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Viral engagement with host (co-)receptors blocked by a novel class of tryptophan dendrimers that targets the 5-fold-axis of the enterovirus-A71 capsid.

Sun L, Lee H, Thibaut HJ, Lanko K, Rivero-Buceta E, Bator C, Martinez-Gualda B, Dallmeier K, Delang L, Leyssen P, Gago F, San-Félix A, Hafenstein S, Mirabelli C, Neyts J.

PLoS Pathog. 2019 May 9;15(5):e1007760. doi: 10.1371/journal.ppat.1007760. [Epub ahead of print]


PI4KIII inhibitor enviroxime impedes the replication of the hepatitis C virus by inhibiting PI3 kinases.

Delang L, Harak C, Benkheil M, Khan H, Leyssen P, Andrews M, Lohmann V, Neyts J.

J Antimicrob Chemother. 2018 Dec 1;73(12):3375-3384. doi: 10.1093/jac/dky327.


Antiplasmodial, anti-chikungunya virus and antioxidant activities of 64 endemic plants from the Mascarene Islands.

Ledoux A, Cao M, Jansen O, Mamede L, Campos PE, Payet B, Clerc P, Grondin I, Girard-Valenciennes E, Hermann T, Litaudon M, Vanderheydt C, Delang L, Neyts J, Leyssen P, Frédérich M, Smadja J.

Int J Antimicrob Agents. 2018 Nov;52(5):622-628. doi: 10.1016/j.ijantimicag.2018.07.017. Epub 2018 Jul 29.


Assessing medicinal plants traditionally used in the Chirang Reserve Forest, Northeast India for antimicrobial activity.

Panda SK, Das R, Leyssen P, Neyts J, Luyten W.

J Ethnopharmacol. 2018 Oct 28;225:220-233. doi: 10.1016/j.jep.2018.07.011. Epub 2018 Jul 11.


Rational modifications on a benzylidene-acrylohydrazide antiviral scaffold, synthesis and evaluation of bioactivity against Chikungunya virus.

Giancotti G, Cancellieri M, Balboni A, Giustiniano M, Novellino E, Delang L, Neyts J, Leyssen P, Brancale A, Bassetto M.

Eur J Med Chem. 2018 Apr 10;149:56-68. doi: 10.1016/j.ejmech.2018.02.054. Epub 2018 Feb 23.


Bioactivity-Based Molecular Networking for the Discovery of Drug Leads in Natural Product Bioassay-Guided Fractionation.

Nothias LF, Nothias-Esposito M, da Silva R, Wang M, Protsyuk I, Zhang Z, Sarvepalli A, Leyssen P, Touboul D, Costa J, Paolini J, Alexandrov T, Litaudon M, Dorrestein PC.

J Nat Prod. 2018 Apr 27;81(4):758-767. doi: 10.1021/acs.jnatprod.7b00737. Epub 2018 Mar 2.


Structurally Diverse Diterpenoids from Sandwithia guyanensis.

Remy S, Olivon F, Desrat S, Blanchard F, Eparvier V, Leyssen P, Neyts J, Roussi F, Touboul D, Litaudon M.

J Nat Prod. 2018 Apr 27;81(4):901-912. doi: 10.1021/acs.jnatprod.7b01025. Epub 2018 Mar 1.


Inhibition of the Replication of Different Strains of Chikungunya Virus by 3-Aryl-[1,2,3]triazolo[4,5- d]pyrimidin-7(6 H)-ones.

Gómez-SanJuan A, Gamo AM, Delang L, Pérez-Sánchez A, Amrun SN, Abdelnabi R, Jacobs S, Priego EM, Camarasa MJ, Jochmans D, Leyssen P, Ng LFP, Querat G, Neyts J, Pérez-Pérez MJ.

ACS Infect Dis. 2018 Apr 13;4(4):605-619. doi: 10.1021/acsinfecdis.7b00219. Epub 2018 Feb 14.


Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents.

Tardugno R, Giancotti G, De Burghgraeve T, Delang L, Neyts J, Leyssen P, Brancale A, Bassetto M.

Bioorg Med Chem. 2018 Feb 15;26(4):869-874. doi: 10.1016/j.bmc.2018.01.002. Epub 2018 Jan 6.


Antimicrobial, Anthelmintic, and Antiviral Activity of Plants Traditionally Used for Treating Infectious Disease in the Similipal Biosphere Reserve, Odisha, India.

Panda SK, Padhi L, Leyssen P, Liu M, Neyts J, Luyten W.

