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Page 1
Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A.
Wortmann L, Bräuer N, Holton SJ, Irlbacher H, Weiske J, Lechner C, Meier R, Karén J, Siöberg CB, Pütter V, Christ CD, Ter Laak A, Lienau P, Lesche R, Nicke B, Cheung SH, Bauser M, Haegebarth A, von Nussbaum F, Mumberg D, Lemos C. Wortmann L, et al. J Med Chem. 2021 Nov 11;64(21):15883-15911. doi: 10.1021/acs.jmedchem.1c01245. Epub 2021 Oct 26. J Med Chem. 2021. PMID: 34699202 Free 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: wortmann l. 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: wortmann l. 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.
The Novel ATR Inhibitor BAY 1895344 Is Efficacious as Monotherapy and Combined with DNA Damage-Inducing or Repair-Compromising Therapies in Preclinical Cancer Models.
Wengner AM, Siemeister G, Lücking U, Lefranc J, Wortmann L, Lienau P, Bader B, Bömer U, Moosmayer D, Eberspächer U, Golfier S, Schatz CA, Baumgart SJ, Haendler B, Lejeune P, Schlicker A, von Nussbaum F, Brands M, Ziegelbauer K, Mumberg D. Wengner AM, et al. Among authors: wortmann l. Mol Cancer Ther. 2020 Jan;19(1):26-38. doi: 10.1158/1535-7163.MCT-19-0019. Epub 2019 Oct 3. Mol Cancer Ther. 2020. PMID: 31582533
Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo.
Wortmann L, Lindenthal B, Muhn P, Walter A, Nubbemeyer R, Heldmann D, Sobek L, Morandi F, Schrey AK, Moosmayer D, Günther J, Kuhnke J, Koppitz M, Lücking U, Röhn U, Schäfer M, Nowak-Reppel K, Kühne R, Weinmann H, Langer G. Wortmann L, et al. J Med Chem. 2019 Nov 27;62(22):10321-10341. doi: 10.1021/acs.jmedchem.9b01382. Epub 2019 Nov 13. J Med Chem. 2019. PMID: 31670515
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: wortmann l. 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
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: wortmann l. 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 of a Novel Potent and Selective HSD17B13 Inhibitor, BI-3231, a Well-Characterized Chemical Probe Available for Open Science.
Thamm S, Willwacher MK, Aspnes GE, Bretschneider T, Brown NF, Buschbom-Helmke S, Fox T, Gargano EM, Grabowski D, Hoenke C, Matera D, Mueck K, Peters S, Reindl S, Riether D, Schmid M, Tautermann CS, Teitelbaum AM, Trünkle C, Veser T, Winter M, Wortmann L. Thamm S, et al. Among authors: wortmann l. J Med Chem. 2023 Feb 23;66(4):2832-2850. doi: 10.1021/acs.jmedchem.2c01884. Epub 2023 Feb 2. J Med Chem. 2023. PMID: 36727857 Free PMC article.
Localized Inhibition of Protein Phosphatase 1 by NUAK1 Promotes Spliceosome Activity and Reveals a MYC-Sensitive Feedback Control of Transcription.
Cossa G, Roeschert I, Prinz F, Baluapuri A, Silveira Vidal R, Schülein-Völk C, Chang YC, Ade CP, Mastrobuoni G, Girard C, Wortmann L, Walz S, Lührmann R, Kempa S, Kuster B, Wolf E, Mumberg D, Eilers M. Cossa G, et al. Among authors: wortmann l. Mol Cell. 2020 Mar 19;77(6):1322-1339.e11. doi: 10.1016/j.molcel.2020.01.008. Epub 2020 Jan 31. Mol Cell. 2020. PMID: 32006464 Free PMC article.
CACHE Challenge #1: Targeting the WDR Domain of LRRK2, A Parkinson's Disease Associated Protein.
Li F, Ackloo S, Arrowsmith CH, Ban F, Barden CJ, Beck H, Beránek J, Berenger F, Bolotokova A, Bret G, Breznik M, Carosati E, Chau I, Chen Y, Cherkasov A, Corte DD, Denzinger K, Dong A, Draga S, Dunn I, Edfeldt K, Edwards A, Eguida M, Eisenhuth P, Friedrich L, Fuerll A, Gardiner SS, Gentile F, Ghiabi P, Gibson E, Glavatskikh M, Gorgulla C, Guenther J, Gunnarsson A, Gusev F, Gutkin E, Halabelian L, Harding RJ, Hillisch A, Hoffer L, Hogner A, Houliston S, Irwin JJ, Isayev O, Ivanova A, Jacquemard C, Jarrett AJ, Jensen JH, Kireev D, Kleber J, Koby SB, Koes D, Kumar A, Kurnikova MG, Kutlushina A, Lessel U, Liessmann F, Liu S, Lu W, Meiler J, Mettu A, Minibaeva G, Moretti R, Morris CJ, Narangoda C, Noonan T, Obendorf L, Pach S, Pandit A, Perveen S, Poda G, Polishchuk P, Puls K, Pütter V, Rognan D, Roskams-Edris D, Schindler C, Sindt F, Spiwok V, Steinmann C, Stevens RL, Talagayev V, Tingey D, Vu O, Walters WP, Wang X, Wang Z, Wolber G, Wolf CA, Wortmann L, Zeng H, Zepeda CA, Zhang KYJ, Zhang J, Zheng S, Schapira M. Li F, et al. Among authors: wortmann l. J Chem Inf Model. 2024 Nov 25;64(22):8521-8536. doi: 10.1021/acs.jcim.4c01267. Epub 2024 Nov 5. J Chem Inf Model. 2024. PMID: 39499532
26 results