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Open science discovery of potent noncovalent SARS-CoV-2 main protease inhibitors.
Boby ML, Fearon D, Ferla M, Filep M, Koekemoer L, Robinson MC; COVID Moonshot Consortium‡; Chodera JD, Lee AA, London N, von Delft A, von Delft F, Achdout H, Aimon A, Alonzi DS, Arbon R, Aschenbrenner JC, Balcomb BH, Bar-David E, Barr H, Ben-Shmuel A, Bennett J, Bilenko VA, Borden B, Boulet P, Bowman GR, Brewitz L, Brun J, Bvnbs S, Calmiano M, Carbery A, Carney DW, Cattermole E, Chang E, Chernyshenko E, Clyde A, Coffland JE, Cohen G, Cole JC, Contini A, Cox L, Croll TI, Cvitkovic M, De Jonghe S, Dias A, Donckers K, Dotson DL, Douangamath A, Duberstein S, Dudgeon T, Dunnett LE, Eastman P, Erez N, Eyermann CJ, Fairhead M, Fate G, Fedorov O, Fernandes RS, Ferrins L, Foster R, Foster H, Fraisse L, Gabizon R, García-Sastre A, Gawriljuk VO, Gehrtz P, Gileadi C, Giroud C, Glass WG, Glen RC, Glinert I, Godoy AS, Gorichko M, Gorrie-Stone T, Griffen EJ, Haneef A, Hassell Hart S, Heer J, Henry M, Hill M, Horrell S, Huang QYJ, Huliak VD, Hurley MFD, Israely T, Jajack A, Jansen J, Jnoff E, Jochmans D, John T, Kaminow B, Kang L, Kantsadi AL, Kenny PW, Kiappes JL, Kinakh SO, Kovar B, Krojer T, La VNT, Laghnimi-Hahn S, Lefker BA, Levy H, Lithgo RM, Logvinenko IG, Lukacik P, Macdonald HB, M… See abstract for full author list ➔ Boby ML, et al. Among authors: donckers k. Science. 2023 Nov 10;382(6671):eabo7201. doi: 10.1126/science.abo7201. Epub 2023 Nov 10. Science. 2023. PMID: 37943932 Free PMC article.
The Substitutions L50F, E166A, and L167F in SARS-CoV-2 3CLpro Are Selected by a Protease Inhibitor In Vitro and Confer Resistance To Nirmatrelvir.
Jochmans D, Liu C, Donckers K, Stoycheva A, Boland S, Stevens SK, De Vita C, Vanmechelen B, Maes P, Trüeb B, Ebert N, Thiel V, De Jonghe S, Vangeel L, Bardiot D, Jekle A, Blatt LM, Beigelman L, Symons JA, Raboisson P, Chaltin P, Marchand A, Neyts J, Deval J, Vandyck K. Jochmans D, et al. Among authors: donckers k. mBio. 2023 Feb 28;14(1):e0281522. doi: 10.1128/mbio.02815-22. Epub 2023 Jan 10. mBio. 2023. PMID: 36625640 Free PMC article.
SARS-CoV-2 infects the human kidney and drives fibrosis in kidney organoids.
Jansen J, Reimer KC, Nagai JS, Varghese FS, Overheul GJ, de Beer M, Roverts R, Daviran D, Fermin LAS, Willemsen B, Beukenboom M, Djudjaj S, von Stillfried S, van Eijk LE, Mastik M, Bulthuis M, Dunnen WD, van Goor H, Hillebrands JL, Triana SH, Alexandrov T, Timm MC, van den Berge BT, van den Broek M, Nlandu Q, Heijnert J, Bindels EMJ, Hoogenboezem RM, Mooren F, Kuppe C, Miesen P, Grünberg K, Ijzermans T, Steenbergen EJ, Czogalla J, Schreuder MF, Sommerdijk N, Akiva A, Boor P, Puelles VG, Floege J, Huber TB; COVID Moonshot consortium; van Rij RP, Costa IG, Schneider RK, Smeets B, Kramann R. Jansen J, et al. Cell Stem Cell. 2022 Feb 3;29(2):217-231.e8. doi: 10.1016/j.stem.2021.12.010. Epub 2021 Dec 25. Cell Stem Cell. 2022. PMID: 35032430 Free PMC article.
Novel Class of Chikungunya Virus Small Molecule Inhibitors That Targets the Viral Capping Machinery.
Abdelnabi R, Kovacikova K, Moesslacher J, Donckers K, Battisti V, Leyssen P, Langer T, Puerstinger G, Quérat G, Li C, Decroly E, Tas A, Marchand A, Chaltin P, Coutard B, van Hemert M, Neyts J, Delang L. Abdelnabi R, et al. Among authors: donckers k. Antimicrob Agents Chemother. 2020 Jun 23;64(7):e00649-20. doi: 10.1128/AAC.00649-20. Print 2020 Jun 23. Antimicrob Agents Chemother. 2020. PMID: 32340991 Free PMC article.
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. Rivero-Buceta E, et al. Among authors: donckers k. Antimicrob Agents Chemother. 2016 Jul 22;60(8):5064-7. doi: 10.1128/AAC.00626-16. Print 2016 Aug. Antimicrob Agents Chemother. 2016. PMID: 27246775 Free PMC article.