Front Pharmacol. 2017 Oct 23;8:658. doi: 10.3389/fphar.2017.00658. eCollection 2017.


Environmentally Friendly Procedure Based on Supercritical Fluid Chromatography and Tandem Mass Spectrometry Molecular Networking for the Discovery of Potent Antiviral Compounds from Euphorbia semiperfoliata.

Nothias LF, Boutet-Mercey S, Cachet X, De La Torre E, Laboureur L, Gallard JF, Retailleau P, Brunelle A, Dorrestein PC, Costa J, Bedoya LM, Roussi F, Leyssen P, Alcami J, Paolini J, Litaudon M, Touboul D.

J Nat Prod. 2017 Oct 27;80(10):2620-2629. doi: 10.1021/acs.jnatprod.7b00113. Epub 2017 Sep 19.


Fluorination of Naturally Occurring N⁶-Benzyladenosine Remarkably Increased Its Antiviral Activity and Selectivity.

Oslovsky VE, Drenichev MS, Sun L, Kurochkin NN, Kunetsky VE, Mirabelli C, Neyts J, Leyssen P, Mikhailov SN.

Molecules. 2017 Jul 20;22(7). pii: E1219. doi: 10.3390/molecules22071219.


Isolation of Premyrsinane, Myrsinane, and Tigliane Diterpenoids from Euphorbia pithyusa Using a Chikungunya Virus Cell-Based Assay and Analogue Annotation by Molecular Networking.

Esposito M, Nothias LF, Retailleau P, Costa J, Roussi F, Neyts J, Leyssen P, Touboul D, Litaudon M, Paolini J.

J Nat Prod. 2017 Jul 28;80(7):2051-2059. doi: 10.1021/acs.jnatprod.7b00233. Epub 2017 Jul 3.


Antiviral activity of [1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-ones against chikungunya virus targeting the viral capping nsP1.

Gigante A, Gómez-SanJuan A, Delang L, Li C, Bueno O, Gamo AM, Priego EM, Camarasa MJ, Jochmans D, Leyssen P, Decroly E, Coutard B, Querat G, Neyts J, Pérez-Pérez MJ.

Antiviral Res. 2017 Aug;144:216-222. doi: 10.1016/j.antiviral.2017.06.003. Epub 2017 Jun 12.


Understanding the Mechanism of the Broad-Spectrum Antiviral Activity of Favipiravir (T-705): Key Role of the F1 Motif of the Viral Polymerase.

Abdelnabi R, Morais ATS, Leyssen P, Imbert I, Beaucourt S, Blanc H, Froeyen M, Vignuzzi M, Canard B, Neyts J, Delang L.

J Virol. 2017 May 26;91(12). pii: e00487-17. doi: 10.1128/JVI.00487-17. Print 2017 Jun 15.


Discovery of Multitarget Agents Active as Broad-Spectrum Antivirals and Correctors of Cystic Fibrosis Transmembrane Conductance Regulator for Associated Pulmonary Diseases.

Tassini S, Sun L, Lanko K, Crespan E, Langron E, Falchi F, Kissova M, Armijos-Rivera JI, Delang L, Mirabelli C, Neyts J, Pieroni M, Cavalli A, Costantino G, Maga G, Vergani P, Leyssen P, Radi M.

J Med Chem. 2017 Feb 23;60(4):1400-1416. doi: 10.1021/acs.jmedchem.6b01521. Epub 2017 Feb 10.


Shape-based virtual screening, synthesis and evaluation of novel pyrrolone derivatives as antiviral agents against HCV.

Bassetto M, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, Brancale A.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):936-940. doi: 10.1016/j.bmcl.2016.12.087. Epub 2017 Jan 3.


Protein kinases C as potential host targets for the inhibition of chikungunya virus replication.

Abdelnabi R, Amrun SN, Ng LF, Leyssen P, Neyts J, Delang L.

Antiviral Res. 2017 Mar;139:79-87. doi: 10.1016/j.antiviral.2016.12.020. Epub 2016 Dec 27.


Structure-activity relationship studies on a Trp dendrimer with dual activities against HIV and enterovirus A71. Modifications on the amino acid.

Martínez-Gualda B, Sun L, Rivero-Buceta E, Flores A, Quesada E, Balzarini J, Noppen S, Liekens S, Schols D, Neyts J, Leyssen P, Mirabelli C, Camarasa MJ, San-Félix A.

Antiviral Res. 2017 Mar;139:32-40. doi: 10.1016/j.antiviral.2016.12.010. Epub 2016 Dec 23.


