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Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.
Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, Guo J, Plotnikov A, Reznik N, Ruda GF, Díaz-Sáez L, Straub VM, Szommer T, Velupillai S, Zaidman D, Zhang Y, Coker AR, Dowson CG, Barr HM, Wang C, Huber KVM, Brennan PE, Ovaa H, von Delft F, London N. Resnick E, et al. Among authors: szommer t. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22. J Am Chem Soc. 2019. PMID: 31060360 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: szommer t. 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.
Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death.
Cottone L, Cribbs AP, Khandelwal G, Wells G, Ligammari L, Philpott M, Tumber A, Lombard P, Hookway ES, Szommer T, Johansson C, Brennan PE, Pillay N, Jenner RG, Oppermann U, Flanagan AM. Cottone L, et al. Among authors: szommer t. Cancer Res. 2020 Oct 15;80(20):4540-4551. doi: 10.1158/0008-5472.CAN-20-1387. Epub 2020 Aug 27. Cancer Res. 2020. PMID: 32855205
Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.
Balıkçı E, Marques AMC, Bauer LG, Seupel R, Bennett J, Raux B, Buchan K, Simelis K, Singh U, Rogers C, Ward J, Cheng C, Szommer T, Schützenhofer K, Elkins JM, Sloman DL, Ahel I, Fedorov O, Brennan PE, Huber KVM. Balıkçı E, et al. Among authors: szommer t. J Med Chem. 2024 May 9;67(9):7245-7259. doi: 10.1021/acs.jmedchem.4c00072. Epub 2024 Apr 18. J Med Chem. 2024. PMID: 38635563 Free PMC article.