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Items: 45

1.

Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.

von Berg S, Xue Y, Collins M, Llinas A, Olsson RI, Halvarsson T, Lindskog M, Malmberg J, Jirholt J, Krutrök N, Ramnegård M, Brännström M, Lundqvist A, Lepistö M, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG, Narjes F.

ACS Med Chem Lett. 2019 May 29;10(6):972-977. doi: 10.1021/acsmedchemlett.9b00158. eCollection 2019 Jun 13.

PMID:
31223457
2.

Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design.

Narjes F, Xue Y, von Berg S, Malmberg J, Llinas A, Olsson RI, Jirholt J, Grindebacke H, Leffler A, Hossain N, Lepistö M, Thunberg L, Leek H, Aagaard A, McPheat J, Hansson EL, Bäck E, Tångefjord S, Chen R, Xiong Y, Hongbin G, Hansson TG.

J Med Chem. 2018 Sep 13;61(17):7796-7813. doi: 10.1021/acs.jmedchem.8b00783. Epub 2018 Aug 27.

PMID:
30095900
3.

Theoretical studies of the second step of the nitric oxide synthase reaction: Electron tunneling prevents uncoupling.

Shamovsky I, Belfield G, Lewis R, Narjes F, Ripa L, Tyrchan C, Öberg L, Sjö P.

J Inorg Biochem. 2018 Apr;181:28-40. doi: 10.1016/j.jinorgbio.2018.01.009. Epub 2018 Jan 10.

PMID:
29407906
4.

Benzoxazepines Achieve Potent Suppression of IL-17 Release in Human T-Helper 17 (TH 17) Cells through an Induced-Fit Binding Mode to the Nuclear Receptor RORγ.

Olsson RI, Xue Y, von Berg S, Aagaard A, McPheat J, Hansson EL, Bernström J, Hansson P, Jirholt J, Grindebacke H, Leffler A, Chen R, Xiong Y, Ge H, Hansson TG, Narjes F.

ChemMedChem. 2016 Jan 19;11(2):207-16. doi: 10.1002/cmdc.201500432. Epub 2015 Nov 10.

PMID:
26553345
5.

Identification of indole inhibitors of human hematopoietic prostaglandin D2 synthase (hH-PGDS).

Edfeldt F, Evenäs J, Lepistö M, Ward A, Petersen J, Wissler L, Rohman M, Sivars U, Svensson K, Perry M, Feierberg I, Zhou XH, Hansson T, Narjes F.

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2496-500. doi: 10.1016/j.bmcl.2015.04.065. Epub 2015 Apr 28.

PMID:
25978964
6.

HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.

Evenäs J, Edfeldt F, Lepistö M, Svitacheva N, Synnergren A, Lundquist B, Gränse M, Rönnholm A, Varga M, Wright J, Wei M, Yue S, Wang J, Li C, Li X, Chen G, Liao Y, Lv G, Tjörnebo A, Narjes F.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1315-21. doi: 10.1016/j.bmcl.2014.01.050. Epub 2014 Jan 28.

PMID:
24508129
7.

Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.

Narjes F, Crescenzi B, Ferrara M, Habermann J, Colarusso S, Ferreira Mdel R, Stansfield I, Mackay AC, Conte I, Ercolani C, Zaramella S, Palumbi MC, Meuleman P, Leroux-Roels G, Giuliano C, Fiore F, Di Marco S, Baiocco P, Koch U, Migliaccio G, Altamura S, Laufer R, De Francesco R, Rowley M.

J Med Chem. 2011 Jan 13;54(1):289-301. doi: 10.1021/jm1013105. Epub 2010 Dec 8.

PMID:
21141896
8.

Enhancement of intestinal absorption of 2-methyl cytidine prodrugs.

Cianetti S, Cooper VB, Attenni B, Pucci V, Fiore F, Giuliano C, Laufer R, Gardelli C, Monteagudo E, Narjes F, Pearce GE, Rowley M.

Drug Deliv. 2010 May;17(4):214-22. doi: 10.3109/10717541003667814.

PMID:
20233089
9.

Mechanism of hepatitis C virus RNA polymerase inhibition with dihydroxypyrimidines.

Powdrill MH, Deval J, Narjes F, De Francesco R, Götte M.

Antimicrob Agents Chemother. 2010 Mar;54(3):977-83. doi: 10.1128/AAC.01216-09. Epub 2009 Dec 22.

10.