Discovery of novel multi-target indole-based derivatives as potent and selective inhibitors of chikungunya virus replication.

Scuotto M, Abdelnabi R, Collarile S, Schiraldi C, Delang L, Massa A, Ferla S, Brancale A, Leyssen P, Neyts J, Filosa R.

Bioorg Med Chem. 2017 Jan 1;25(1):327-337. doi: 10.1016/j.bmc.2016.10.037. Epub 2016 Oct 31.


Novel symmetrical phenylenediamines as potential anti-hepatitis C virus agents.

Bassetto M, Ferla S, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, O'Donnell R, Brancale A.

Antivir Chem Chemother. 2015 Dec;24(5-6):155-160. doi: 10.1177/2040206616676353. Epub 2016 Nov 4.


In silico identification, design and synthesis of novel piperazine-based antiviral agents targeting the hepatitis C virus helicase.

Bassetto M, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, Courtney-Smith M, Brancale A.

Eur J Med Chem. 2017 Jan 5;125:1115-1131. doi: 10.1016/j.ejmech.2016.10.043. Epub 2016 Oct 23.


Euphorbia dendroides Latex as a Source of Jatrophane Esters: Isolation, Structural Analysis, Conformational Study, and Anti-CHIKV Activity.

Esposito M, Nothias LF, Nedev H, Gallard JF, Leyssen P, Retailleau P, Costa J, Roussi F, Iorga BI, Paolini J, Litaudon M.

J Nat Prod. 2016 Nov 23;79(11):2873-2882. Epub 2016 Oct 27.


Comparative analysis of the anti-chikungunya virus activity of novel bryostatin analogs confirms the existence of a PKC-independent mechanism.

Abdelnabi R, Staveness D, Near KE, Wender PA, Delang L, Neyts J, Leyssen P.

Biochem Pharmacol. 2016 Nov 15;120:15-21. doi: 10.1016/j.bcp.2016.09.020. Epub 2016 Sep 21.


The viral capping enzyme nsP1: a novel target for the inhibition of chikungunya virus infection.

Delang L, Li C, Tas A, Quérat G, Albulescu IC, De Burghgraeve T, Guerrero NA, Gigante A, Piorkowski G, Decroly E, Jochmans D, Canard B, Snijder EJ, Pérez-Pérez MJ, van Hemert MJ, Coutard B, Leyssen P, Neyts J.

Sci Rep. 2016 Aug 22;6:31819. doi: 10.1038/srep31819.


Computer-aided identification, synthesis and evaluation of substituted thienopyrimidines as novel inhibitors of HCV replication.

Bassetto M, Leyssen P, Neyts J, Yerukhimovich MM, Frick DN, Brancale A.

Eur J Med Chem. 2016 Nov 10;123:31-47. doi: 10.1016/j.ejmech.2016.07.035. Epub 2016 Jul 19.


Optimization of a Class of Tryptophan Dendrimers That Inhibit HIV Replication Leads to a Selective, Specific, and Low-Nanomolar Inhibitor of Clinical Isolates of Enterovirus A71.

Rivero-Buceta E, Sun L, Martínez-Gualda B, Doyagüez EG, Donckers K, Quesada E, Camarasa MJ, Delang L, San-Félix A, Neyts J, Leyssen P.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):5064-7. doi: 10.1128/AAC.00626-16. Print 2016 Aug.


VP1 crystal structure-guided exploration and optimization of 4,5-dimethoxybenzene-based inhibitors of rhinovirus 14 infection.

Da Costa L, Roche M, Scheers E, Coluccia A, Neyts J, Terme T, Leyssen P, Silvestri R, Vanelle P.

Eur J Med Chem. 2016 Jun 10;115:453-62. doi: 10.1016/j.ejmech.2016.03.049. Epub 2016 Mar 19.


Identification and Analysis of Antiviral Compounds Against Poliovirus.

Leyssen P, Franco D, Tijsma A, Lacroix C, De Palma A, Neyts J.

Methods Mol Biol. 2016;1387:325-38. doi: 10.1007/978-1-4939-3292-4_17.


3-(imidazo[1,2-a:5,4-b']dipyridin-2-yl)aniline inhibits pestivirus replication by targeting a hot spot drug binding pocket in the RNA-dependent RNA polymerase.

Musiu S, Leyssen P, Froeyen M, Chezal JM, Neyts J, Paeshuyse J.

Antiviral Res. 2016 May;129:99-103. doi: 10.1016/j.antiviral.2016.03.007. Epub 2016 Mar 9.


