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Items: 1 to 50 of 54

1.

Androgen-mediated sex bias impairs efficiency of leukotriene biosynthesis inhibitors in males.

Pace S, Pergola C, Dehm F, Rossi A, Gerstmeier J, Troisi F, Pein H, Schaible AM, Weinigel C, Rummler S, Northoff H, Laufer S, Maier TJ, Rådmark O, Samuelsson B, Koeberle A, Sautebin L, Werz O.

J Clin Invest. 2017 Aug 1;127(8):3167-3176. doi: 10.1172/JCI92885. Epub 2017 Jul 24.

2.

Evaluation of Dual 5-Lipoxygenase/Microsomal Prostaglandin E2 Synthase-1 Inhibitory Effect of Natural and Synthetic Acronychia-Type Isoprenylated Acetophenones.

Svouraki A, Garscha U, Kouloura E, Pace S, Pergola C, Krauth V, Rossi A, Sautebin L, Halabalaki M, Werz O, Gaboriaud-Kolar N, Skaltsounis AL.

J Nat Prod. 2017 Mar 24;80(3):699-706. doi: 10.1021/acs.jnatprod.6b01008. Epub 2017 Feb 27.

PMID:
28240894
3.

Selective upregulation of TNFα expression in classically-activated human monocyte-derived macrophages (M1) through pharmacological interference with V-ATPase.

Thomas L, Rao Z, Gerstmeier J, Raasch M, Weinigel C, Rummler S, Menche D, Müller R, Pergola C, Mosig A, Werz O.

Biochem Pharmacol. 2017 Apr 15;130:71-82. doi: 10.1016/j.bcp.2017.02.004. Epub 2017 Feb 9.

PMID:
28189727
4.

Modulation of actin dynamics as potential macrophage subtype-targeting anti-tumour strategy.

Pergola C, Schubert K, Pace S, Ziereisen J, Nikels F, Scherer O, Hüttel S, Zahler S, Vollmar AM, Weinigel C, Rummler S, Müller R, Raasch M, Mosig A, Koeberle A, Werz O.

Sci Rep. 2017 Jan 30;7:41434. doi: 10.1038/srep41434.

5.

Multiplex immunoassay for in vitro characterization of acellular pertussis antigens in combination vaccines.

Agnolon V, Bruno C, Galletti B, Mori E, Ugozzoli M, Pergola C, O'Hagan DT, Baudner BC.

Vaccine. 2016 Feb 17;34(8):1040-6. doi: 10.1016/j.vaccine.2016.01.012. Epub 2016 Jan 17.

PMID:
26784684
6.

2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors.

Di Micco S, Spatafora C, Cardullo N, Riccio R, Fischer K, Pergola C, Koeberle A, Werz O, Chalal M, Vervandier-Fasseur D, Tringali C, Bifulco G.

Bioorg Med Chem. 2016 Feb 15;24(4):820-6. doi: 10.1016/j.bmc.2016.01.002. Epub 2016 Jan 4.

PMID:
26777299
7.

Bronchipret® syrup containing thyme and ivy extracts suppresses bronchoalveolar inflammation and goblet cell hyperplasia in experimental bronchoalveolitis.

Seibel J, Pergola C, Werz O, Kryshen K, Wosikowski K, Lehner MD, Haunschild J.

Phytomedicine. 2015 Dec 1;22(13):1172-7. doi: 10.1016/j.phymed.2015.09.001. Epub 2015 Oct 1.

PMID:
26598916
8.

Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.

Iranshahi M, Chini MG, Masullo M, Sahebkar A, Javidnia A, Chitsazian Yazdi M, Pergola C, Koeberle A, Werz O, Pizza C, Terracciano S, Piacente S, Bifulco G.

J Nat Prod. 2015 Dec 24;78(12):2867-79. doi: 10.1021/acs.jnatprod.5b00700. Epub 2015 Nov 20.

PMID:
26588603
9.

Epidemiology of HEV in the Mediterranean basin: 10-year prevalence in Italy.

Lanini S, Garbuglia AR, Lapa D, Puro V, Navarra A, Pergola C, Ippolito G, Capobianchi MR.

BMJ Open. 2015 Jul 14;5(7):e007110. doi: 10.1136/bmjopen-2014-007110.

10.

Progesterone rapidly down-regulates the biosynthesis of 5-lipoxygenase products in human primary monocytes.

Pergola C, Schaible AM, Nikels F, Dodt G, Northoff H, Werz O.