Identification and biological evaluation of a series of 1H-benzo[de]isoquinoline-1,3(2H)-diones as hepatitis C virus NS5B polymerase inhibitors.

Ontoria JM, Rydberg EH, Di Marco S, Tomei L, Attenni B, Malancona S, Martin Hernando JI, Gennari N, Koch U, Narjes F, Rowley M, Summa V, Carroll SS, Olsen DB, De Francesco R, Altamura S, Migliaccio G, Carfì A.

J Med Chem. 2009 Aug 27;52(16):5217-27. doi: 10.1021/jm900517t.

PMID:
19877603
11.

2-(3-Thienyl)-5,6-dihydroxypyrimidine-4-carboxylic acids as inhibitors of HCV NS5B RdRp.

Pacini B, Avolio S, Ercolani C, Koch U, Migliaccio G, Narjes F, Pacini L, Tomei L, Harper S.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6245-9. doi: 10.1016/j.bmcl.2009.06.106. Epub 2009 Jul 17.

PMID:
19800789
12.

Phosphoramidate prodrugs of 2'-C-methylcytidine for therapy of hepatitis C virus infection.

Gardelli C, Attenni B, Donghi M, Meppen M, Pacini B, Harper S, Di Marco A, Fiore F, Giuliano C, Pucci V, Laufer R, Gennari N, Marcucci I, Leone JF, Olsen DB, MacCoss M, Rowley M, Narjes F.

J Med Chem. 2009 Sep 10;52(17):5394-407. doi: 10.1021/jm900447q.

PMID:
19725579
13.

Optimization of thienopyrrole-based finger-loop inhibitors of the hepatitis C virus NS5B polymerase.

Martin Hernando JI, Ontoria JM, Malancona S, Attenni B, Fiore F, Bonelli F, Koch U, Di Marco S, Colarusso S, Ponzi S, Gennari N, Vignetti SE, Del Rosario Rico Ferreira M, Habermann J, Rowley M, Narjes F.

ChemMedChem. 2009 Oct;4(10):1695-713. doi: 10.1002/cmdc.200900184.

PMID:
19672916
14.

Cyclic phosphoramidates as prodrugs of 2'-C-methylcytidine.

Meppen M, Pacini B, Bazzo R, Koch U, Leone JF, Koeplinger KA, Rowley M, Altamura S, Di Marco A, Fiore F, Giuliano C, Gonzalez-Paz O, Laufer R, Pucci V, Narjes F, Gardelli C.

Eur J Med Chem. 2009 Sep;44(9):3765-70. doi: 10.1016/j.ejmech.2009.04.043. Epub 2009 May 8.

PMID:
19493593
15.

Synthesis and SAR of piperazinyl-N-phenylbenzamides as inhibitors of hepatitis C virus RNA replication in cell culture.

Conte I, Giuliano C, Ercolani C, Narjes F, Koch U, Rowley M, Altamura S, De Francesco R, Neddermann P, Migliaccio G, Stansfield I.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1779-83. doi: 10.1016/j.bmcl.2009.01.066. Epub 2009 Jan 27.

PMID:
19216075
16.

Synthesis and evaluation of novel phosphoramidate prodrugs of 2'-methyl cytidine as inhibitors of hepatitis C virus NS5B polymerase.

Donghi M, Attenni B, Gardelli C, Marco AD, Fiore F, Giuliano C, Laufer R, Leone JF, Pucci V, Rowley M, Narjes F.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1392-5. doi: 10.1016/j.bmcl.2009.01.035. Epub 2009 Jan 19.

PMID:
19181520
17.

Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase.

Stansfield I, Ercolani C, Mackay A, Conte I, Pompei M, Koch U, Gennari N, Giuliano C, Rowley M, Narjes F.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):627-32. doi: 10.1016/j.bmcl.2008.12.068. Epub 2008 Dec 24.

PMID:
19131244
18.

Discovery of pentacyclic compounds as potent inhibitors of hepatitis C virus NS5B RNA polymerase.

Habermann J, Capitò E, Ferreira Mdel R, Koch U, Narjes F.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):633-8. doi: 10.1016/j.bmcl.2008.12.039. Epub 2008 Dec 13.

PMID:
19109015
19.

Binding of a noncovalent inhibitor exploiting the S' region stabilizes the hepatitis C virus NS3 protease conformation in the absence of cofactor.