Synthesis and Structure-Activity Relationships of Imidazole-Coumarin Conjugates against Hepatitis C Virus.

Tsay SC, Lin SY, Huang WC, Hsu MH, Hwang KC, Lin CC, Horng JC, Chen IC, Hwu JR, Shieh FK, Leyssen P, Neyts J.

Molecules. 2016 Feb 18;21(2). pii: E228. doi: 10.3390/molecules21020228.


Inhibition of Chikungunya Virus-Induced Cell Death by Salicylate-Derived Bryostatin Analogues Provides Additional Evidence for a PKC-Independent Pathway.

Staveness D, Abdelnabi R, Near KE, Nakagawa Y, Neyts J, Delang L, Leyssen P, Wender PA.

J Nat Prod. 2016 Apr 22;79(4):680-4. doi: 10.1021/acs.jnatprod.5b01017. Epub 2016 Feb 22.


Simplified Bryostatin Analogues Protect Cells from Chikungunya Virus-Induced Cell Death.

Staveness D, Abdelnabi R, Schrier AJ, Loy BA, Verma VA, DeChristopher BA, Near KE, Neyts J, Delang L, Leyssen P, Wender PA.

J Nat Prod. 2016 Apr 22;79(4):675-9. doi: 10.1021/acs.jnatprod.5b01016. Epub 2016 Feb 22.


Modification of the length and structure of the linker of N(6)-benzyladenosine modulates its selective antiviral activity against enterovirus 71.

Drenichev MS, Oslovsky VE, Sun L, Tijsma A, Kurochkin NN, Tararov VI, Chizhov AO, Neyts J, Pannecouque C, Leyssen P, Mikhailov SN.

Eur J Med Chem. 2016 Mar 23;111:84-94. doi: 10.1016/j.ejmech.2016.01.036. Epub 2016 Jan 26.


Exploring the importance of zinc binding and steric/hydrophobic factors in novel HCV replication inhibitors.

Talley DC, Delang L, Neyts J, Leyssen P, Smith PJ.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1196-9. doi: 10.1016/j.bmcl.2016.01.035. Epub 2016 Jan 16.


Structure Elucidation of Coxsackievirus A16 in Complex with GPP3 Informs a Systematic Review of Highly Potent Capsid Binders to Enteroviruses.

De Colibus L, Wang X, Tijsma A, Neyts J, Spyrou JA, Ren J, Grimes JM, Puerstinger G, Leyssen P, Fry EE, Rao Z, Stuart DI.

PLoS Pathog. 2015 Oct 20;11(10):e1005165. doi: 10.1371/journal.ppat.1005165. eCollection 2015 Oct.


Antiviral Activity of Broad-Spectrum and Enterovirus-Specific Inhibitors against Clinical Isolates of Enterovirus D68.

Sun L, Meijer A, Froeyen M, Zhang L, Thibaut HJ, Baggen J, George S, Vernachio J, van Kuppeveld FJ, Leyssen P, Hilgenfeld R, Neyts J, Delang L.

Antimicrob Agents Chemother. 2015 Dec;59(12):7782-5. doi: 10.1128/AAC.01375-15. Epub 2015 Sep 14.


NMR-based conformational analysis of 2',6-disubstituted uridines and antiviral evaluation of new phosphoramidate prodrugs.

da Paixão Soares F, Groaz E, Lescrinier E, Neyts J, Leyssen P, Herdewijn P.

Bioorg Med Chem. 2015 Sep 1;23(17):5809-15. doi: 10.1016/j.bmc.2015.07.003. Epub 2015 Jul 10.


In vitro characterisation of a pleconaril/pirodavir-like compound with potent activity against rhinoviruses.

Lacroix C, Laconi S, Angius F, Coluccia A, Silvestri R, Pompei R, Neyts J, Leyssen P.

Virol J. 2015 Jul 14;12:106. doi: 10.1186/s12985-015-0330-4.


LC-MS²-Based dereplication of Euphorbia extracts with anti-Chikungunya virus activity.

Nothias-Scaglia LF, Dumontet V, Neyts J, Roussi F, Costa J, Leyssen P, Litaudon M, Paolini J.

Fitoterapia. 2015 Sep;105:202-9. doi: 10.1016/j.fitote.2015.06.021. Epub 2015 Jul 4.


Exploration of the anti-enterovirus activity of a series of pleconaril/pirodavir-like compounds.

Bernard A, Lacroix C, Cabiddu MG, Neyts J, Leyssen P, Pompei R.

Antivir Chem Chemother. 2015 Apr;24(2):56-61. doi: 10.1177/2040206615589035. Epub 2015 Jun 11.