Pharmacol Res. 2015 Apr;94:42-50. doi: 10.1016/j.phrs.2015.01.007. Epub 2015 Feb 11.

PMID:
25681061
11.

Role of p38 mitogen-activated protein kinase in linking stearoyl-CoA desaturase-1 activity with endoplasmic reticulum homeostasis.

Koeberle A, Pergola C, Shindou H, Koeberle SC, Shimizu T, Laufer SA, Werz O.

FASEB J. 2015 Jun;29(6):2439-49. doi: 10.1096/fj.14-268474. Epub 2015 Feb 12.

PMID:
25678624
12.

Targeting V-ATPase in primary human monocytes by archazolid potently represses the classical secretion of cytokines due to accumulation at the endoplasmic reticulum.

Scherer O, Steinmetz H, Kaether C, Weinigel C, Barz D, Kleinert H, Menche D, Müller R, Pergola C, Werz O.

Biochem Pharmacol. 2014 Oct 15;91(4):490-500. doi: 10.1016/j.bcp.2014.07.028. Epub 2014 Aug 12.

PMID:
25107704
13.

Evaluation in a clinical setting of the performances of a new rapid confirmatory assay for HIV1/2 serodiagnosis.

Abbate I, Pergola C, Pisciotta M, Sciamanna R, Sias C, Orchi N, Libertone R, Ippolito G, Capobianchi MR.

J Clin Virol. 2014 Sep;61(1):166-9. doi: 10.1016/j.jcv.2014.06.015. Epub 2014 Jun 24.

PMID:
25037532
14.

In vivo sex differences in leukotriene biosynthesis in zymosan-induced peritonitis.

Rossi A, Pergola C, Pace S, Rådmark O, Werz O, Sautebin L.

Pharmacol Res. 2014 Sep;87:1-7. doi: 10.1016/j.phrs.2014.05.011. Epub 2014 Jun 2.

PMID:
24892983
15.

Exploration of the dihydropyrimidine scaffold for the development of new potential anti-inflammatory agents blocking prostaglandin E₂ synthase-1 enzyme (mPGES-1).

Lauro G, Strocchia M, Terracciano S, Bruno I, Fischer K, Pergola C, Werz O, Riccio R, Bifulco G.

Eur J Med Chem. 2014 Jun 10;80:407-15. doi: 10.1016/j.ejmech.2014.04.061. Epub 2014 Apr 24.

PMID:
24794772
16.

Indirubin core structure of glycogen synthase kinase-3 inhibitors as novel chemotype for intervention with 5-lipoxygenase.

Pergola C, Gaboriaud-Kolar N, Jestädt N, König S, Kritsanida M, Schaible AM, Li H, Garscha U, Weinigel C, Barz D, Albring KF, Huber O, Skaltsounis AL, Werz O.

J Med Chem. 2014 May 8;57(9):3715-23. doi: 10.1021/jm401740w. Epub 2014 Apr 17.

PMID:
24697244
17.

The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesis in vitro and in vivo by targeting 5-lipoxygenase-activating protein (FLAP).

Pergola C, Gerstmeier J, Mönch B, Çalışkan B, Luderer S, Weinigel C, Barz D, Maczewsky J, Pace S, Rossi A, Sautebin L, Banoglu E, Werz O.

Br J Pharmacol. 2014 Jun;171(12):3051-64. doi: 10.1111/bph.12625.

18.

One-step semisynthesis of oleacein and the determination as a 5-lipoxygenase inhibitor.

Vougogiannopoulou K, Lemus C, Halabalaki M, Pergola C, Werz O, Smith AB 3rd, Michel S, Skaltsounis L, Deguin B.

J Nat Prod. 2014 Mar 28;77(3):441-5. doi: 10.1021/np401010x. Epub 2014 Feb 25.

PMID:
24568174
19.

Elucidation of the molecular mechanism and the efficacy in vivo of a novel 1,4-benzoquinone that inhibits 5-lipoxygenase.

Schaible AM, Filosa R, Temml V, Krauth V, Matteis M, Peduto A, Bruno F, Luderer S, Roviezzo F, Di Mola A, de Rosa M, D'Agostino B, Weinigel C, Barz D, Koeberle A, Pergola C, Schuster D, Werz O.

Br J Pharmacol. 2014 May;171(9):2399-412. doi: 10.1111/bph.12592.

20.

Indirubin-3'-monoxime exerts a dual mode of inhibition towards leukotriene-mediated vascular smooth muscle cell migration.

