Search Results - "Szommer, Tamas"

Discovery of a Highly Selective Cell‐Active Inhibitor of the Histone Lysine Demethylases KDM2/7 by Gerken, Philip A., Wolstenhulme, Jamie R., Tumber, Anthony, Hatch, Stephanie B., Zhang, Yijia, Müller, Susanne, Chandler, Shane A., Mair, Barbara, Li, Fengling, Nijman, Sebastian M. B., Konietzny, Rebecca, Szommer, Tamas, Yapp, Clarence, Fedorov, Oleg, Benesch, Justin L. P., Vedadi, Masoud, Kessler, Benedikt M., Kawamura, Akane, Brennan, Paul E., Smith, Martin D.

“…Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell‐permeable…”
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Novel Starting Points for Human Glycolate Oxidase Inhibitors, Revealed by Crystallography-Based Fragment Screening by Mackinnon, Sabrina R, Bezerra, Gustavo A, Krojer, Tobias, Szommer, Tamas, von Delft, Frank, Brennan, Paul E, Yue, Wyatt W

“…Primary hyperoxaluria type I (PH1) is caused by AGXT gene mutations that decrease the functional activity of alanine:glyoxylate aminotransferase. A build-up of…”
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Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening by Resnick, Efrat, Bradley, Anthony, Gan, Jinrui, Douangamath, Alice, Krojer, Tobias, Sethi, Ritika, Geurink, Paul P, Aimon, Anthony, Amitai, Gabriel, Bellini, Dom, Bennett, James, Fairhead, Michael, Fedorov, Oleg, Gabizon, Ronen, Gan, Jin, Guo, Jingxu, Plotnikov, Alexander, Reznik, Nava, Ruda, Gian Filippo, Díaz-Sáez, Laura, Straub, Verena M, Szommer, Tamas, Velupillai, Srikannathasan, Zaidman, Daniel, Zhang, Yanling, Coker, Alun R, Dowson, Christopher G, Barr, Haim M, Wang, Chu, Huber, Kilian V.M, Brennan, Paul E, Ovaa, Huib, von Delft, Frank, London, Nir

“…Covalent probes can display unmatched potency, selectivity, and duration of action; however, their discovery is challenging. In principle, fragments that can…”
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Covalent Inhibitors of S100A4 Block the Formation of a Pro-Metastasis Non-Muscle Myosin 2A Complex by Giroud, Charline, Szommer, Tamas, Coxon, Carmen, Monteiro, Octovia, Grimes, Thomas, Zarganes-Tzitzikas, Tryfon, Christott, Thomas, Bennett, James, Buchan, Karly, Brennan, Paul E., Fedorov, Oleg

“…The S100 protein family functions as protein–protein interaction adaptors regulated by Ca2+ binding. Formation of various S100 complexes plays a central role…”
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Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death by Cottone, Lucia, Cribbs, Adam P, Khandelwal, Garima, Wells, Graham, Ligammari, Lorena, Philpott, Martin, Tumber, Anthony, Lombard, Patrick, Hookway, Edward S, Szommer, Tamas, Johansson, Catrine, Brennan, Paul E, Pillay, Nischalan, Jenner, Richard G, Oppermann, Udo, Flanagan, Adrienne M

“…Expression of the transcription factor brachyury (TBXT) is normally restricted to the embryo, and its silencing is epigenetically regulated. TBXT promotes…”
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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist by Balıkçı, Esra, Marques, Anne-Sophie M. C., Bauer, Ludwig G., Seupel, Raina, Bennett, James, Raux, Brigitt, Buchan, Karly, Simelis, Klemensas, Singh, Usha, Rogers, Catherine, Ward, Jennifer, Cheng, Carol, Szommer, Tamas, Schützenhofer, Kira, Elkins, Jonathan M., Sloman, David L., Ahel, Ivan, Fedorov, Oleg, Brennan, Paul E., Huber, Kilian V. M.

“…Cofactor mimicry represents an attractive strategy for the development of enzyme inhibitors but can lead to off-target effects due to the evolutionary…”
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Parallel synthesis of 1,2,4-triazole derivatives using microwave and continuous-flow techniques by Szommer, Tamás, Lukács, András, Kovács, József, Szabó, Miklós J., Hoffmann, Michael G., Schmitt, Monika H., Gerencsér, János

“…An efficient and convenient solution-phase synthesis of a 1 H -1,2,4-triazole library with potential agrochemical activity is reported employing…”
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Discovery of a Highly Selective Cell‐Active Inhibitor of the Histone Lysine Demethylases KDM2/7 by Gerken, Philip A., Wolstenhulme, Jamie R., Tumber, Anthony, Hatch, Stephanie B., Zhang, Yijia, Müller, Susanne, Chandler, Shane A., Mair, Barbara, Li, Fengling, Nijman, Sebastian M. B., Konietzny, Rebecca, Szommer, Tamas, Yapp, Clarence, Fedorov, Oleg, Benesch, Justin L. P., Vedadi, Masoud, Kessler, Benedikt M., Kawamura, Akane, Brennan, Paul E., Smith, Martin D.

“…Histone lysine demethylases (KDMs) are of critical importance in the epigenetic regulation of gene expression, yet there are few selective, cell‐permeable…”
Get full text