A pan-serotype dengue virus inhibitor targeting the NS3–NS4B interaction
Kaptein, Suzanne J. F., Goethals, Olivia, Kiemel, Dominik, Marchand, Arnaud, Kesteleyn, Bart, Bonfanti, Jean-François, Bardiot, Dorothée, Stoops, Bart, Jonckers, Tim H. M., Dallmeier, Kai, Geluykens, Peggy, Thys, Kim, Crabbe, Marjolein, Chatel-Chaix, Laurent, Münster, Max, Querat, Gilles, Touret, Franck, de Lamballerie, Xavier, Raboisson, Pierre, Simmen, Kenny, Chaltin, Patrick, Bartenschlager, Ralf, Van Loock, Marnix, Neyts, Johan
Published in Nature (London) (21.10.2021)
Published in Nature (London) (21.10.2021)
Get full text
Journal Article
Discovery of 3‑({5-Chloro-1-[3-(methylsulfonyl)propyl]‑1H‑indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro‑2H‑imidazo[4,5‑c]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus
Vendeville, Sandrine, Tahri, Abdellah, Hu, Lili, Demin, Samuel, Cooymans, Ludwig, Vos, Ann, Kwanten, Leen, Van den Berg, Joke, Battles, Michael B, McLellan, Jason S, Koul, Anil, Raboisson, Pierre, Roymans, Dirk, Jonckers, Tim H. M
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
Get full text
Journal Article
Molecular mechanism of respiratory syncytial virus fusion inhibitors
Battles, Michael B, Langedijk, Johannes P, Furmanova-Hollenstein, Polina, Chaiwatpongsakorn, Supranee, Costello, Heather M, Kwanten, Leen, Vranckx, Luc, Vink, Paul, Jaensch, Steffen, Jonckers, Tim H M, Koul, Anil, Arnoult, Eric, Peeples, Mark E, Roymans, Dirk, McLellan, Jason S
Published in Nature chemical biology (01.02.2016)
Published in Nature chemical biology (01.02.2016)
Get full text
Journal Article
A small-molecule fusion inhibitor of influenza virus is orally active in mice
van Dongen, Maria J P, Kadam, Rameshwar U, Juraszek, Jarek, Lawson, Edward, Brandenburg, Boerries, Schmitz, Frederike, Schepens, Wim B G, Stoops, Bart, van Diepen, Harry A, Jongeneelen, Mandy, Tang, Chan, Vermond, Jan, van Eijgen-Obregoso Real, Alida, Blokland, Sven, Garg, Divita, Yu, Wenli, Goutier, Wouter, Lanckacker, Ellen, Klap, Jaco M, Peeters, Daniëlle C G, Wu, Jin, Buyck, Christophe, Jonckers, Tim H M, Roymans, Dirk, Roevens, Peter, Vogels, Ronald, Koudstaal, Wouter, Friesen, Robert H E, Raboisson, Pierre, Dhanak, Dashyant, Goudsmit, Jaap, Wilson, Ian A
Published in Science (American Association for the Advancement of Science) (08.03.2019)
Published in Science (American Association for the Advancement of Science) (08.03.2019)
Get full text
Journal Article
Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region
McGowan, David C, Balemans, Wendy, Embrechts, Werner, Motte, Magali, Keown, Jeremy R, Buyck, Christophe, Corbera, Jordi, Funes, Mario, Moreno, Laura, Cooymans, Ludwig, Tahri, Abdellah, Eymard, Julien, Stoops, Bart, Strijbos, Rudy, Van den Berg, Joke, Fodor, Ervin, Grimes, Jonathan M, Koul, Anil, Jonckers, Tim H. M, Raboisson, Pierre, Guillemont, Jérôme
Published in Journal of medicinal chemistry (14.11.2019)
Published in Journal of medicinal chemistry (14.11.2019)
Get full text
Journal Article
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus
Embrechts, Werner, Herschke, Florence, Pauwels, Frederik, Stoops, Bart, Last, Stefaan, Pieters, Serge, Pande, Vineet, Pille, Geert, Amssoms, Katie, Smyej, Ilham, Dhuyvetter, Deborah, Scholliers, Annick, Mostmans, Wendy, Van Dijck, Kris, Van Schoubroeck, Bertrand, Thone, Tine, De Pooter, Dorien, Fanning, Gregory, Jonckers, Tim H. M, Horton, Helen, Raboisson, Pierre, McGowan, David
Published in Journal of medicinal chemistry (26.07.2018)
Published in Journal of medicinal chemistry (26.07.2018)
Get full text
Journal Article
Discovery of JNJ-1802, a First-in-Class Pan-Serotype Dengue Virus NS4B Inhibitor
Kesteleyn, Bart, Bonfanti, Jean-François, Bardiot, Dorothée, De Boeck, Benoît, Goethals, Olivia, Kaptein, Suzanne J. F., Stoops, Bart, Coesemans, Erwin, Fortin, Jérôme, Muller, Philippe, Doublet, Frédéric, Carlens, Gunter, Koukni, Mohamed, Smets, Wim, Raboisson, Pierre, Chaltin, Patrick, Simmen, Kenny, Loock, Marnix Van, Neyts, Johan, Marchand, Arnaud, Jonckers, Tim H. M.