Blazevic T, Schaible AM, Weinhäupl K, Schachner D, Nikels F, Weinigel C, Barz D, Atanasov AG, Pergola C, Werz O, Dirsch VM, Heiss EH.

Cardiovasc Res. 2014 Mar 1;101(3):522-32. doi: 10.1093/cvr/cvt339. Epub 2013 Dec 23.

21.

Chromatographic separation and biological evaluation of benzimidazole derivative enantiomers as inhibitors of leukotriene biosynthesis.

Sardella R, Levent S, Ianni F, Calişkan B, Gerstmeier J, Pergola C, Werz O, Banoglu E, Natalini B.

J Pharm Biomed Anal. 2014 Feb;89:88-92. doi: 10.1016/j.jpba.2013.10.039. Epub 2013 Nov 7.

PMID:
24270288
22.

High capacity for leukotriene biosynthesis in peripheral blood during pregnancy.

Schaible AM, Koeberle A, Northoff H, Lawrenz B, Weinigel C, Barz D, Werz O, Pergola C.

Prostaglandins Leukot Essent Fatty Acids. 2013 Sep;89(4):245-55. doi: 10.1016/j.plefa.2013.06.004. Epub 2013 Jul 16.

PMID:
23870194
23.

Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP).

Banoglu E, Çalişkan B, Luderer S, Eren G, Özkan Y, Altenhofen W, Weinigel C, Barz D, Gerstmeier J, Pergola C, Werz O.

Bioorg Med Chem. 2012 Jun 15;20(12):3728-41. doi: 10.1016/j.bmc.2012.04.048. Epub 2012 May 1.

PMID:
22607880
24.

Strategy for catch and release of azide-tagged biomolecules utilizing a photolabile strained alkyne construct.

Golkowski M, Pergola C, Werz O, Ziegler T.

Org Biomol Chem. 2012 Jun 21;10(23):4496-9. doi: 10.1039/c2ob25440a. Epub 2012 May 9.

PMID:
22573264
25.

On the inhibition of 5-lipoxygenase product formation by tryptanthrin: mechanistic studies and efficacy in vivo.

Pergola C, Jazzar B, Rossi A, Northoff H, Hamburger M, Sautebin L, Werz O.

Br J Pharmacol. 2012 Feb;165(3):765-76. doi: 10.1111/j.1476-5381.2011.01605.x.

26.

Testosterone suppresses phospholipase D, causing sex differences in leukotriene biosynthesis in human monocytes.

Pergola C, Rogge A, Dodt G, Northoff H, Weinigel C, Barz D, Rådmark O, Sautebin L, Werz O.

FASEB J. 2011 Oct;25(10):3377-87. doi: 10.1096/fj.11-182758. Epub 2011 Jun 21.

PMID:
21693622
27.

Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1.

Greiner C, Zettl H, Koeberle A, Pergola C, Northoff H, Schubert-Zsilavecz M, Werz O.

Bioorg Med Chem. 2011 Jun 1;19(11):3394-401. doi: 10.1016/j.bmc.2011.04.034. Epub 2011 Apr 22.

PMID:
21570310
28.

2-(4-(Biphenyl-4-ylamino)-6-chloropyrimidin-2-ylthio)octanoic acid (HZ52)--a novel type of 5-lipoxygenase inhibitor with favourable molecular pharmacology and efficacy in vivo.

Greiner C, Hörnig C, Rossi A, Pergola C, Zettl H, Schubert-Zsilavecz M, Steinhilber D, Sautebin L, Werz O.

Br J Pharmacol. 2011 Sep;164(2b):781-93. doi: 10.1111/j.1476-5381.2011.01451.x.

29.

Cinnamyl-3,4-dihydroxy-α-cyanocinnamate is a potent inhibitor of 5-lipoxygenase.

Pergola C, Jazzar B, Rossi A, Buehring U, Luderer S, Dehm F, Northoff H, Sautebin L, Werz O.

J Pharmacol Exp Ther. 2011 Jul;338(1):205-13. doi: 10.1124/jpet.111.180794. Epub 2011 Mar 29.

PMID:
21447614
30.

Enlarging the NSAIDs family: ether, ester and acid derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.

Biava M, Porretta GC, Poce G, Battilocchio C, Botta M, Manetti F, Rovini M, Cappelli A, Sautebin L, Rossi A, Pergola C, Ghelardini C, Galeotti N, Makovec F, Giordani A, Anzellotti P, Tacconelli S, Patrignani P, Anzini M.

Curr Med Chem. 2011;18(10):1540-54. Review.

