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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: kantsadi al. Science. 2023 Nov 10;382(6671):eabo7201. doi: 10.1126/science.abo7201. Epub 2023 Nov 10. Science. 2023. PMID: 37943932 Free PMC article.
A quinolin-8-ol sub-millimolar inhibitor of UGGT, the ER glycoprotein folding quality control checkpoint.
Guay KP, Ibba R, Kiappes JL, Vasiljević S, Bonì F, De Benedictis M, Zeni I, Le Cornu JD, Hensen M, Chandran AV, Kantsadi AL, Caputo AT, Blanco Capurro JI, Bayo Y, Hill JC, Hudson K, Lia A, Brun J, Withers SG, Martí M, Biasini E, Santino A, De Rosa M, Milani M, Modenutti CP, Hebert DN, Zitzmann N, Roversi P. Guay KP, et al. Among authors: kantsadi al. iScience. 2023 Sep 20;26(10):107919. doi: 10.1016/j.isci.2023.107919. eCollection 2023 Oct 20. iScience. 2023. PMID: 37822503 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.
Probing the β-pocket of the active site of human liver glycogen phosphorylase with 3-(C-β-d-glucopyranosyl)-5-(4-substituted-phenyl)-1, 2, 4-triazole inhibitors.
Kyriakis E, Solovou TGA, Kun S, Czifrák K, Szőcs B, Juhász L, Bokor É, Stravodimos GA, Kantsadi AL, Chatzileontiadou DSM, Skamnaki VT, Somsák L, Leonidas DD. Kyriakis E, et al. Among authors: kantsadi al. Bioorg Chem. 2018 Apr;77:485-493. doi: 10.1016/j.bioorg.2018.02.008. Epub 2018 Feb 12. Bioorg Chem. 2018. PMID: 29454281
Nanomolar Inhibitors of Glycogen Phosphorylase Based on β-d-Glucosaminyl Heterocycles: A Combined Synthetic, Enzyme Kinetic, and Protein Crystallography Study.
Bokor É, Kyriakis E, Solovou TGA, Koppány C, Kantsadi AL, Szabó KE, Szakács A, Stravodimos GA, Docsa T, Skamnaki VT, Zographos SE, Gergely P, Leonidas DD, Somsák L. Bokor É, et al. Among authors: kantsadi al. J Med Chem. 2017 Nov 22;60(22):9251-9262. doi: 10.1021/acs.jmedchem.7b01056. Epub 2017 Oct 3. J Med Chem. 2017. PMID: 28925695
26 results