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Development of New Inhibitors of HDAC1-3 Enzymes Aided by In Silico Design Strategies.
Cheshmazar N, Hemmati S, Hamzeh-Mivehroud M, Sokouti B, Zessin M, Schutkowski M, Sippl W, Nozad Charoudeh H, Dastmalchi S. Cheshmazar N, et al. Among authors: schutkowski m. J Chem Inf Model. 2022 May 23;62(10):2387-2397. doi: 10.1021/acs.jcim.1c01557. Epub 2022 Apr 25. J Chem Inf Model. 2022. PMID: 35467871
Development of Alkylated Hydrazides as Highly Potent and Selective Class I Histone Deacetylase Inhibitors with T cell Modulatory Properties.
Sun P, Wang J, Khan KS, Yang W, Ng BW, Ilment N, Zessin M, Bülbül EF, Robaa D, Erdmann F, Schmidt M, Romier C, Schutkowski M, Cheng AS, Sippl W. Sun P, et al. Among authors: schutkowski m. J Med Chem. 2022 Dec 22;65(24):16313-16337. doi: 10.1021/acs.jmedchem.2c01132. Epub 2022 Nov 30. J Med Chem. 2022. PMID: 36449385
Potent and Selective Inhibitors of Human Sirtuin 5.
Kalbas D, Liebscher S, Nowak T, Meleshin M, Pannek M, Popp C, Alhalabi Z, Bordusa F, Sippl W, Steegborn C, Schutkowski M. Kalbas D, et al. Among authors: schutkowski m. J Med Chem. 2018 Mar 22;61(6):2460-2471. doi: 10.1021/acs.jmedchem.7b01648. Epub 2018 Mar 12. J Med Chem. 2018. PMID: 29494161
Continuous Sirtuin/HDAC (histone deacetylase) activity assay using thioamides as PET (Photoinduced Electron Transfer)-based fluorescence quencher.
Zessin M, Meleshin M, Simic Z, Kalbas D, Arbach M, Gebhardt P, Melesina J, Liebscher S, Bordusa F, Sippl W, Barinka C, Schutkowski M. Zessin M, et al. Among authors: schutkowski m. Bioorg Chem. 2021 Dec;117:105425. doi: 10.1016/j.bioorg.2021.105425. Epub 2021 Oct 12. Bioorg Chem. 2021. PMID: 34695733 Free article.
Synthesis, Molecular Docking and Biological Characterization of Pyrazine Linked 2-Aminobenzamides as New Class I Selective Histone Deacetylase (HDAC) Inhibitors with Anti-Leukemic Activity.
Ibrahim HS, Abdelsalam M, Zeyn Y, Zessin M, Mustafa AM, Fischer MA, Zeyen P, Sun P, Bülbül EF, Vecchio A, Erdmann F, Schmidt M, Robaa D, Barinka C, Romier C, Schutkowski M, Krämer OH, Sippl W. Ibrahim HS, et al. Among authors: schutkowski m. Int J Mol Sci. 2021 Dec 29;23(1):369. doi: 10.3390/ijms23010369. Int J Mol Sci. 2021. PMID: 35008795 Free PMC article.
Continuous Histone Deacylase Activity Assays.
Zessin M, Meleshin M, Sippl W, Schutkowski M. Zessin M, et al. Among authors: schutkowski m. Methods Mol Biol. 2023;2589:411-428. doi: 10.1007/978-1-0716-2788-4_27. Methods Mol Biol. 2023. PMID: 36255640
Design and synthesis of bioreductive prodrugs of class I histone deacetylase inhibitors and their biological evaluation in virally transfected acute myeloid leukemia cells.
Abdelsalam M, Zmyslia M, Schmidtkunz K, Vecchio A, Hilscher S, Ibrahim HS, Schutkowski M, Jung M, Jessen-Trefzer C, Sippl W. Abdelsalam M, et al. Among authors: schutkowski m. Arch Pharm (Weinheim). 2024 Feb;357(2):e2300536. doi: 10.1002/ardp.202300536. Epub 2023 Nov 6. Arch Pharm (Weinheim). 2024. PMID: 37932028
112 results