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Page 1
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: jnoff e. Science. 2023 Nov 10;382(6671):eabo7201. doi: 10.1126/science.abo7201. Epub 2023 Nov 10. Science. 2023. PMID: 37943932 Free PMC article.
Back-up strategies in drug discovery: what, how and when?
Provins L, Jnoff E, Genicot C. Provins L, et al. Among authors: jnoff e. Drug Discov Today. 2014 Nov;19(11):1808-1811. doi: 10.1016/j.drudis.2014.07.001. Epub 2014 Jul 10. Drug Discov Today. 2014. PMID: 25017046 Review.
Binding mode and structure-activity relationships around direct inhibitors of the Nrf2-Keap1 complex.
Jnoff E, Albrecht C, Barker JJ, Barker O, Beaumont E, Bromidge S, Brookfield F, Brooks M, Bubert C, Ceska T, Corden V, Dawson G, Duclos S, Fryatt T, Genicot C, Jigorel E, Kwong J, Maghames R, Mushi I, Pike R, Sands ZA, Smith MA, Stimson CC, Courade JP. Jnoff E, et al. ChemMedChem. 2014 Apr;9(4):699-705. doi: 10.1002/cmdc.201300525. Epub 2014 Feb 6. ChemMedChem. 2014. PMID: 24504667
Discovery of selective alpha(2C) adrenergic receptor agonists.
Jnoff E, Christophe B, Collart P, Coloretti F, Debeuckelaere A, De Ryck M, Fuks B, Genicot C, Gillard M, Guyaux M, Price N, Vandergeten MC, Vermeiren C. Jnoff E, et al. ChemMedChem. 2012 Mar 5;7(3):385-90. doi: 10.1002/cmdc.201100528. Epub 2012 Jan 19. ChemMedChem. 2012. PMID: 22262529 No abstract available.
Reversible inhibition of the glycine transporter GlyT2 circumvents acute toxicity while preserving efficacy in the treatment of pain.
Mingorance-Le Meur A, Ghisdal P, Mullier B, De Ron P, Downey P, Van Der Perren C, Declercq V, Cornelis S, Famelart M, Van Asperen J, Jnoff E, Courade JP. Mingorance-Le Meur A, et al. Among authors: jnoff e. Br J Pharmacol. 2013 Nov;170(5):1053-63. doi: 10.1111/bph.12343. Br J Pharmacol. 2013. PMID: 23962079 Free PMC article.
Discovery of heterocyclic nonacetamide synaptic vesicle protein 2A (SV2A) ligands with single-digit nanomolar potency: opening avenues towards the first SV2A positron emission tomography (PET) ligands.
Mercier J, Archen L, Bollu V, Carré S, Evrard Y, Jnoff E, Kenda B, Lallemand B, Michel P, Montel F, Moureau F, Price N, Quesnel Y, Sauvage X, Valade A, Provins L. Mercier J, et al. Among authors: jnoff e. ChemMedChem. 2014 Apr;9(4):693-8. doi: 10.1002/cmdc.201300482. Epub 2014 Jan 20. ChemMedChem. 2014. PMID: 24446373
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.
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