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Specific inhibition of CK2α from an anchor outside the active site.
Brear P, De Fusco C, Hadje Georgiou K, Francis-Newton NJ, Stubbs CJ, Sore HF, Venkitaraman AR, Abell C, Spring DR, Hyvönen M. Brear P, et al. Chem Sci. 2016 Nov 1;7(11):6839-6845. doi: 10.1039/c6sc02335e. Epub 2016 Jul 12. Chem Sci. 2016. PMID: 28451126 Free PMC article.
Second-generation CK2α inhibitors targeting the αD pocket.
Iegre J, Brear P, De Fusco C, Yoshida M, Mitchell SL, Rossmann M, Carro L, Sore HF, Hyvönen M, Spring DR. Iegre J, et al. Chem Sci. 2018 Feb 20;9(11):3041-3049. doi: 10.1039/c7sc05122k. eCollection 2018 Mar 21. Chem Sci. 2018. PMID: 29732088 Free PMC article.
Novel non-ATP competitive small molecules targeting the CK2 α/β interface.
Brear P, North A, Iegre J, Hadje Georgiou K, Lubin A, Carro L, Green W, Sore HF, Hyvönen M, Spring DR. Brear P, et al. Bioorg Med Chem. 2018 Jul 15;26(11):3016-3020. doi: 10.1016/j.bmc.2018.05.011. Epub 2018 May 9. Bioorg Med Chem. 2018. PMID: 29759799 Free PMC article.
Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α.
Brear P, Ball D, Stott K, D'Arcy S, Hyvönen M. Brear P, et al. J Med Chem. 2020 Nov 12;63(21):12786-12798. doi: 10.1021/acs.jmedchem.0c01173. Epub 2020 Oct 29. J Med Chem. 2020. PMID: 33119282 Free PMC article.
Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.
Kidd SL, Fowler E, Reinhardt T, Compton T, Mateu N, Newman H, Bellini D, Talon R, McLoughlin J, Krojer T, Aimon A, Bradley A, Fairhead M, Brear P, Díaz-Sáez L, McAuley K, Sore HF, Madin A, O'Donovan DH, Huber KVM, Hyvönen M, von Delft F, Dowson CG, Spring DR. Kidd SL, et al. Chem Sci. 2020 May 14;11(39):10792-10801. doi: 10.1039/d0sc01232g. Chem Sci. 2020. PMID: 34094333 Free PMC article.
33 results