PMID:
21428878
31.

The 5-lipoxygenase inhibitor, zileuton, suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages.

Rossi A, Pergola C, Koeberle A, Hoffmann M, Dehm F, Bramanti P, Cuzzocrea S, Werz O, Sautebin L.

Br J Pharmacol. 2010 Oct;161(3):555-70. doi: 10.1111/j.1476-5381.2010.00930.x.

32.

5-Lipoxygenase inhibitors: a review of recent developments and patents.

Pergola C, Werz O.

Expert Opin Ther Pat. 2010 Mar;20(3):355-75. doi: 10.1517/13543771003602012. Review.

PMID:
20180620
33.

Sulindac sulfide suppresses 5-lipoxygenase at clinically relevant concentrations.

Steinbrink SD, Pergola C, Bühring U, George S, Metzner J, Fischer AS, Häfner AK, Wisniewska JM, Geisslinger G, Werz O, Steinhilber D, Maier TJ.

Cell Mol Life Sci. 2010 Mar;67(5):797-806. doi: 10.1007/s00018-009-0206-0. Epub 2009 Nov 29.

PMID:
20091083
34.

Hyperforin induces Ca(2+)-independent arachidonic acid release in human platelets by facilitating cytosolic phospholipase A(2) activation through select phospholipid interactions.

Hoffmann M, Lopez JJ, Pergola C, Feisst C, Pawelczik S, Jakobsson PJ, Sorg BL, Glaubitz C, Steinhilber D, Werz O.

Biochim Biophys Acta. 2010 Apr;1801(4):462-72. doi: 10.1016/j.bbalip.2009.12.007. Epub 2009 Dec 28.

PMID:
20044029
35.

Novel ester and acid derivatives of the 1,5-diarylpyrrole scaffold as anti-inflammatory and analgesic agents. Synthesis and in vitro and in vivo biological evaluation.

Biava M, Porretta GC, Poce G, Battilocchio C, Manetti F, Botta M, Forli S, Sautebin L, Rossi A, Pergola C, Ghelardini C, Galeotti N, Makovec F, Giordani A, Anzellotti P, Patrignani P, Anzini M.

J Med Chem. 2010 Jan 28;53(2):723-33. doi: 10.1021/jm901269y.

PMID:
19957931
36.

The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.

Koeberle A, Rossi A, Zettl H, Pergola C, Dehm F, Bauer J, Greiner C, Reckel S, Hoernig C, Northoff H, Bernhard F, Dötsch V, Sautebin L, Schubert-Zsilavecz M, Werz O.

J Pharmacol Exp Ther. 2010 Mar;332(3):840-8. doi: 10.1124/jpet.109.160663. Epub 2009 Nov 24.

PMID:
19934399
37.

Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.

Koeberle A, Haberl EM, Rossi A, Pergola C, Dehm F, Northoff H, Troschuetz R, Sautebin L, Werz O.

Bioorg Med Chem. 2009 Dec 1;17(23):7924-32. doi: 10.1016/j.bmc.2009.10.025. Epub 2009 Oct 31.

PMID:
19884011
38.

Interference of alpha-alkyl-substituted pirinixic acid derivatives with neutrophil functions and signalling pathways.

Poeckel D, Greiner C, Pergola C, Henkel A, Popescu L, Rau O, Schubert-Zsilavecz M, Werz O.

Eur J Pharmacol. 2009 Oct 1;619(1-3):1-7. doi: 10.1016/j.ejphar.2009.08.014. Epub 2009 Aug 15.

PMID:
19686721
39.

Hyperforin is a novel type of 5-lipoxygenase inhibitor with high efficacy in vivo.

Feisst C, Pergola C, Rakonjac M, Rossi A, Koeberle A, Dodt G, Hoffmann M, Hoernig C, Fischer L, Steinhilber D, Franke L, Schneider G, Rådmark O, Sautebin L, Werz O.

Cell Mol Life Sci. 2009 Aug;66(16):2759-71. doi: 10.1007/s00018-009-0078-3. Epub 2009 Jul 5.

PMID:
19579006
40.

Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase.

Karg EM, Luderer S, Pergola C, Bühring U, Rossi A, Northoff H, Sautebin L, Troschütz R, Werz O.

J Med Chem. 2009 Jun 11;52(11):3474-83. doi: 10.1021/jm900212y.

PMID:
19492852
41.

On the interference of boswellic acids with 5-lipoxygenase: mechanistic studies in vitro and pharmacological relevance.