Gallo M, Pennestri M, Bottomley MJ, Barbato G, Eliseo T, Paci M, Narjes F, De Francesco R, Summa V, Koch U, Bazzo R, Cicero DO.

J Mol Biol. 2009 Jan 30;385(4):1142-55. doi: 10.1016/j.jmb.2008.11.017. Epub 2008 Nov 24.

PMID:
19061898
20.

Development of carboxylic acid replacements in indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.

Stansfield I, Pompei M, Conte I, Ercolani C, Migliaccio G, Jairaj M, Giuliano C, Rowley M, Narjes F.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5143-9. Epub 2007 Jul 7.

PMID:
17681757
21.
22.

Allosteric inhibition of the hepatitis C virus NS5B RNA dependent RNA polymerase.

Koch U, Narjes F.

Infect Disord Drug Targets. 2006 Mar;6(1):31-41. Review.

PMID:
16787302
23.

Identification of thieno[3,2-b]pyrroles as allosteric inhibitors of hepatitis C virus NS5B polymerase.

Ontoria JM, Martìn Hernando JI, Malancona S, Attenni B, Stansfield I, Conte I, Ercolani C, Habermann J, Ponzi S, Di Filippo M, Koch U, Rowley M, Narjes F.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4026-30. Epub 2006 May 22.

PMID:
16714108
24.

2-(2-Thienyl)-5,6-dihydroxy-4-carboxypyrimidines as inhibitors of the hepatitis C virus NS5B polymerase: discovery, SAR, modeling, and mutagenesis.

Koch U, Attenni B, Malancona S, Colarusso S, Conte I, Di Filippo M, Harper S, Pacini B, Giomini C, Thomas S, Incitti I, Tomei L, De Francesco R, Altamura S, Matassa VG, Narjes F.

J Med Chem. 2006 Mar 9;49(5):1693-705.

PMID:
16509585
25.

Preclinical pharmacokinetics and metabolism of a potent non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.

Giuliano C, Fiore F, Di Marco A, Padron Velazquez J, Bishop A, Bonelli F, Gonzalez-Paz O, Marcucci I, Harper S, Narjes F, Pacini B, Monteagudo E, Migliaccio G, Rowley M, Laufer R.

Xenobiotica. 2005 Oct-Nov;35(10-11):1035-54.

PMID:
16393860
26.

Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase.

Harper S, Avolio S, Pacini B, Di Filippo M, Altamura S, Tomei L, Paonessa G, Di Marco S, Carfi A, Giuliano C, Padron J, Bonelli F, Migliaccio G, De Francesco R, Laufer R, Rowley M, Narjes F.

J Med Chem. 2005 Jul 14;48(14):4547-57.

PMID:
15999993
27.

Interdomain communication in hepatitis C virus polymerase abolished by small molecule inhibitors bound to a novel allosteric site.

Di Marco S, Volpari C, Tomei L, Altamura S, Harper S, Narjes F, Koch U, Rowley M, De Francesco R, Migliaccio G, Carfí A.

J Biol Chem. 2005 Aug 19;280(33):29765-70. Epub 2005 Jun 13.

28.

Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.

Harper S, Pacini B, Avolio S, Di Filippo M, Migliaccio G, Laufer R, De Francesco R, Rowley M, Narjes F.

J Med Chem. 2005 Mar 10;48(5):1314-7.

PMID:
15743173
29.

Active site inhibitors of HCV NS5B polymerase. The development and pharmacophore of 2-thienyl-5,6-dihydroxypyrimidine-4-carboxylic acid.

Stansfield I, Avolio S, Colarusso S, Gennari N, Narjes F, Pacini B, Ponzi S, Harper S.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5085-8.

PMID:
15380204
30.

SAR and pharmacokinetic studies on phenethylamide inhibitors of the hepatitis C virus NS3/NS4A serine protease.

Malancona S, Colarusso S, Ontoria JM, Marchetti A, Poma M, Stansfield I, Laufer R, Di Marco A, Taliani M, Verdirame M, Gonzalez-Paz O, Matassa VG, Narjes F.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4575-9.

PMID:
15357995
31.

Capped dipeptide phenethylamide inhibitors of the HCV NS3 protease.

Nizi E, Koch U, Ontoria JM, Marchetti A, Narjes F, Malancona S, Matassa VG, Gardelli C.

Bioorg Med Chem Lett. 2004 May 3;14(9):2151-4.

PMID:
15080998
32.

Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.

