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Cyclic peptides target the aromatic cage of a PHD-finger reader domain to modulate epigenetic protein function.
Coleman OD, Macdonald J, Thomson B, Ward JA, Stubbs CJ, McAllister TE, Clark S, Amin S, Cao Y, Abboud MI, Zhang Y, Sanganee H, Huber KVM, Claridge TDW, Kawamura A. Coleman OD, et al. Among authors: kawamura a. Chem Sci. 2023 Apr 17;14(26):7136-7146. doi: 10.1039/d2sc05944d. eCollection 2023 Jul 5. Chem Sci. 2023. PMID: 37416723 Free PMC article.
5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation.
Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JBL, King ONF, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, Lejeune C, Rydzik AM, Rose NR, Bagg EA, McDonough MA, Krojer T, Yue WW, Ng SS, Olsen L, Brennan PE, Oppermann U, Muller-Knapp S, Klose RJ, Ratcliffe PJ, Schofield CJ, Kawamura A. Hopkinson RJ, et al. Among authors: kawamura a. Chem Sci. 2013 Aug 1;4(8):3110-3117. doi: 10.1039/C3SC51122G. Chem Sci. 2013. PMID: 26682036 Free PMC article.
Recent Progress in Histone Demethylase Inhibitors.
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. McAllister TE, et al. Among authors: kawamura a. 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.
KDM4A regulates HIF-1 levels through H3K9me3.
Dobrynin G, McAllister TE, Leszczynska KB, Ramachandran S, Krieg AJ, Kawamura A, Hammond EM. Dobrynin G, et al. Among authors: kawamura a. Sci Rep. 2017 Sep 11;7(1):11094. doi: 10.1038/s41598-017-11658-3. Sci Rep. 2017. PMID: 28894274 Free PMC article.
Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7.
Gerken PA, Wolstenhulme JR, Tumber A, Hatch SB, Zhang Y, Müller S, Chandler SA, Mair B, Li F, Nijman SMB, Konietzny R, Szommer T, Yapp C, Fedorov O, Benesch JLP, Vedadi M, Kessler BM, Kawamura A, Brennan PE, Smith MD. Gerken PA, et al. Among authors: kawamura a. Angew Chem Int Ed Engl. 2017 Dec 4;56(49):15555-15559. doi: 10.1002/anie.201706788. Epub 2017 Nov 7. Angew Chem Int Ed Engl. 2017. PMID: 28976073 Free PMC article.
Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials.
Yeh TL, Leissing TM, Abboud MI, Thinnes CC, Atasoylu O, Holt-Martyn JP, Zhang D, Tumber A, Lippl K, Lohans CT, Leung IKH, Morcrette H, Clifton IJ, Claridge TDW, Kawamura A, Flashman E, Lu X, Ratcliffe PJ, Chowdhury R, Pugh CW, Schofield CJ. Yeh TL, et al. Among authors: kawamura a. Chem Sci. 2017 Nov 1;8(11):7651-7668. doi: 10.1039/c7sc02103h. Epub 2017 Sep 11. Chem Sci. 2017. PMID: 29435217 Free PMC article.
2-Oxoglutarate regulates binding of hydroxylated hypoxia-inducible factor to prolyl hydroxylase domain 2.
Abboud MI, McAllister TE, Leung IKH, Chowdhury R, Jorgensen C, Domene C, Mecinović J, Lippl K, Hancock RL, Hopkinson RJ, Kawamura A, Claridge TDW, Schofield CJ. Abboud MI, et al. Among authors: kawamura a. Chem Commun (Camb). 2018 Mar 28;54(25):3130-3133. doi: 10.1039/c8cc00387d. Epub 2018 Mar 9. Chem Commun (Camb). 2018. PMID: 29522057 Free PMC article.
1,188 results