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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.
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
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 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 TH, Tahri A, Vijgen L, Berke JM, Lachau-Durand S, Stoops B, Snoeys J, Leclercq L, Tambuyzer L, Lin TI, Simmen K, Raboisson P. Jonckers TH, et al. J Med Chem. 2016 Jun 23;59(12):5790-8. doi: 10.1021/acs.jmedchem.6b00382. Epub 2016 Jun 3. J Med Chem. 2016. PMID: 27181575
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.
McGowan DC, Herschke F, Pauwels F, Stoops B, Smyej I, Last S, Pieters S, Embrechts W, Khamlichi MD, Thoné T, Van Schoubroeck B, Mostmans W, Wuyts D, Verstappen D, Scholliers A, De Pooter D, Dhuyvetter D, Borghys H, Tuefferd M, Arnoult E, Hong J, Fanning G, Bollekens J, Urmaliya V, Teisman A, Horton H, Jonckers THM, Raboisson P. McGowan DC, et al. Among authors: jonckers thm. J Med Chem. 2017 Jul 27;60(14):6137-6151. doi: 10.1021/acs.jmedchem.7b00365. Epub 2017 Jul 14. J Med Chem. 2017. PMID: 28671847
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
31 results