The enterovirus 3C protease inhibitor SG85 efficiently blocks rhinovirus replication and is not cross-resistant with rupintrivir.

Lacroix C, George S, Leyssen P, Hilgenfeld R, Neyts J.

Antimicrob Agents Chemother. 2015 Sep;59(9):5814-8. doi: 10.1128/AAC.00534-15. Epub 2015 Jun 8.


Discovery of Multitarget Antivirals Acting on Both the Dengue Virus NS5-NS3 Interaction and the Host Src/Fyn Kinases.

Vincetti P, Caporuscio F, Kaptein S, Gioiello A, Mancino V, Suzuki Y, Yamamoto N, Crespan E, Lossani A, Maga G, Rastelli G, Castagnolo D, Neyts J, Leyssen P, Costantino G, Radi M.

J Med Chem. 2015 Jun 25;58(12):4964-75. doi: 10.1021/acs.jmedchem.5b00108. Epub 2015 Jun 15.


Antiviral Activity of Diterpene Esters on Chikungunya Virus and HIV Replication.

Nothias-Scaglia LF, Pannecouque C, Renucci F, Delang L, Neyts J, Roussi F, Costa J, Leyssen P, Litaudon M, Paolini J.

J Nat Prod. 2015 Jun 26;78(6):1277-83. doi: 10.1021/acs.jnatprod.5b00073. Epub 2015 May 13.


Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata.

Olivon F, Palenzuela H, Girard-Valenciennes E, Neyts J, Pannecouque C, Roussi F, Grondin I, Leyssen P, Litaudon M.

J Nat Prod. 2015 May 22;78(5):1119-28. doi: 10.1021/acs.jnatprod.5b00116. Epub 2015 May 6.


Benzouracil-coumarin-arene conjugates as inhibiting agents for chikungunya virus.

Hwu JR, Kapoor M, Tsay SC, Lin CC, Hwang KC, Horng JC, Chen IC, Shieh FK, Leyssen P, Neyts J.

Antiviral Res. 2015 Jun;118:103-9. doi: 10.1016/j.antiviral.2015.03.013. Epub 2015 Apr 1.


The RNA template channel of the RNA-dependent RNA polymerase as a target for development of antiviral therapy of multiple genera within a virus family.

van der Linden L, Vives-Adrián L, Selisko B, Ferrer-Orta C, Liu X, Lanke K, Ulferts R, De Palma AM, Tanchis F, Goris N, Lefebvre D, De Clercq K, Leyssen P, Lacroix C, Pürstinger G, Coutard B, Canard B, Boehr DD, Arnold JJ, Cameron CE, Verdaguer N, Neyts J, van Kuppeveld FJ.

PLoS Pathog. 2015 Mar 23;11(3):e1004733. doi: 10.1371/journal.ppat.1004733. eCollection 2015 Mar.


Design, synthesis, optimization and antiviral activity of a class of hybrid dengue virus E protein inhibitors.

Jadav SS, Kaptein S, Timiri A, De Burghgraeve T, Badavath VN, Ganesan R, Sinha BN, Neyts J, Leyssen P, Jayaprakash V.

Bioorg Med Chem Lett. 2015 Apr 15;25(8):1747-1752. doi: 10.1016/j.bmcl.2015.02.059. Epub 2015 Mar 2.


Itraconazole inhibits enterovirus replication by targeting the oxysterol-binding protein.

Strating JR, van der Linden L, Albulescu L, Bigay J, Arita M, Delang L, Leyssen P, van der Schaar HM, Lanke KH, Thibaut HJ, Ulferts R, Drin G, Schlinck N, Wubbolts RW, Sever N, Head SA, Liu JO, Beachy PA, De Matteis MA, Shair MD, Olkkonen VM, Neyts J, van Kuppeveld FJ.

Cell Rep. 2015 Feb 3;10(4):600-15. doi: 10.1016/j.celrep.2014.12.054. Epub 2015 Jan 29.


Bioengineering and semisynthesis of an optimized cyclophilin inhibitor for treatment of chronic viral infection.

Hansson MJ, Moss SJ, Bobardt M, Chatterji U, Coates N, Garcia-Rivera JA, Elmér E, Kendrew S, Leyssen P, Neyts J, Nur-E-Alam M, Warneck T, Wilkinson B, Gallay P, Gregory MA.

Chem Biol. 2015 Feb 19;22(2):285-92. doi: 10.1016/j.chembiol.2014.10.023. Epub 2015 Jan 22.

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