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Page 1
Identification of Atuveciclib (BAY 1143572), the First Highly Selective, Clinical PTEFb/CDK9 Inhibitor for the Treatment of Cancer.
Lücking U, Scholz A, Lienau P, Siemeister G, Kosemund D, Bohlmann R, Briem H, Terebesi I, Meyer K, Prelle K, Denner K, Bömer U, Schäfer M, Eis K, Valencia R, Ince S, von Nussbaum F, Mumberg D, Ziegelbauer K, Klebl B, Choidas A, Nussbaumer P, Baumann M, Schultz-Fademrecht C, Rühter G, Eickhoff J, Brands M. Lücking U, et al. Among authors: eis k. ChemMedChem. 2017 Nov 8;12(21):1776-1793. doi: 10.1002/cmdc.201700447. Epub 2017 Oct 16. ChemMedChem. 2017. PMID: 28961375 Free PMC article.
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.
Nguyen D, Lemos C, Wortmann L, Eis K, Holton SJ, Boemer U, Moosmayer D, Eberspaecher U, Weiske J, Lechner C, Prechtl S, Suelzle D, Siegel F, Prinz F, Lesche R, Nicke B, Nowak-Reppel K, Himmel H, Mumberg D, von Nussbaum F, Nising CF, Bauser M, Haegebarth A. Nguyen D, et al. Among authors: eis k. J Med Chem. 2019 Jan 24;62(2):928-940. doi: 10.1021/acs.jmedchem.8b01606. Epub 2019 Jan 9. J Med Chem. 2019. PMID: 30563338
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Hillig RC, Sautier B, Schroeder J, Moosmayer D, Hilpmann A, Stegmann CM, Werbeck ND, Briem H, Boemer U, Weiske J, Badock V, Mastouri J, Petersen K, Siemeister G, Kahmann JD, Wegener D, Böhnke N, Eis K, Graham K, Wortmann L, von Nussbaum F, Bader B. Hillig RC, et al. Among authors: eis k. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560. doi: 10.1073/pnas.1812963116. Epub 2019 Jan 25. Proc Natl Acad Sci U S A. 2019. PMID: 30683722 Free PMC article.
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.
Lücking U, Wortmann L, Wengner AM, Lefranc J, Lienau P, Briem H, Siemeister G, Bömer U, Denner K, Schäfer M, Koppitz M, Eis K, Bartels F, Bader B, Bone W, Moosmayer D, Holton SJ, Eberspächer U, Grudzinska-Goebel J, Schatz C, Deeg G, Mumberg D, von Nussbaum F. Lücking U, et al. Among authors: eis k. J Med Chem. 2020 Jul 9;63(13):7293-7325. doi: 10.1021/acs.jmedchem.0c00369. Epub 2020 Jun 28. J Med Chem. 2020. PMID: 32502336
Identification of Small Molecules that Modulate Mutant p53 Condensation.
Lemos C, Schulze L, Weiske J, Meyer H, Braeuer N, Barak N, Eberspächer U, Werbeck N, Stresemann C, Lange M, Lesche R, Zablowsky N, Juenemann K, Kamburov A, Luh LM, Leissing TM, Mortier J, Steckel M, Steuber H, Eis K, Eheim A, Steigemann P. Lemos C, et al. Among authors: eis k. iScience. 2020 Sep 1;23(9):101517. doi: 10.1016/j.isci.2020.101517. eCollection 2020 Sep 25. iScience. 2020. PMID: 32927263 Free PMC article.
BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.
Berger M, Wortmann L, Buchgraber P, Lücking U, Zitzmann-Kolbe S, Wengner AM, Bader B, Bömer U, Briem H, Eis K, Rehwinkel H, Bartels F, Moosmayer D, Eberspächer U, Lienau P, Hammer S, Schatz CA, Wang Q, Wang Q, Mumberg D, Nising CF, Siemeister G. Berger M, et al. Among authors: eis k. J Med Chem. 2021 Sep 9;64(17):12723-12737. doi: 10.1021/acs.jmedchem.1c00762. Epub 2021 Aug 24. J Med Chem. 2021. PMID: 34428039 Free article.
Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069.
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: eis k. J Med Chem. 2022 Nov 10;65(21):14843-14863. doi: 10.1021/acs.jmedchem.2c01379. Epub 2022 Oct 21. J Med Chem. 2022. PMID: 36270630 Free PMC article.
Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Orsi DL, Ferrara SJ, Siegel S, Friberg A, Bouché L, Pook E, Lienau P, Bluck JP, Lemke CT, Akcay G, Stellfeld T, Meyer H, Pütter V, Holton SJ, Korr D, Jerchel-Furau I, Pantelidou C, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: eis k. Bioorg Med Chem. 2023 Jan 15;78:117130. doi: 10.1016/j.bmc.2022.117130. Epub 2022 Dec 13. Bioorg Med Chem. 2023. PMID: 36542958 Free article.
18 results