Published in Journal of medicinal chemistry (14.03.2024)
Published in Journal of medicinal chemistry (14.03.2024)
Get full text
Journal Article
Blocking NS3–NS4B interaction inhibits dengue virus in non-human primates
Goethals, Olivia, Kaptein, Suzanne J. F., Kesteleyn, Bart, Bonfanti, Jean-François, Van Wesenbeeck, Liesbeth, Bardiot, Dorothée, Verschoor, Ernst J., Verstrepen, Babs E., Fagrouch, Zahra, Putnak, J. Robert, Kiemel, Dominik, Ackaert, Oliver, Straetemans, Roel, Lachau-Durand, Sophie, Geluykens, Peggy, Crabbe, Marjolein, Thys, Kim, Stoops, Bart, Lenz, Oliver, Tambuyzer, Lotke, De Meyer, Sandra, Dallmeier, Kai, McCracken, Michael K., Gromowski, Gregory D., Rutvisuttinunt, Wiriya, Jarman, Richard G., Karasavvas, Nicos, Touret, Franck, Querat, Gilles, de Lamballerie, Xavier, Chatel-Chaix, Laurent, Milligan, Gregg N., Beasley, David W. C., Bourne, Nigel, Barrett, Alan D. T., Marchand, Arnaud, Jonckers, Tim H. M., Raboisson, Pierre, Simmen, Kenny, Chaltin, Patrick, Bartenschlager, Ralf, Bogers, Willy M., Neyts, Johan, Van Loock, Marnix
Published in Nature (London) (23.03.2023)
Published in Nature (London) (23.03.2023)
Get full text
Journal Article
Structural and mechanistic insights into the inhibition of respiratory syncytial virus polymerase by a non-nucleoside inhibitor
Yu, Xiaodi, Abeywickrema, Pravien, Bonneux, Brecht, Behera, Ishani, Anson, Brandon, Jacoby, Edgar, Fung, Amy, Adhikary, Suraj, Bhaumik, Anusarka, Carbajo, Rodrigo J., De Bruyn, Suzanne, Miller, Robyn, Patrick, Aaron, Pham, Quyen, Piassek, Madison, Verheyen, Nick, Shareef, Afzaal, Sutto-Ortiz, Priscila, Ysebaert, Nina, Van Vlijmen, Herman, Jonckers, Tim H. M., Herschke, Florence, McLellan, Jason S., Decroly, Etienne, Fearns, Rachel, Grosse, Sandrine, Roymans, Dirk, Sharma, Sujata, Rigaux, Peter, Jin, Zhinan
Published in Communications biology (21.10.2023)
Published in Communications biology (21.10.2023)
Get full text
Journal Article
Discovery of 1‑((2R,4aR,6R,7R,7aR)‑2-Isopropoxy-2-oxidodihydro‑4H,6H‑spiro[furo[3,2‑d][1,3,2]dioxaphosphinine-7,2′-oxetan]-6-yl)pyrimidine-2,4(1H,3H)‑dione (JNJ-54257099), a 3′-5′-Cyclic Phosphate Ester Prodrug of 2′-Deoxy-2′-Spirooxetane Uridine Triphosphate Useful for HCV Inhibition
Jonckers, Tim H. M, Tahri, Abdellah, Vijgen, Leen, Berke, Jan Martin, Lachau-Durand, Sophie, Stoops, Bart, Snoeys, Jan, Leclercq, Laurent, Tambuyzer, Lotke, Lin, Tse-I, Simmen, Kenny, Raboisson, Pierre
Published in Journal of medicinal chemistry (23.06.2016)
Published in Journal of medicinal chemistry (23.06.2016)
Get full text
Journal Article
Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors
Jonckers, Tim H.M., Rouan, Marie-Claude, Haché, Geerwin, Schepens, Wim, Hallenberger, Sabine, Baumeister, Judith, Sasaki, Jennifer C.
Published in Bioorganic & medicinal chemistry letters (01.08.2012)
Published in Bioorganic & medicinal chemistry letters (01.08.2012)
Get full text
Journal Article
Discovery of Acyl-Indole Derivatives as Pan-Serotype Dengue Virus NS4B Inhibitors
Kesteleyn, Bart, Bardiot, Dorothée, Bonfanti, Jean-François, De Boeck, Benoît, Goethals, Olivia, Kaptein, Suzanne J. F., Stoops, Bart, Coesemans, Erwin, Fortin, Jérôme, Muller, Philippe, Doublet, Frédéric, Carlens, Gunter, Koukni, Mohamed, Smets, Wim, Raboisson, Pierre, Chaltin, Patrick, Simmen, Kenny, Van Loock, Marnix, Neyts, Johan, Marchand, Arnaud, Jonckers, Tim H. M.
