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Page 1
Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine.
Brewitz L, Dumjahn L, Zhao Y, Owen CD, Laidlaw SM, Malla TR, Nguyen D, Lukacik P, Salah E, Crawshaw AD, Warren AJ, Trincao J, Strain-Damerell C, Carroll MW, Walsh MA, Schofield CJ. Brewitz L, et al. Among authors: schofield cj. J Med Chem. 2023 Feb 23;66(4):2663-2680. doi: 10.1021/acs.jmedchem.2c01627. Epub 2023 Feb 9. J Med Chem. 2023. PMID: 36757959 Free PMC article.
Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A. Rose NR, et al. Among authors: schofield cj. J Med Chem. 2012 Jul 26;55(14):6639-43. doi: 10.1021/jm300677j. Epub 2012 Jul 11. J Med Chem. 2012. PMID: 22724510 Free PMC article.
Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors.
Leung IK, Demetriades M, Hardy AP, Lejeune C, Smart TJ, Szöllössi A, Kawamura A, Schofield CJ, Claridge TD. Leung IK, et al. Among authors: schofield cj. J Med Chem. 2013 Jan 24;56(2):547-55. doi: 10.1021/jm301583m. Epub 2013 Jan 4. J Med Chem. 2013. PMID: 23234607 Free PMC article.
On the histone lysine methyltransferase activity of fungal metabolite chaetocin.
Cherblanc FL, Chapman KL, Reid J, Borg AJ, Sundriyal S, Alcazar-Fuoli L, Bignell E, Demetriades M, Schofield CJ, DiMaggio PA Jr, Brown R, Fuchter MJ. Cherblanc FL, et al. Among authors: schofield cj. J Med Chem. 2013 Nov 14;56(21):8616-25. doi: 10.1021/jm401063r. Epub 2013 Oct 25. J Med Chem. 2013. PMID: 24099080
Recent Progress in Histone Demethylase Inhibitors.
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. McAllister TE, et al. Among authors: schofield cj. J Med Chem. 2016 Feb 25;59(4):1308-29. doi: 10.1021/acs.jmedchem.5b01758. Epub 2016 Feb 2. J Med Chem. 2016. PMID: 26710088 Review.
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: schofield cj. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
770 results