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220 results

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Page 1
Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, Valenti M, De Haven Brandon A, TePoele R, Leuthner B, Workman P, Aherne W, Poeschke O, Dale T, Wienke D, Esdar C, Rohdich F, Raynaud F, Clarke PA, Eccles SA, Stieber F, Schiemann K, Blagg J. Mallinger A, et al. Among authors: dale t. J Med Chem. 2015 Feb 26;58(4):1717-35. doi: 10.1021/jm501436m. Epub 2015 Feb 13. J Med Chem. 2015. PMID: 25680029 Free PMC article.
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D, Schwarz D, Schneider K, Stubbs M, Ewan K, Fraser E, TePoele R, Court W, Box G, Valenti M, de Haven Brandon A, Gowan S, Rohdich F, Raynaud F, Schneider R, Poeschke O, Blaukat A, Workman P, Schiemann K, Eccles SA, Wienke D, Blagg J. Dale T, et al. Nat Chem Biol. 2015 Dec;11(12):973-980. doi: 10.1038/nchembio.1952. Epub 2015 Oct 26. Nat Chem Biol. 2015. PMID: 26502155 Free PMC article.
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.
Mallinger A, Schiemann K, Rink C, Stieber F, Calderini M, Crumpler S, Stubbs M, Adeniji-Popoola O, Poeschke O, Busch M, Czodrowski P, Musil D, Schwarz D, Ortiz-Ruiz MJ, Schneider R, Thai C, Valenti M, de Haven Brandon A, Burke R, Workman P, Dale T, Wienke D, Clarke PA, Esdar C, Raynaud FI, Eccles SA, Rohdich F, Blagg J. Mallinger A, et al. Among authors: dale t. J Med Chem. 2016 Feb 11;59(3):1078-101. doi: 10.1021/acs.jmedchem.5b01685. Epub 2016 Jan 21. J Med Chem. 2016. PMID: 26796641 Free PMC article.
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.
Czodrowski P, Mallinger A, Wienke D, Esdar C, Pöschke O, Busch M, Rohdich F, Eccles SA, Ortiz-Ruiz MJ, Schneider R, Raynaud FI, Clarke PA, Musil D, Schwarz D, Dale T, Urbahns K, Blagg J, Schiemann K. Czodrowski P, et al. Among authors: dale t. J Med Chem. 2016 Oct 27;59(20):9337-9349. doi: 10.1021/acs.jmedchem.6b00597. Epub 2016 Oct 7. J Med Chem. 2016. PMID: 27490956 Free article.
Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases.
Clarke PA, Ortiz-Ruiz MJ, TePoele R, Adeniji-Popoola O, Box G, Court W, Czasch S, El Bawab S, Esdar C, Ewan K, Gowan S, De Haven Brandon A, Hewitt P, Hobbs SM, Kaufmann W, Mallinger A, Raynaud F, Roe T, Rohdich F, Schiemann K, Simon S, Schneider R, Valenti M, Weigt S, Blagg J, Blaukat A, Dale TC, Eccles SA, Hecht S, Urbahns K, Workman P, Wienke D. Clarke PA, et al. Among authors: dale tc. Elife. 2016 Dec 9;5:e20722. doi: 10.7554/eLife.20722. Elife. 2016. PMID: 27935476 Free PMC article.
A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription.
Ewan K, Pajak B, Stubbs M, Todd H, Barbeau O, Quevedo C, Botfield H, Young R, Ruddle R, Samuel L, Battersby A, Raynaud F, Allen N, Wilson S, Latinkic B, Workman P, McDonald E, Blagg J, Aherne W, Dale T. Ewan K, et al. Among authors: dale t. Cancer Res. 2010 Jul 15;70(14):5963-73. doi: 10.1158/0008-5472.CAN-10-1028. Epub 2010 Jul 7. Cancer Res. 2010. PMID: 20610623 Free PMC article.
3D imaging of colorectal cancer organoids identifies responses to Tankyrase inhibitors.
Badder LM, Hollins AJ, Herpers B, Yan K, Ewan KB, Thomas M, Shone JR, Badder DA, Naven M, Ashelford KE, Hargest R, Clarke AR, Esdar C, Buchstaller HP, Treherne JM, Boj S, Ramezanpour B, Wienke D, Price LS, Shaw PH, Dale TC. Badder LM, et al. PLoS One. 2020 Aug 18;15(8):e0235319. doi: 10.1371/journal.pone.0235319. eCollection 2020. PLoS One. 2020. PMID: 32810173 Free PMC article.
Wnt signalling modulates transcribed-ultraconserved regions in hepatobiliary cancers.
Carotenuto P, Fassan M, Pandolfo R, Lampis A, Vicentini C, Cascione L, Paulus-Hock V, Boulter L, Guest R, Quagliata L, Hahne JC, Ridgway R, Jamieson T, Athineos D, Veronese A, Visone R, Murgia C, Ferrari G, Guzzardo V, Evans TRJ, MacLeod M, Feng GJ, Dale T, Negrini M, Forbes SJ, Terracciano L, Scarpa A, Patel T, Valeri N, Workman P, Sansom O, Braconi C. Carotenuto P, et al. Among authors: dale t. Gut. 2017 Jul;66(7):1268-1277. doi: 10.1136/gutjnl-2016-312278. Epub 2016 Sep 12. Gut. 2017. PMID: 27618837 Free PMC article.
220 results