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Page 1
Structural and mechanistic insights into the inhibition of respiratory syncytial virus polymerase by a non-nucleoside inhibitor.
Yu X, Abeywickrema P, Bonneux B, Behera I, Anson B, Jacoby E, Fung A, Adhikary S, Bhaumik A, Carbajo RJ, De Bruyn S, Miller R, Patrick A, Pham Q, Piassek M, Verheyen N, Shareef A, Sutto-Ortiz P, Ysebaert N, Van Vlijmen H, Jonckers THM, Herschke F, McLellan JS, Decroly E, Fearns R, Grosse S, Roymans D, Sharma S, Rigaux P, Jin Z. Yu X, et al. Among authors: jonckers thm. Commun Biol. 2023 Oct 21;6(1):1074. doi: 10.1038/s42003-023-05451-4. Commun Biol. 2023. PMID: 37865687 Free PMC article.
Molecular mechanism of respiratory syncytial virus fusion inhibitors.
Battles MB, Langedijk JP, Furmanova-Hollenstein P, Chaiwatpongsakorn S, Costello HM, Kwanten L, Vranckx L, Vink P, Jaensch S, Jonckers TH, Koul A, Arnoult E, Peeples ME, Roymans D, McLellan JS. Battles MB, et al. Nat Chem Biol. 2016 Feb;12(2):87-93. doi: 10.1038/nchembio.1982. Epub 2015 Dec 7. Nat Chem Biol. 2016. PMID: 26641933 Free PMC 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 S, Tahri A, Hu L, Demin S, Cooymans L, Vos A, Kwanten L, Van den Berg J, Battles MB, McLellan JS, Koul A, Raboisson P, Roymans D, Jonckers THM. Vendeville S, et al. Among authors: jonckers thm. J Med Chem. 2020 Aug 13;63(15):8046-8058. doi: 10.1021/acs.jmedchem.0c00226. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32407115
From Oxetane to Thietane: Extending the Antiviral Spectrum of 2'-Spirocyclic Uridines by Substituting Oxygen with Sulfur.
Grosse S, Tahri A, Raboisson P, Houpis Y, Stoops B, Jacoby E, Neefs JM, Van Loock M, Goethals O, Geluykens P, Bonfanti JF, Jonckers THM. Grosse S, et al. Among authors: jonckers thm. ACS Med Chem Lett. 2022 Nov 28;13(12):1879-1884. doi: 10.1021/acsmedchemlett.2c00372. eCollection 2022 Dec 8. ACS Med Chem Lett. 2022. PMID: 36518706 Free PMC article.
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists.
Pieters S, McGowan D, Herschke F, Pauwels F, Stoops B, Last S, Embrechts W, Scholliers A, Mostmans W, Van Dijck K, Van Schoubroeck B, Thoné T, De Pooter D, Fanning G, Rosauro ML, Khamlichi MD, Houpis I, Arnoult E, Jonckers THM, Raboisson P. Pieters S, et al. Among authors: jonckers thm. Bioorg Med Chem Lett. 2018 Feb 15;28(4):711-719. doi: 10.1016/j.bmcl.2018.01.014. Epub 2018 Jan 16. Bioorg Med Chem Lett. 2018. PMID: 29366653
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.
Embrechts W, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Pande V, Pille G, Amssoms K, Smyej I, Dhuyvetter D, Scholliers A, Mostmans W, Van Dijck K, Van Schoubroeck B, Thone T, De Pooter D, Fanning G, Jonckers THM, Horton H, Raboisson P, McGowan D. Embrechts W, et al. Among authors: jonckers thm. J Med Chem. 2018 Jul 26;61(14):6236-6246. doi: 10.1021/acs.jmedchem.8b00643. Epub 2018 Jul 17. J Med Chem. 2018. PMID: 29965759
Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists.
McGowan DC, Herschke F, Khamlichi MD, Rosauro ML, Benedicto SMP, Pauwels F, Stoops B, Pande V, Scholliers A, Van Schoubroeck B, Mostmans W, Van Dijck K, Thoné T, Horton H, Fanning G, Jonckers THM, Raboisson P. McGowan DC, et al. Among authors: jonckers thm. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3216-3221. doi: 10.1016/j.bmcl.2018.08.015. Epub 2018 Aug 16. Bioorg Med Chem Lett. 2018. PMID: 30143425
A small-molecule fusion inhibitor of influenza virus is orally active in mice.
van Dongen MJP, Kadam RU, Juraszek J, Lawson E, Brandenburg B, Schmitz F, Schepens WBG, Stoops B, van Diepen HA, Jongeneelen M, Tang C, Vermond J, van Eijgen-Obregoso Real A, Blokland S, Garg D, Yu W, Goutier W, Lanckacker E, Klap JM, Peeters DCG, Wu J, Buyck C, Jonckers THM, Roymans D, Roevens P, Vogels R, Koudstaal W, Friesen RHE, Raboisson P, Dhanak D, Goudsmit J, Wilson IA. van Dongen MJP, et al. Among authors: jonckers thm. Science. 2019 Mar 8;363(6431):eaar6221. doi: 10.1126/science.aar6221. Science. 2019. PMID: 30846569 Free PMC article.
Blocking NS3-NS4B interaction inhibits dengue virus in non-human primates.
Goethals O, Kaptein SJF, Kesteleyn B, Bonfanti JF, Van Wesenbeeck L, Bardiot D, Verschoor EJ, Verstrepen BE, Fagrouch Z, Putnak JR, Kiemel D, Ackaert O, Straetemans R, Lachau-Durand S, Geluykens P, Crabbe M, Thys K, Stoops B, Lenz O, Tambuyzer L, De Meyer S, Dallmeier K, McCracken MK, Gromowski GD, Rutvisuttinunt W, Jarman RG, Karasavvas N, Touret F, Querat G, de Lamballerie X, Chatel-Chaix L, Milligan GN, Beasley DWC, Bourne N, Barrett ADT, Marchand A, Jonckers THM, Raboisson P, Simmen K, Chaltin P, Bartenschlager R, Bogers WM, Neyts J, Van Loock M. Goethals O, et al. Among authors: jonckers thm. Nature. 2023 Mar;615(7953):678-686. doi: 10.1038/s41586-023-05790-6. Epub 2023 Mar 15. Nature. 2023. PMID: 36922586 Free PMC article.
2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase.
Jonckers TH, Lin TI, Buyck C, Lachau-Durand S, Vandyck K, Van Hoof S, Vandekerckhove LA, Hu L, Berke JM, Vijgen L, Dillen LL, Cummings MD, de Kock H, Nilsson M, Sund C, Rydegård C, Samuelsson B, Rosenquist A, Fanning G, Van Emelen K, Simmen K, Raboisson P. Jonckers TH, et al. J Med Chem. 2010 Nov 25;53(22):8150-60. doi: 10.1021/jm101050a. Epub 2010 Oct 29. J Med Chem. 2010. PMID: 21033671
29 results