Tomei L, Altamura S, Bartholomew L, Biroccio A, Ceccacci A, Pacini L, Narjes F, Gennari N, Bisbocci M, Incitti I, Orsatti L, Harper S, Stansfield I, Rowley M, De Francesco R, Migliaccio G.

J Virol. 2003 Dec;77(24):13225-31.

33.

In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor.

Trozzi C, Bartholomew L, Ceccacci A, Biasiol G, Pacini L, Altamura S, Narjes F, Muraglia E, Paonessa G, Koch U, De Francesco R, Steinkuhler C, Migliaccio G.

J Virol. 2003 Mar;77(6):3669-79.

34.

Recent developments in the discovery of hepatitis C virus serine protease inhibitors--towards a new class of antiviral agents?

Narjes F, Koch U, Steinkühler C.

Expert Opin Investig Drugs. 2003 Feb;12(2):153-63. Review.

PMID:
12556211
35.

Phenethyl amides as novel noncovalent inhibitors of hepatitis C virus NS3/4A protease: discovery, initial SAR, and molecular modeling.

Colarusso S, Koch U, Gerlach B, Steinkühler C, De Francesco R, Altamura S, Matassa VG, Narjes F.

J Med Chem. 2003 Jan 30;46(3):345-8.

PMID:
12540231
36.

Evolution, synthesis and SAR of tripeptide alpha-ketoacid inhibitors of the hepatitis C virus NS3/NS4A serine protease.

Colarusso S, Gerlach B, Koch U, Muraglia E, Conte I, Stansfield I, Matassa VG, Narjes F.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):705-8.

PMID:
11844706
37.

A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCV NS3 protease.

Narjes F, Koehler KF, Koch U, Gerlach B, Colarusso S, Steinkühler C, Brunetti M, Altamura S, De Francesco R, Matassa VG.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):701-4.

PMID:
11844705
38.

Characterization of the hepatitis C virus NS2/3 processing reaction by using a purified precursor protein.

Pallaoro M, Lahm A, Biasiol G, Brunetti M, Nardella C, Orsatti L, Bonelli F, Orrù S, Narjes F, Steinkühler C.

J Virol. 2001 Oct;75(20):9939-46.

39.

Hepatitis C virus protease inhibitors: current progress and future challenges.

Steinkühler C, Koch U, Narjes F, Matassa VG.

Curr Med Chem. 2001 Jul;8(8):919-932. Review.

PMID:
11375758
40.

Probing the active site of the hepatitis C virus serine protease by fluorescence resonance energy transfer.

Fattori D, Urbani A, Brunetti M, Ingenito R, Pessi A, Prendergast K, Narjes F, Matassa VG, De Francesco R, Steinkühler C.

J Biol Chem. 2000 May 19;275(20):15106-13.

41.

Inhibitor binding induces active site stabilization of the HCV NS3 protein serine protease domain.

Barbato G, Cicero DO, Cordier F, Narjes F, Gerlach B, Sambucini S, Grzesiek S, Matassa VG, De Francesco R, Bazzo R.

EMBO J. 2000 Mar 15;19(6):1195-206.

42.

Inhibition of the hepatitis C virus NS3/4A protease. The crystal structures of two protease-inhibitor complexes.

Di Marco S, Rizzi M, Volpari C, Walsh MA, Narjes F, Colarusso S, De Francesco R, Matassa VG, Sollazzo M.

J Biol Chem. 2000 Mar 10;275(10):7152-7.

43.

Alpha-ketoacids are potent slow binding inhibitors of the hepatitis C virus NS3 protease.

Narjes F, Brunetti M, Colarusso S, Gerlach B, Koch U, Biasiol G, Fattori D, De Francesco R, Matassa VG, Steinkühler C.

Biochemistry. 2000 Feb 22;39(7):1849-61.

PMID:
10677236
44.

Substrate specificity of the hepatitis C virus serine protease NS3.

Urbani A, Bianchi E, Narjes F, Tramontano A, De Francesco R, Steinkühler C, Pessi A.

J Biol Chem. 1997 Apr 4;272(14):9204-9.

45.

A continuous assay of hepatitis C virus protease based on resonance energy transfer depsipeptide substrates.

Taliani M, Bianchi E, Narjes F, Fossatelli M, Urbani A, Steinkühler C, De Francesco R, Pessi A.

Anal Biochem. 1996 Aug 15;240(1):60-7.

PMID:
8811880

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