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Discovery of holoenzyme-disrupting chemicals as substrate-selective CK2 inhibitors.
Kufareva I, Bestgen B, Brear P, Prudent R, Laudet B, Moucadel V, Ettaoussi M, Sautel CF, Krimm I, Engel M, Filhol O, Borgne ML, Lomberget T, Cochet C, Abagyan R. Kufareva I, et al. Among authors: brear p. Sci Rep. 2019 Nov 4;9(1):15893. doi: 10.1038/s41598-019-52141-5. Sci Rep. 2019. PMID: 31685885 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.
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.
Development of small cyclic peptides targeting the CK2α/β interface.
Atkinson EL, Iegre J, D'Amore C, Brear P, Salvi M, Hyvönen M, Spring DR. Atkinson EL, et al. Among authors: brear p. Chem Commun (Camb). 2022 Apr 12;58(30):4791-4794. doi: 10.1039/d2cc00707j. Chem Commun (Camb). 2022. PMID: 35343996 Free PMC article.
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.
38 results