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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: esdar c. 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.
Fragment-based discovery of focal adhesion kinase inhibitors.
Grädler U, Bomke J, Musil D, Dresing V, Lehmann M, Hölzemann G, Greiner H, Esdar C, Krier M, Heinrich T. Grädler U, et al. Among authors: esdar c. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5401-9. doi: 10.1016/j.bmcl.2013.07.050. Epub 2013 Jul 31. Bioorg Med Chem Lett. 2013. PMID: 23973211
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. Among authors: esdar c. 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: esdar c. 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.
Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.
Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J. Schiemann K, et al. Among authors: esdar c. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1443-51. doi: 10.1016/j.bmcl.2016.01.062. Epub 2016 Jan 22. Bioorg Med Chem Lett. 2016. PMID: 26852363
Discovery of novel 7-azaindoles as PDK1 inhibitors.
Wucherer-Plietker M, Merkul E, Müller TJJ, Esdar C, Knöchel T, Heinrich T, Buchstaller HP, Greiner H, Dorsch D, Finsinger D, Calderini M, Bruge D, Grädler U. Wucherer-Plietker M, et al. Among authors: esdar c. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3073-3080. doi: 10.1016/j.bmcl.2016.05.005. Epub 2016 May 4. Bioorg Med Chem Lett. 2016. PMID: 27217002
2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R, Schwarz D, Musil D, Burke R, Urbahns K, Workman P, Wienke D, Clarke PA, Raynaud FI, Eccles SA, Esdar C, Rohdich F, Blagg J. Mallinger A, et al. Among authors: esdar c. ACS Med Chem Lett. 2016 Mar 28;7(6):573-8. doi: 10.1021/acsmedchemlett.6b00022. eCollection 2016 Jun 9. ACS Med Chem Lett. 2016. PMID: 27326329 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: esdar c. 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: esdar c. Elife. 2016 Dec 9;5:e20722. doi: 10.7554/eLife.20722. Elife. 2016. PMID: 27935476 Free PMC article.
35 results