Published in Journal of medicinal chemistry (13.07.2023)
Published in Journal of medicinal chemistry (13.07.2023)
Get full text
Journal Article
Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1 H -indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2 H -imidazo[4,5- c ]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus
Vendeville, Sandrine, Tahri, Abdellah, Hu, Lili, Demin, Samuel, Cooymans, Ludwig, Vos, Ann, Kwanten, Leen, Van den Berg, Joke, Battles, Michael B., McLellan, Jason S., Koul, Anil, Raboisson, Pierre, Roymans, Dirk, Jonckers, Tim H. M.
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
Get full text
Journal Article
Identification and Optimization of Pyrrolo[3,2‑d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B
McGowan, David C, Herschke, Florence, Pauwels, Frederik, Stoops, Bart, Smyej, Ilham, Last, Stefaan, Pieters, Serge, Embrechts, Werner, Khamlichi, Mourad Daoubi, Thoné, Tine, Van Schoubroeck, Bertrand, Mostmans, Wendy, Wuyts, Debbie, Verstappen, Dorien, Scholliers, Annick, De Pooter, Dorien, Dhuyvetter, Deborah, Borghys, Herman, Tuefferd, Marianne, Arnoult, Eric, Hong, Jin, Fanning, Gregory, Bollekens, Jacques, Urmaliya, Vijay, Teisman, Ard, Horton, Helen, Jonckers, Tim H. M, Raboisson, Pierre
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
Get full text
Journal Article
Discovery of gem-Dimethyl-hydroxymethylpyridine Derivatives as Potent Non-nucleoside RSV Polymerase Inhibitors
Grosse, Sandrine, Cooymans, Ludwig, Embrechts, Werner, McGowan, David, Jacoby, Edgar, Stoops, Bart, Gupta, Kusum, Ackermann, Mark, Alnajjar, Sarhad, Guillemont, Jerome, Jin, Zhinan, Kesteleyn, Bart, Matcha, Kiran, Sriboonyapirat, Pun, Truong, Anh, Van Den Berg, Joke, Yu, Xiaodi, Herschke, Florence, Roymans, Dirk, Raboisson, Pierre, Rigaux, Peter, Jonckers, Tim H. M.
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
Get full text
Journal Article
Discovery and Selection of TMC114, a Next Generation HIV-1 Protease Inhibitor
Surleraux, Dominique L. N. G, Tahri, Abdellah, Verschueren, Wim G, Pille, Geert M. E, de Kock, Herman A, Jonckers, Tim H. M, Peeters, Anik, De Meyer, Sandra, Azijn, Hilde, Pauwels, Rudi, de Bethune, Marie-Pierre, King, Nancy M, Prabu-Jeyabalan, Moses, Schiffer, Celia A, Wigerinck, Piet B. T. P
Published in Journal of medicinal chemistry (24.03.2005)
Published in Journal of medicinal chemistry (24.03.2005)
Get full text
Journal Article
Spiro-Azetidine Oxindoles as Long-Acting Injectables for Pre-Exposure Prophylaxis against Respiratory Syncytial Virus Infections
Kesteleyn, Bart, Herschke, Florence, Darville, Nicolas, Stoops, Bart, Jacobs, Tom, Jacoby, Edgar, Shaffer, Paul, Lammens, Lieve, Van Rompaey, Dries, Matcha, Kiran, Martinez Lamenca, Carolina, Coesemans, Erwin, Hache, Geerwin, Pieters, Serge, Lecomte, Morgan, Hu, Lili, Demin, Samuel, Milligan, Cynthia, Abeywickrema, Pravien, De Bruyn, Suzanne, Van Den Berg, Joke, Ysebaert, Nina, De Zwart, Loeckie, Nájera, Isabel, Rigaux, Peter, Roymans, Dirk, Jonckers, Tim H. M.
Published in Journal of medicinal chemistry (11.07.2024)
Published in Journal of medicinal chemistry (11.07.2024)
Get full text
Journal Article
Nucleotide Prodrugs of 2′-Deoxy-2′-spirooxetane Ribonucleosides as Novel Inhibitors of the HCV NS5B Polymerase
Jonckers, Tim H. M., Vandyck, Koen, Vandekerckhove, Leen, Hu, Lili, Tahri, Abdellah, Van Hoof, Steven, Lin, Tse-I, Vijgen, Leen, Berke, Jan Martin, Lachau-Durand, Sophie, Stoops, Bart, Leclercq, Laurent, Fanning, Gregory, Samuelsson, Bertil, Nilsson, Magnus, Rosenquist, Åsa, Simmen, Kenny, Raboisson, Pierre
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
Get full text
Journal Article
From Oxetane to Thietane: Extending the Antiviral Spectrum of 2′-Spirocyclic Uridines by Substituting Oxygen with Sulfur
Grosse, Sandrine, Tahri, Abdellah, Raboisson, Pierre, Houpis, Yannis, Stoops, Bart, Jacoby, Edgar, Neefs, Jean-Marc, Van Loock, Marnix, Goethals, Olivia, Geluykens, Peggy, Bonfanti, Jean-François, Jonckers, Tim H. M.
Published in ACS medicinal chemistry letters (08.12.2022)
Published in ACS medicinal chemistry letters (08.12.2022)
Get full text
Journal Article