharmacological treatment of diseases associated with elevated 5-lipoxygenase activity, in particular certain types of cancer...
  51. ncbi request reprint GC-rich sequences in the 5-lipoxygenase gene promoter are required for expression in Mono Mac 6 cells, characterization of a novel Sp1 binding site
    David Dishart
    Department of Medical Biochemistry and Biophysics, Division of Physiological Chemistry II Karolinska Institutet, S 171 77 Stockholm, Sweden
    Biochim Biophys Acta 1738:37-47. 2005
    ..Thus, the GC-rich part of the 5LO gene promoter, including a novel Sp1 site, appear important for basal (rather than upregulated) transcription of 5LO in MM6 cells...
  52. ncbi request reprint Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid
    Oliver Werz
    Department of Pharmaceutical Analytics, Pharmaceutical Institute, Eberhard Karls University Tuebingen, Auf der Morgenstelle 8, D 72076 Tuebingen, Germany
    J Med Chem 51:5449-53. 2008
    ..6 microM). These derivatives may possess potential for intervention with inflammatory and allergic diseases...
  53. ncbi request reprint Identification of natural-product-derived inhibitors of 5-lipoxygenase activity by ligand-based virtual screening
    Lutz Franke
    Institut für Organische Chemie und Chemische Biologie ZAFES, Johann Wolfgang Goethe Universitat, Siesmayerstrasse 70, D 60323 Frankfurt am Main, Germany
    J Med Chem 50:2640-6. 2007
    ..The results demonstrate the potential of natural-product-derived screening libraries for hit and lead structure identification...
  54. doi request reprint ALOX5 variants associated with susceptibility to human pulmonary tuberculosis
    Florian Herb
    Department of Molecular Medicine, Bernhard Nocht Institute for Tropical Medicine, Hamburg, Germany
    Hum Mol Genet 17:1052-60. 2008
    ..003, OR 1.50). Our observation of an association of ALOX5 variants with susceptibility to TB contributes evidence of the importance of 5-LO products to the regulation of immune responses to M. tuberculosis...
  55. ncbi request reprint Identification and functional analysis of cyclooxygenase-1 as a molecular target of boswellic acids
    Ulf Siemoneit
    Department of Pharmaceutical Analytics, Institute of Pharmacy, Eberhard Karls University Tuebingen, D 72076 Tuebingen, Germany
    Biochem Pharmacol 75:503-13. 2008
    ..In conclusion, BAs, in particular AKBA, directly interfere with COX-1 and may mediate their anti-inflammatory actions not only by suppression of lipoxygenases, but also by inhibiting cyclooxygenases, preferentially COX-1...
  56. ncbi request reprint Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase
    Jens Landwehr
    Department of Medicinal Chemistry, Institute for Pharmacy and Food Chemistry at the Emil Fischer Center, Friedrich Alexander University Erlangen, Schuhstrasse 19, D 91052 Erlangen, Germany
    J Med Chem 49:4327-32. 2006
    ..On the basis of their 5-LO inhibitory properties, these novel 2-amino-5-hydroxyindoles represent potential candidates for the pharmacological intervention with LT-associated diseases...