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Page 1
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: lienau p. 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.
Correction to "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: lienau p. J Med Chem. 2023 Jan 12;66(1):1082. doi: 10.1021/acs.jmedchem.2c02002. Epub 2022 Dec 21. J Med Chem. 2023. PMID: 36542814 Free PMC article. No abstract available.
Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling.
Graham K, Lienau P, Bader B, Prechtl S, Naujoks J, Lesche R, Weiske J, Kuehnlenz J, Brzezinka K, Potze L, Zanconato F, Nicke B, Montebaur A, Bone W, Golfier S, Kaulfuss S, Kopitz C, Pilari S, Steuber H, Hayat S, Kamburov A, Steffen A, Schlicker A, Buchgraber P, Braeuer N, Font NA, Heinrich T, Kuhnke L, Nowak-Reppel K, Stresemann C, Steigemann P, Walter AO, Blotta S, Ocker M, Lakner A, von Nussbaum F, Mumberg D, Eis K, Piccolo S, Lange M. Graham K, et al. Among authors: lienau p. Cell Chem Biol. 2024 Mar 19:S2451-9456(24)00087-4. doi: 10.1016/j.chembiol.2024.02.013. Online ahead of print. Cell Chem Biol. 2024. PMID: 38537632
Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21.
Göricke F, Vu V, Smith L, Scheib U, Böhm R, Akkilic N, Wohlfahrt G, Weiske J, Bömer U, Brzezinka K, Lindner N, Lienau P, Gradl S, Beck H, Brown PJ, Santhakumar V, Vedadi M, Barsyte-Lovejoy D, Arrowsmith CH, Schmees N, Petersen K. Göricke F, et al. Among authors: lienau p. J Med Chem. 2023 Mar 9;66(5):3431-3447. doi: 10.1021/acs.jmedchem.2c01933. Epub 2023 Feb 20. J Med Chem. 2023. PMID: 36802665 Free PMC 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: lienau p. 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 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. Among authors: lienau p. 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.
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: lienau p. 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.
Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer.
Lücking U, Kosemund D, Böhnke N, Lienau P, Siemeister G, Denner K, Bohlmann R, Briem H, Terebesi I, Bömer U, Schäfer M, Ince S, Mumberg D, Scholz A, Izumi R, Hwang S, von Nussbaum F. Lücking U, et al. Among authors: lienau p. J Med Chem. 2021 Aug 12;64(15):11651-11674. doi: 10.1021/acs.jmedchem.1c01000. Epub 2021 Jul 15. J Med Chem. 2021. PMID: 34264057
The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models.
Lemos C, Schulze VK, Baumgart SJ, Nevedomskaya E, Heinrich T, Lefranc J, Bader B, Christ CD, Briem H, Kuhnke LP, Holton SJ, Bömer U, Lienau P, von Nussbaum F, Nising CF, Bauser M, Hägebarth A, Mumberg D, Haendler B. Lemos C, et al. Among authors: lienau p. Cell Oncol (Dordr). 2021 Jun;44(3):581-594. doi: 10.1007/s13402-020-00584-8. Epub 2021 Jan 25. Cell Oncol (Dordr). 2021. PMID: 33492659
33 results