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Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.
Gradl S, Steuber H, Weiske J, Szewczyk MM, Schmees N, Siegel S, Stoeckigt D, Christ CD, Li F, Organ S, Abbey M, Kennedy S, Chau I, Trush V, Barsyte-Lovejoy D, Brown PJ, Vedadi M, Arrowsmith C, Husemann M, Badock V, Bauser M, Haegebarth A, Hartung IV, Stresemann C. Gradl S, et al. Among authors: siegel s. SLAS Discov. 2021 Sep;26(8):947-960. doi: 10.1177/24725552211019409. Epub 2021 Jun 21. SLAS Discov. 2021. PMID: 34154424 Free article.
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Bouché L, Christ CD, Siegel S, Fernández-Montalván AE, Holton SJ, Fedorov O, Ter Laak A, Sugawara T, Stöckigt D, Tallant C, Bennett J, Monteiro O, Díaz-Sáez L, Siejka P, Meier J, Pütter V, Weiske J, Müller S, Huber KVM, Hartung IV, Haendler B. Bouché L, et al. Among authors: siegel s. J Med Chem. 2017 May 11;60(9):4002-4022. doi: 10.1021/acs.jmedchem.7b00306. Epub 2017 May 1. J Med Chem. 2017. PMID: 28402630 Free PMC article.
Preclinical evaluation of the BET bromodomain inhibitor BAY 1238097 for the treatment of lymphoma.
Bernasconi E, Gaudio E, Lejeune P, Tarantelli C, Cascione L, Kwee I, Spriano F, Rinaldi A, Mensah AA, Chung E, Stathis A, Siegel S, Schmees N, Ocker M, Zucca E, Haendler B, Bertoni F. Bernasconi E, et al. Among authors: siegel s. Br J Haematol. 2017 Sep;178(6):936-948. doi: 10.1111/bjh.14803. Epub 2017 Jun 27. Br J Haematol. 2017. PMID: 28653353 Free article.
Characterization of the Menin-MLL Interaction as Therapeutic Cancer Target.
Brzezinka K, Nevedomskaya E, Lesche R, Haegebarth A, Ter Laak A, Fernández-Montalván AE, Eberspaecher U, Werbeck ND, Moenning U, Siegel S, Haendler B, Eheim AL, Stresemann C. Brzezinka K, et al. Among authors: siegel s. Cancers (Basel). 2020 Jan 14;12(1):201. doi: 10.3390/cancers12010201. Cancers (Basel). 2020. PMID: 31947537 Free PMC article.
Targeting BET bromodomains for cancer treatment.
Jung M, Gelato KA, Fernández-Montalván A, Siegel S, Haendler B. Jung M, et al. Among authors: siegel s. Epigenomics. 2015;7(3):487-501. doi: 10.2217/epi.14.91. Epigenomics. 2015. PMID: 26077433 Review.
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: siegel s. 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.
1,322 results