Siemoneit U, Pergola C, Jazzar B, Northoff H, Skarke C, Jauch J, Werz O.

Eur J Pharmacol. 2009 Mar 15;606(1-3):246-54. doi: 10.1016/j.ejphar.2009.01.044. Epub 2009 Feb 5.

PMID:
19374837
42.

ERK-mediated regulation of leukotriene biosynthesis by androgens: a molecular basis for gender differences in inflammation and asthma.

Pergola C, Dodt G, Rossi A, Neunhoeffer E, Lawrenz B, Northoff H, Samuelsson B, Rådmark O, Sautebin L, Werz O.

Proc Natl Acad Sci U S A. 2008 Dec 16;105(50):19881-6. doi: 10.1073/pnas.0809120105. Epub 2008 Dec 8.

43.

Myrtucommulone from Myrtus communis exhibits potent anti-inflammatory effectiveness in vivo.

Rossi A, Di Paola R, Mazzon E, Genovese T, Caminiti R, Bramanti P, Pergola C, Koeberle A, Werz O, Sautebin L, Cuzzocrea S.

J Pharmacol Exp Ther. 2009 Apr;329(1):76-86. doi: 10.1124/jpet.108.143214. Epub 2008 Dec 4.

PMID:
19056932
44.

Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.

Biava M, Porretta GC, Poce G, Supino S, Manetti F, Forli S, Botta M, Sautebin L, Rossi A, Pergola C, Ghelardini C, Norcini M, Makovec F, Giordani A, Anzellotti P, Cirilli R, Ferretti R, Gallinella B, La Torre F, Anzini M, Patrignani P.

Bioorg Med Chem. 2008 Sep 1;16(17):8072-81. doi: 10.1016/j.bmc.2008.07.058. Epub 2008 Jul 24.

PMID:
18752957
45.

Celecoxib inhibits 5-lipoxygenase.

Maier TJ, Tausch L, Hoernig M, Coste O, Schmidt R, Angioni C, Metzner J, Groesch S, Pergola C, Steinhilber D, Werz O, Geisslinger G.

Biochem Pharmacol. 2008 Oct 1;76(7):862-72. doi: 10.1016/j.bcp.2008.07.009. Epub 2008 Jul 19.

PMID:
18692027
46.

Synthesis, biological evaluation, and enzyme docking simulations of 1,5-diarylpyrrole-3-alkoxyethyl ethers as selective cyclooxygenase-2 inhibitors endowed with anti-inflammatory and antinociceptive activity.

Anzini M, Rovini M, Cappelli A, Vomero S, Manetti F, Botta M, Sautebin L, Rossi A, Pergola C, Ghelardini C, Norcini M, Giordani A, Makovec F, Anzellotti P, Patrignani P, Biava M.

J Med Chem. 2008 Aug 14;51(15):4476-81. doi: 10.1021/jm800084s. Epub 2008 Jul 4.

PMID:
18598017
47.

The role of diacylglyceride generation by phospholipase D and phosphatidic acid phosphatase in the activation of 5-lipoxygenase in polymorphonuclear leukocytes.

Albert D, Pergola C, Koeberle A, Dodt G, Steinhilber D, Werz O.

J Leukoc Biol. 2008 Apr;83(4):1019-27. doi: 10.1189/jlb.0807531. Epub 2008 Jan 24.

PMID:
18218859
48.

Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity.

Biava M, Porretta GC, Poce G, Supino S, Forli S, Rovini M, Cappelli A, Manetti F, Botta M, Sautebin L, Rossi A, Pergola C, Ghelardini C, Vivoli E, Makovec F, Anzellotti P, Patrignani P, Anzini M.

J Med Chem. 2007 Nov 1;50(22):5403-11. Epub 2007 Oct 4.

PMID:
17915854
49.

The molecular mechanism of the inhibition by licofelone of the biosynthesis of 5-lipoxygenase products.

Fischer L, Hornig M, Pergola C, Meindl N, Franke L, Tanrikulu Y, Dodt G, Schneider G, Steinhilber D, Werz O.

Br J Pharmacol. 2007 Oct;152(4):471-80. Epub 2007 Aug 20.

50.

Inhibition of inducible nitric oxide synthase expression by an acetonic extract from Feijoa sellowiana Berg. fruits.

Rossi A, Rigano D, Pergola C, Formisano C, Basile A, Bramanti P, Senatore F, Sautebin L.

J Agric Food Chem. 2007 Jun 27;55(13):5053-61. Epub 2007 Jun 6.

PMID:
17550270

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